Functionalized PLA polymers to control loading and/or release properties of drug-loaded nanoparticles
In this study, we sought to show the possibility of influencing these properties by modifying the structure of the constituting polymer. Seven non-functionalized or functionalized PLA polymers were specifically designed and synthesized by microwave-assisted ring-opening polymerization of d,l-lactide. They presented short hydrophobic and/or hydrophilic groups thanks to the use of C20 aliphatic chain, mPEG1000, sorbitan esters (Spans®) or polysorbates (Tweens®), their PEGylated analogues, as initiators. Then, seven types of drug-loaded nanoparticles (NP) were prepared from these polymers and compared in terms of phys...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Influence of cholesterol inclusion on the doxorubicin release characteristics of lysolipid-based thermosensitive liposomes
Publication date: Available online 7 November 2017Source: International Journal of PharmaceuticsAuthor(s): Negar Sadeghi, Roel Deckers, Burcin Ozbakir, Sohail Akthar, Robbert Jan Kok, Twan Lammers, Gert StormAbstractFast hyperthermia (i.e. 39–42 °C) triggered doxorubicin release from lysolipid-containing thermosensitive liposomes (LTSL) in the tumor vasculature has been demonstrated to result in considerable enhancement of bioavailable drug levels in heated tumor tissue in preclinical tumor models. However, there is also significant leakage of doxorubicin already at 37 °C in the bloodstream, mak...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Relationship between polarities of antibiotic and polymer matrix on nanoparticle formulations based on aliphatic polyesters
Publication date: Available online 11 November 2017Source: International Journal of PharmaceuticsAuthor(s): J.A.S. Ritsema, E.M.A. Herschberg, S.E. Borgos, C. Løvmo, R. Schmid, Y.M. te Welscher, G. Storm, C.F. van NostrumAbstractIn the field of nanomedicine, nanoparticles are developed to target antibiotics to sites of bacterial infection thus enabling adequate drug exposure and decrease development of resistant bacteria. In the present study, we investigated the encapsulation of two antibiotics with different polarity into different PEGylated polymeric nanoparticles based on aliphatic polyesters, to obtain a better...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Critical evaluation of quantification methods for oligonucleotides formulated in lipid nanoparticles
Publication date: Available online 21 December 2017Source: International Journal of PharmaceuticsAuthor(s): Erik Oude Blenke, Martijn J.W. Evers, Volker Baumann, Johannes Winkler, Gert Storm, Enrico MastrobattistaAbstractThere is a very large variety in the types of nanoparticulate lipid formulations for oligonucleotides, and remarkably, also a very large heterogeneity in the methods that are used for analyzing oligonucleotide load, encapsulation efficiency and oligonucleotide release. Furthermore, a literature survey showed that the extent to which these procedures are reported in scientific literature varies greatly, wit...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Tablets made from paper
Publication date: Available online 1 June 2018Source: International Journal of PharmaceuticsAuthor(s): Florian Stumpf, Cornelia M. KeckAbstractThe possibility to compress ordinary paper into tablets was systematically investigated in this study. Results proved that tablets can be made from paper, independent of the type of paper used. The tablets appear shiny and with a smooth surface. The pharmaceutical quality was acceptable, i.e. all tablets fulfilled the requirements for tablets according to the European Pharmacopeia. Drug-loaded tablets were produced by compression of drug-loaded paper. Drug loading did not alter the ...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Selected contributions from the 10th European Workshop on Particulate Systems, Copenhagen 19th–20th January 2017
Publication date: Available online 6 June 2018Source: International Journal of PharmaceuticsAuthor(s): C. Foged (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Monoolein cubic phases containing cinnamic acid, poly(ethyleneimine) and gold nanoparticle and their UV- and NIR-responsive release property
Publication date: Available online 19 June 2018Source: International Journal of PharmaceuticsAuthor(s): Danbi Park, Jin-Chul KimAbstractUV and NIR-responsive monoolein cubic phase was prepared by including poly(ethyleneimine) (PEI)/cinnamic acid (CA) conjugate and gold nanoparticle (GNP) within its structure. UV irradiation elevated significantly the release % of Auramine O loaded in cubic phase containing PEI/CA, possibly because of the trans-to-cis isomerization of CA. NIR irradiation also increased significantly the release % of FITC-dextran loaded in cubic phase containing PEI/CA. The release % of the dye loaded in cub...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Exploring gastric drug absorption in fasted and fed state rats
In this study, an in situ gastric bolus administration model was used to study the gastric absorption of pharmaceutical compounds in fasted and fed state rats. Three drugs [paracetamol (neutral), diclofenac (acidic) and posaconazole (basic)] were administered directly into the stomach as solution (paracetamol and diclofenac) or suspension (posaconazole). Transfer to the intestine was blocked by ligating the pylorus; as a reference, non-ligated conditions were used. Blood samples were collected and gastric absorption was assessed by the appearance of compounds in the systemic circulation. Paracetamol and diclofenac were rea...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Direct Quantification of Unencapsulated Doxorubicin in Liposomal Doxorubicin Formulations Using Capillary Electrophoresis
In this study, a capillary electrophoresis (CE) with UV-Vis detection method was developed for the simultaneous separation and quantification of unencapsulated drug from liposome-associated drug using a doxorubicin-containing liposome formulation as the model drug. CE separates the unencapsulated drug and liposomal drugs based on their electrophoretic mobility under the electric field. Liposomal drugs were diluted to the appropriate concentrations with running buffer or 5% dextrose before hydrodynamic sample injection. Using a high-sensitivity detection cell, the doxorubicin detection sensitivity was enhanced about 10-fold...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Optical diagnostics studies of air flow and powder fluidisation in Nexthaler® Part II: Use of fluorescent imaging to characterise transient release of fines from a dry powder inhaler
Publication date: Available online 11 July 2018Source: International Journal of PharmaceuticsAuthor(s): C. Merusi, G. Brambilla, E.J. Long, G.K. Hargrave, H.K. VersteegAbstractThe fine particle fraction is a key indicator of therapeutic effectiveness of inhaled pharmaceutical aerosols. This paper presents a fluorescence imaging technique to visualise and characterise the emission of active pharmaceutical ingredient (API) fines in model formulations containing coarse lactose carrier and 1.5-2 μm diameter fluorescent microspheres (model API fines). A two-camera arrangement was used to acquire simultaneous images of spatia...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of processing parameters and controlled environment storage on the disproportionation and dissolution of extended release capsule of phenytoin sodium
In conclusion, our studies indicated significant effect of process variables and stability conditions on the critical quality attributes of PS extended release capsule that has potential impact on the clinical performance of the product.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Effective sustained release of 5-FU-loaded PLGA implant for improving therapeutic index of 5-FU in colon tumor
In this study, a biodegradable implant composed of poly(lactide co-glycolide) (PLGA) and 5-fluorouracil (5-FU) was fabricated by mold method and used to impede the colon cancer via the local sustained release of 5-FU after transplanting into the peritoneal cavity. To optimize the 5-FU-implant, different factors such type of polymer, polymer-drug ratio, hydrophilic additives and organic solvents were investigated based on in vitro 5-FU release behavior. The optimized 5-FU-implant was subjected to evaluate the capacity of sustained release of 5-FU in vitro and in vivo. In addition, the pharmacokinetics and bio-distribution o...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Drug Metabolites and their Effects on the Development of Adverse Reactions: Revisiting Lipinski’s Rule of Five
Publication date: Available online 21 July 2018Source: International Journal of PharmaceuticsAuthor(s): Caroline Manto Chagas, Sara Moss, Laleh AlisaraieAbstractMany studies have shown that toxicities of anticancer drugs and their adverse effects are related to their chemical structure and high molecular weight that may result in a number of metabolites interacting with drug off-target networks. These factors require further attention for advancing cancer treatment and decreasing toxicities caused by the molecular complexity of antineoplastic agents. Providing more target-selective and tolerable cancer therapy with fewer s...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Development of a Hollow Mesoporous Silica Nanoparticles Vaccine to Protect Against House Dust mite Induced Allergic Inflammation
Publication date: Available online 21 July 2018Source: International Journal of PharmaceuticsAuthor(s): Xia Peng, Yuting Liang, Yue Yin, Huanjin Liao, Li LiAbstractAllergen specific immunotherapy (SIT) is the only specific therapeutic way for house dust mite (HDM) allergy. To improve the efficacy of SIT, hollow mesoporous silica nanoparticles (HMSNs) were used as vehicles for HDM allergen. The HMSNs were prepared and characterized. The major HDM allergen (Der f2) was loaded onto HMSNs, and the drug loading capacity and release profile were determined. Then the Der f2 loaded HMSNs were injected subcutaneously to mouse model...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Curcumin-entrapped MUC-1 aptamer targeted dendrimer-gold hybrid nanostructure as a theranostic system for colon adenocarcinoma
Publication date: Available online 23 July 2018Source: International Journal of PharmaceuticsAuthor(s): Mona Alibolandi, Fazileh Hoseini, Marzieh Mohammadi, Pouria Ramezani, Elham Einafshar, Seyed Mohammad Taghdisi, Mohammad Ramezani, Khalil AbnousAbstractGold NPs have great potential in biomedical applications. PAMAM dendrimers are spherical, hyper branched macromolecules which can encapsulate therapeutic molecules while stabilizing metal nanoparticle such as gold NPs. The aim of the current study was to investigate the theranostic capability of curcumin-loaded dendrimer-gold hybrid structure.Dendrimer-gold hybrid structu...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Design and characterisation of a dissolving microneedle patch for intradermal vaccination with heat-inactivated bacteria: A proof of concept study
Publication date: Available online 23 July 2018Source: International Journal of PharmaceuticsAuthor(s): Aoife M. Rodgers, Maelíosa T.C. McCrudden, Eva.M. Vincente-Perez, Alice V. Dubois, Rebecca J. Ingram, Eneko Larrañeta, Adrien Kissenpfennig, Ryan F. DonnellyAbstractThis work describes the formulation and evaluation of dissolving microneedle patches (MNs) for intradermal delivery of heat-inactivated bacteria. Pseudomonas aeruginosa, strain PA01, was used as a model bacterium. Utilising a simple, cost effective fabrication process, P. aeruginosa was heat-inactivated and formulated into dissolving MNs, fabric...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Prussian blue nanoparticles: Synthesis, surface modification, and application in cancer treatment
Publication date: Available online 24 July 2018Source: International Journal of PharmaceuticsAuthor(s): Milan Gautam, Kishwor Poudel, Chul Soon Yong, Jong Oh KimAbstractThis review outlines recently developed Prussian blue nanoparticle (PB NPs)-based multimodal imaging-guided chemo-photothermal strategies for cancer diagnosis and treatment in order to provide insight into the future of the field. The primary limitation of existing therapeutics is the lack of selectivity in drug delivery: they target healthy and cancerous cells alike. In this paper, we provide a thorough review of diverse synthetic and surface engineering t...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Dosing considerations for inhaled biologics
Publication date: Available online 24 July 2018Source: International Journal of PharmaceuticsAuthor(s): Silvia Ferrati, Tian Wu, Sekhar R. Kanapuram, Hugh D.C. SmythAbstractThe number of biologics in the therapeutic development pipeline is increasing including those delivered though inhalation (Morales, 2017, Fathe, 2016). Biologics comprise a broad variety of complex macromolecules with unique physicochemical characteristics. These distinctive characteristics control their pharmacological mechanisms of action, stability, and ultimately affect their processing, formulation, and delivery requirements. This review systematic...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Intravaginal rings for continuous low-dose administration of cervical ripening agents
Publication date: Available online 24 July 2018Source: International Journal of PharmaceuticsAuthor(s): Yujing Wang, Peter Boyd, Alyson Hunter, R. Karl MalcolmAbstractIntravaginal rings (VRs) have been widely reported for administration of pharmaceutical drugs – most notably estrogens, progestogens and antiretrovirals – to the vagina for clinical benefit. Here, for the first time, we describe the design, manufacture and preclinical testing of VRs for sustained/controlled release of the cervical ripening agents isosorbide mononitrate (ISMN) and misoprostol (MP), either singly or in combination. Matrix-type silic...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Novel Skin Penetrating Berberine Oleate Complex Capitalizing on Hydrophobic Ion Pairing Approach
Publication date: Available online 24 July 2018Source: International Journal of PharmaceuticsAuthor(s): Abrar S. Torky, May S. Freag, Maha M.A. Nasra, Ossama Y. AbdallahAbstractBerberine hydrochloride (Brb) is a well-known herbal drug that holds a great promise in the recent years thanks to its various pharmacological actions. Currently, Brb is extensively researched as a natural surrogate with evidenced potentiality against numerous types of skin diseases including skin cancer. However, Brb’s high aqueous solubility and limited permeability hinder its clinical topical application. In the current work, to enhance Brb...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Ciclesonide and budesonide suspensions for nebulization delivery: An in vivo inhalation biopharmaceutics investigation
In this study, the main objective was to investigate the in vivo inhalation biopharmaceutics in the aspects of dissolution, mucociliary clearance, absorption and tissue binding using intratracheally administered budesonide and ciclesonide suspensions as model drugs. In doing so, this study first developed a method to differentiate between dissolved and undissolved ciclesonide in the lungs for evaluating in vivo dissolution. Following deposited in rat airways, the drug particles underwent rapid dissolution and mucociliary clearance, leading to the complete removal of drugs from the airways within 2 h and a limited absorpt...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Facile continuous production of soy peptide nanogels via nanoscale flash desolvation for drug entrapment
Publication date: 5 October 2018Source: International Journal of Pharmaceutics, Volume 549, Issues 1–2Author(s): Li-Ju Wang, Yu-Chung Chang, Allison T. Osmanson, Jinwen Zhang, Lei LiAbstractA facile continuous production of soy peptide nanogels was demonstrated using a multi-inlet vortex micromixer for the entrapment of active ingredients. The full flow regime in the micromixer was systematically studied to understand the flow impact on nanogel size, drug encapsulation efficiency and drug loading efficiency. Ibuprofen was chosen as a model drug to demonstrate encapsulation capability. The study showed that the nanoge...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

A multifunctional ternary Cu(II)-carboxylate coordination polymeric nanocomplex for cancer thermochemotherapy
This study demonstrated that the Cu(II)-carboxylate coordination nanocomplex is a promising new effective and facilely prepared thermochemotherapy agent for combination therapy against cancer.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Corrigendum to “In vitro and preclinical assessment of an intranasal spray formulation of parathyroid hormone PTH 1–34 for the treatment of osteoporosis” [Int. J. Pharm. 535 (2018) 113–119]
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Allan J. Williams, Faron Jordan, Gareth King, Andrew L. Lewis, Lisbeth Illum, Tahir Masud, Alan C. Perkins, Richard G. Pearson (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 20, 2018 Category: Drugs & Pharmacology Source Type: research

Exploring the role of polymeric conjugates toward anti-cancer drug delivery: Current trends and future projections
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Junaid Khan, Amit Alexander, Ajazuddin, Swarnlata Saraf, Shailendra SarafAbstractUtilizing the diverse features of biocompatible polymers to target drugs into the tumor/s has been a research hotspot since last decade. Such polymeric conjugates of anti-cancer drugs have proven their potential in providing sustained release of drugs with reduced systemic toxicity and improved tumor retention. Polymers like polyethylene glycol (PEG), N-(2-Hydroxypropyl) methacrylamide (HPMA), Polylactic-co-glycolic acid (PLGA), Poly...
Source: International Journal of Pharmaceutics - July 18, 2018 Category: Drugs & Pharmacology Source Type: research

Design-oriented regression models for H2O2 decontamination processes in sterile drug product manufacturing considering rapidity and sterility
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Keisho Yabuta, Haruka Futamura, Koji Kawasaki, Masahiko Hirao, Hirokazu SugiyamaAbstractWe developed regression models for designing rapid and effective H2O2 decontamination processes in the manufacturing of sterile drug products such as injectables. Decontamination, which is typically performed by using H2O2, is a critical changeover process used to establish a sterile environment for filling products. In the process, there is a trade-off relationship between the duration of the process and the level of sterilit...
Source: International Journal of Pharmaceutics - July 18, 2018 Category: Drugs & Pharmacology Source Type: research

Dermal delivery of Fe-chlorophyllin via ultradeformable nanovesicles for photodynamic therapy in melanoma animal model
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Mai Rady, Iman Gomaa, Nagia Afifi, Mahmoud Abdel-KaderAbstractMelanoma is resistant to chemotherapeutics with poor prognosis and high potential of metastasis. Photodynamic therapy (PDT) represents a localized therapeutic modality, as cytotoxicity occurs when light activates photosensitizer (PS) at the tumour site. The aim of this study is dermal delivery of a high molecular weight hydrophilic photosensitizer (PS), ferrous chlorophyllin (Fe-CHL) via transethosomes for treatment of melanoma by PDT.Transethosomes we...
Source: International Journal of Pharmaceutics - July 18, 2018 Category: Drugs & Pharmacology Source Type: research

Post-resection treatment of glioblastoma with an injectable nanomedicine-loaded photopolymerizable hydrogel induces long-term survival
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Mengnan Zhao, Fabienne Danhier, Chiara Bastiancich, Nicolas Joudiou, Lakshmi Pallavi Ganipineni, Nikolaos Tsakiris, Bernard Gallez, Anne des Rieux, Aleksandar Jankovski, John Bianco, Véronique PréatAbstractGlioblastoma multiforme (GBM) is the most common primary malignant brain tumor. Despite available therapeutic options, the prognosis for patients with GBM remains very poor. We hypothesized that the intra-operative injection of a photopolymerizable hydrogel into the tumor resection cavity could su...
Source: International Journal of Pharmaceutics - July 18, 2018 Category: Drugs & Pharmacology Source Type: research

Microfluidic-assisted nanoprecipitation of (PEGylated) poly (d,l-lactic acid-co-caprolactone): Effect of macromolecular and microfluidic parameters on particle size and paclitaxel encapsulation
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Enrique Lallana, Roberto Donno, Davide Magrì, Katie Barker, Zahid Nazir, Kevin Treacher, M. Jayne Lawrence, Marianne Ashford, Nicola TirelliAbstractIn this work we evaluate the effect of polymer composition and architecture of (PEGylated) polyesters on particle size and paclitaxel (PTX) loading for particles manufactured via microfluidic-assisted, continuous-flow nanoprecipitation using two microfluidic chips with different geometries and mixing principles.We have prepared poly (d,l-lactic acid-co-caprolac...
Source: International Journal of Pharmaceutics - July 18, 2018 Category: Drugs & Pharmacology Source Type: research

Predicting physical stability of ternary amorphous solid dispersions using specific mechanical energy in a hot melt extrusion process
This study focuses on the relationship between drug dissolution properties, physical stability against recrystallization, and specific mechanical energy (SME) from a hot melt extrusion (HME) process of ternary amorphous solid dispersions (ASDs) containing indomethacin (IND), HPMC and mesoporous silica (XDP) prepared using different HME screw condition (the number of kneading zones/rotation speed). The screw condition greatly influenced the amorphous characteristics of the processed material and SME values. The higher SME samples demonstrated a larger parachute effect in dissolution test and reduced the rate of recrystalliz...
Source: International Journal of Pharmaceutics - July 18, 2018 Category: Drugs & Pharmacology Source Type: research

Multi-drug delivery system based on lipid membrane mimetic coated nano-hydroxyapatite formulations
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Damián Placente, Luciano A. Benedini, Mónica Baldini, Juan A. Laiuppa, Graciela E. Santillán, Paula V. MessinaAbstractLocal delivery systems from an osteoconductive biomaterial are suggested as a promising strategy to avoid simultaneously peri-implant traumas and to induce tissue regeneration. In this work, it is detailed the design and construction of a multi-drug delivery formulation based on lipid membrane mimetic coated nano-hydroxyapatite, LMm/nano-HA, as a bone-specific drug delivery ap...
Source: International Journal of Pharmaceutics - July 18, 2018 Category: Drugs & Pharmacology Source Type: research

Improvement of cutaneous delivery of methylene blue by liquid crystals
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Maria Teresa Junqueira Garcia, Thalita Pedralino Gonçalves, Éricka São Félix Martins, Tereza Silva Martins, Márcia Carvalho de Abreu Fantini, Paulo Roberto Regazi Minarini, Sandra Costa Fernandez, Giovanna Cassone Salata, Luciana Biagini LopesAbstractThe purpose of this study was to evaluate the effect of composition and characteristics of liquid crystalline phases (LCPs) on cutaneous delivery of methylene blue (MB). LCPs were obtained by mixing Brij97® with water at various...
Source: International Journal of Pharmaceutics - July 18, 2018 Category: Drugs & Pharmacology Source Type: research

Composite particle formulations of colistin and meropenem with improved in-vitro bacterial killing and aerosolization for inhalation
In conclusion, our results show that co-spray drying with colistin improves the antibacterial activity and aerosol performance of meropenem and produces a formulation with synergistic bacterial killing.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 13, 2018 Category: Drugs & Pharmacology Source Type: research

Challenges for pulmonary delivery of high powder doses
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Imco Sibum, Paul Hagedoorn, Anne Haaije de Boer, Henderik Willem Frijlink, Floris GrasmeijerAbstractIn recent years there is an increasing interest in the pulmonary delivery of large cohesive powder doses, i.e. drugs with a low potency such as antibiotics or drugs with a high potency that need a substantial fraction of excipient(s) such as vaccines stabilized in sugar glasses. The pulmonary delivery of high powder doses comes with unique challenges. For low potency drugs, the use of excipients should be minimized...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

A practical framework for implementing Quality by Design to the development of topical drug products: Nanosystem-based dosage forms
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Ana Simões, Francisco Veiga, Ana Figueiras, Carla VitorinoAbstractSkin has been increasingly recognized as an important drug administration route with topical formulations, offering a targeted approach for the treatment of several dermatological disorders. The effectiveness of this route is hampered by its natural barrier, the stratum corneum (SC), and hence, different strategies have been investigated to improve percutaneous drug transport. The design of nanodelivery systems, aiming at solving skin delive...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

All disease begins in the gut: Influence of gastrointestinal disorders and surgery on oral drug performance
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Grace B. Hatton, Christine M. Madla, Sarit C. Rabbie, Abdul W. BasitAbstractThe term “disease” conjures a plethora of graphic imagery for many, and the use of drugs to combat symptoms and treat underlying pathology is at the core of modern medicine. However, the effects of the various gastrointestinal diseases, infections, co-morbidities and the impact of gastrointestinal surgery on the pharmacokinetic and pharmacodynamic behaviour of drugs have been largely overlooked. The better elucidation of disea...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

Surface-dependent endocytosis of poly(isobutylcyanoacrylate) nanoparticles by Trichomonas vaginalis
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Sophia Malli, Christian Bories, Mickaël Bourge, Philippe.M. Loiseau, Kawthar BouchemalAbstractPrevious data from our research group showed that chitosan-coated poly(isobutylcyanoacrylate) nanoparticles (NPs) (denoted PIBCA/Chito20) exhibited intrinsic anti-Trichomonas vaginalis activity, while PIBCA/pluronic® F68 without chitosan (PIBCA/F68) were inactive. However, the mechanism of anti-T. vaginalis activity of chitosan-coated PIBCA NPs is still unknown. Our hypothesis is that chitosan-coated NPs are int...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

Characterization of a smart pH-cleavable PEG polymer towards the development of dual pH-sensitive liposomes
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Manju Kanamala, Brian D. Palmer, William R. Wilson, Zimei WuAbstractTo facilitate the development of PEG-cleavable pH-sensitive liposomes (CL-pPSL), this study aimed to fully characterize a new pH-sensitive polymer, PEGB-Hz-CHEMS. Polyethylene glycol (PEG) functionalised with 4-carboxybenzaldehyde (PEGB) was linked to cholesteryl hemisuccinate (CHEMS) via an acid labile hydrazide–hydrazone hybrid bond (CONHNCH) to form PEGB-Hz-CHEMS. The polymer was post-inserted into DOPE/CHEMS liposomes to form CL-pPSL. A...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

Lipid-coated superparamagnetic nanoparticles for thermoresponsive cancer treatment
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Ayat A. Allam, Sarah J. Potter, Sergey L. Bud'ko, Donglu Shi, Dina F. Mohamed, Fawzia S. Habib, Giovanni M. PaulettiAbstractPoor aqueous solubility, chemical instability, and indiscriminate cytotoxicity have limited clinical development of camptothecin (CPT) as potent anticancer therapeutic. This research aimed at fabricating thermoresponsive nanocomposites that enhance solubility and stability of CPT in aqueous milieu and enable stimulus-induced drug release using magnetic hyperthermia. 1,2-Dipalmitoyl-sn-glycer...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

A modified USP induction port to characterize nasal spray plume geometry and predict turbinate deposition under flow
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Daniel Moraga-Espinoza, Zachary Warnken, Amanda Moore, Robert O. Williams, Hugh D.C. SmythAbstractThere is currently no in vitro technique for assessing plume geometry of nasal sprays under airflow conditions. However, a majority of FDA approved nasal products recommend that patients inhale during actuation. Therefore, a reproducible in vitro test that measures plume angles under physiologically relevant inhalation flow rates would be useful. The purpose of this study was to adapt the recently described Plume Ind...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

Deciphering magnesium stearate thermotropic behavior
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Rahul V. Haware, Bhavani Prasad Vinjamuri, Amrita Sarkar, Morgan Stefik, William C. StagnerAbstractMagnesium stearate (MgSt) is the most commonly used excipient for oral solid dosage forms, yet there is significant commercial physicochemical variability that can lead to variable performance of critical product attributes. Differential scanning calorimetry (DSC) is often used as a quality control tool to characterize MgSt, but little data is available regarding the physicochemical relevance for the DSC thermograms...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

In-situ forming PLGA implants for intraocular dexamethasone delivery
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): C. Bode, H. Kranz, F. Siepmann, J. SiepmannAbstractDifferent types of in-situ forming implants based on poly(lactic-co-glycolic acid) (PLGA) and N-methyl-pyrrolidone (NMP) were prepared for controlled ocular delivery of dexamethasone. The impact of the volume of the release medium, initial drug content, polymer molecular weight and PLGA concentration on the resulting drug release kinetics were studied and explained based on a thorough physico-chemical characterization of the systems. This included for instance th...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

Development of customised 3D printed biodegradable projectile for administrating extended-release contraceptive to wildlife
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Jingjunjiao Long, Ashveen V. Nand, Sudip Ray, Sam Mayhew, David White, Craig R. Bunt, Ali SeyfoddinAbstractCustomisation of sustained and controlled release of contraceptives plays a key role in veterinary applications. A biodegradable projectile containing different doses of contraceptive progesterone was prepared using fused deposition modelling 3D printing. Three concentrations of progesterone (2, 5 and 10% w/w) with polylactic acid was prepared as a 1.75 mm filament by hot melt extrusion. Solvent dissolutio...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

Preparation of novel phospholipid-based sonocomplexes for improved intestinal permeability of rosuvastatin: In vitro characterization, dynamic simulation, Caco-2 cell line permeation and in vivo assessment studies
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Wessam Hamdy Abd-Elsalam, Sara Nageeb El-Helaly, Mohammed Abdallah Ahmed, Abdulaziz Mohsen Al-mahallawiAbstractThe study aimed to fabricate innovative drug-phospholipid complexes termed “sonocomplexes” adopting ultrasound irradiation to increase the liposolubility and to enhance the intestinal absorption of rosuvastatin as a model drug for BCS class III active pharmaceutical ingredients (APIs). A 22 full factorial design was fashioned to investigate the influence of phosphatidylcholine content in the ...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

Assessment of hot-processability and performance of ethylcellulose-based materials for injection-molded prolonged-release systems: An investigational approach
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): F. Casati, F. Briatico-Vangosa, F. Baldi, A. Melocchi, A. Maroni, A. Gazzaniga, L. ZemaAbstractThe present work focuses on application of an investigational approach to assess the hot-processability of pharmaceutical-grade polymers with a potential for use in the manufacturing of reservoir drug delivery systems via micromolding, and the performance of resulting molded barriers. An inert thermoplastic polymer, ethylcellulose (EC), widely exploited for preparation of prolonged-release systems, was employed as a mod...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

Self-microemulsifying tablets prepared by direct compression for improved resveratrol delivery
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Katarina Bolko Seljak, Ilija German Ilić, Mirjana Gašperlin, Alenka Zvonar PobirkAbstractThe purpose of this study was to develop self-microemulsifying (SME-) tablets to improve resveratrol solubility whilst delivering resveratrol in a preferred tablet dosage form. Resveratrol was dissolved in liquid self-microemulsifying drug delivery system (SMEDDS) (10% w/w) and solidified through adsorption on several different solid carriers. Two ranges of synthetic amorphous silica (Sylysia® 290, 350, 470, 580; ...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

Preparation of spray dried submicron particles: Part A – Particle generation by aerosol conditioning
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Ramona Strob, Adrian Dobrowolski, Gerhard Schaldach, Peter Walzel, Markus ThommesAbstractThe preparation of submicron-sized particles is relevant in chemical, food and pharmaceutical applications. In pharmaceutics, spray dried submicron-sized particles (0.1–1 µm) can increase the dissolution rate as well as the solubility of poorly water-soluble drugs. Since the particle size during spray drying is mainly influenced by the droplet size, the preparation of uniform droplets smaller than 3 µm i...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

Implication of linker length on cell cytotoxicity, pharmacokinetic and toxicity profile of gemcitabine-docetaxel combinatorial dual drug conjugate
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Varun Kushwah, Sameer S. Katiyar, Ashish Kumar Agrawal, Isha Saraf, Inder Pal Singh, Dimitrios A. Lamprou, Ramesh C. Gupta, Sanyog JainAbstractThe present study investigates effect of linkers [zero length (without linker), short length linker (glycine and lysine) and long length linker (PEG1000, PEG2000 and PEG3500)] on pharmacokinetics and toxicity of docetaxel (DTX) and gemcitabine (GEM) bio-conjugates. Conjugates were synthesized via carbodiimide chemistry and characterized by 1H NMR and FTIR. Conjugation of D...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

Predicting Physical Stability of Ternary Amorphous Solid Dispersion Using Specific Mechanical Energy in a Hot Melt Extrusion Process
This study focuses on the relationship between drug dissolution properties, physical stability against recrystallization, and specific mechanical energy (SME) from a hot melt extrusion (HME) process of ternary amorphous solid dispersions (ASDs) containing indomethacin (IND), HPMC and mesoporous silica (XDP) prepared using different HME screw condition (the number of kneading zones /rotation speed). The screw condition greatly influenced the amorphous characteristics of the processed material and SME values. The higher SME samples demonstrated a larger parachute effect in dissolution test and reduced the rate of recrystalli...
Source: International Journal of Pharmaceutics - July 11, 2018 Category: Drugs & Pharmacology Source Type: research

Amorphous Magnesium Carbonate Nanoparticles with Strong Stabilizing Capability for Amorphous Ibuprofen
This study demonstrates, for the first time, the ability to stabilize an API in the amorphous state using a solid dispersion of magnesium carbonate nanoparticles within the API. Specifically, high proportions of ibuprofen were able to be stabilized in the amorphous state using as little as 17% wt/wt amorphous magnesium carbonate nanoparticles, and drug release rates 83 times faster than from the crystalline state were achieved. Biocompatibility of the nanoparticles was demonstrated in vitro using Human dermal fibroblasts and stability of the nanocomposite formulation was verified with a storage time of six months. The succ...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research