Surface area normalized dissolution to study differences in itraconazole-copovidone solid dispersions prepared by spray-drying and hot melt extrusion
This study provides insight into the complex interplay between formulation, processing and performance of amorphous solid dispersion systems. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Comparison of two DSC-based methods to predict drug-polymer solubility
Publication date: 5 April 2018 Source:International Journal of Pharmaceutics, Volume 540, Issues 1–2 Author(s): Malte Bille Rask, Matthias Manne Knopp, Niels Erik Olesen, René Holm, Thomas Rades The aim of the present study was to compare two DSC-based methods to predict drug-polymer solubility (melting point depression method and recrystallization method) and propose a guideline for selecting the most suitable method based on physicochemical properties of both the drug and the polymer. Using the two methods, the solubilities of celecoxib, indomethacin, carbamazepine, and ritonavir in polyvinylpyrrolidone, hy...
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Dry-powder formulations of non-covalent protein complexes with linear or miktoarm copolymers for pulmonary delivery
Publication date: 5 April 2018 Source:International Journal of Pharmaceutics, Volume 540, Issues 1–2 Author(s): Alejandro Nieto-Orellana, David Coghlan, Malcolm Rothery, Franco H. Falcone, Cynthia Bosquillon, Nick Childerhouse, Giuseppe Mantovani, Snow Stolnik Pulmonary delivery of protein therapeutics has considerable clinical potential for treating both local and systemic diseases. However, poor protein conformational stability, immunogenicity and protein degradation by proteolytic enzymes in the lung are major challenges to overcome for the development of effective therapeutics. To address these, a family of stru...
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Curcumin marinosomes as promising nano-drug delivery system for lung cancer
Publication date: 5 April 2018 Source:International Journal of Pharmaceutics, Volume 540, Issues 1–2 Author(s): Shaimaa Ibrahim, Tatsuaki Tagami, Toshihiro Kishi, Tetsuya Ozeki Lung cancer is the major cause of cancer-related death worldwide. Curcumin attracted attention due to its promising anti-cancer properties, however its poor aqueous solubility and bioavailability have to be overcome. In the current study curcumin is encapsulated in krill lipids-based liposomes (marinosomes) to develop a potential anticancer therapy from low-cost and readily available nutraceuticals. Reflux followed by thin drug-lipid film met...
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Study of a low-dose capsule filling process by dynamic and static tests for advanced process understanding
This study is a further step towards a scientific qualification of dosator nozzles for low-fill weight (1–45 mg) capsule filling. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Impact of chirality on the Glass Forming Ability and the crystallization from the amorphous state of 5-ethyl-5-methylhydantoin, a chiral poor glass former
Publication date: 5 April 2018 Source:International Journal of Pharmaceutics, Volume 540, Issues 1–2 Author(s): Bienvenu Atawa, Nicolas Couvrat, Gérard Coquerel, Eric Dargent, Allisson Saiter The investigation of the glassy state of 5-ethyl-5-methylhydantoin (i.e. 12H, a chiral Active Pharmaceutical Ingredient) was attempted by Differential Scanning Calorimetry (DSC) and Fast Scanning Calorimetry (FSC). This compound exhibits a high crystallization propensity for every enantiomeric composition. Nevertheless, glassy states of pure enantiomer or mixtures between enantiomers were successfully reached by FSC at c...
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Statistical moments in modelling of swelling, erosion and drug release of hydrophilic matrix-tablets
Publication date: 5 April 2018 Source:International Journal of Pharmaceutics, Volume 540, Issues 1–2 Author(s): P. Barmpalexis, K. Kachrimanis, S. Malamataris Statistical moments were evaluated as suitable parameters for describing swelling and erosion processes (along with drug release) in hydrophilic controlled release matrix tablets. The effect of four independent formulation variables, corresponding to the quantity of four polymeric matrix excipients (namely polyethylene glycol, povidone, and two grades of hydroxyl-propylmethyl cellulose) on statistical moments describing swelling (mean swelling time, MST), eros...
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Nanomedicine: An effective tool in cancer therapy
Publication date: 5 April 2018 Source:International Journal of Pharmaceutics, Volume 540, Issues 1–2 Author(s): Saima Aftab, Afzal Shah, Akhtar Nadhman, Sevinc Kurbanoglu, Sibel Aysıl Ozkan, Dionysios D. Dionysiou, Shyam S. Shukla, Tejraj M. Aminabhavi Various types of nanoparticles (NPs) have been used in delivering anticancer drugs to the site of action. This area has become more attractive in recent years due to optimal size and negligible undesirable side effects caused by the NPs. The focus of this review is to explore various types of NPs and their surface/chemical modifications as well as attachment of targe...
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Fabricating 3D printed orally disintegrating printlets using selective laser sintering
Publication date: 25 April 2018 Source:International Journal of Pharmaceutics, Volume 541, Issues 1–2 Author(s): Fabrizio Fina, Christine M. Madla, Alvaro Goyanes, Jiaxin Zhang, Simon Gaisford, Abdul W. Basit Selective laser sintering (SLS) is a three-dimensional printing (3DP) technology employed to manufacture plastic, metallic or ceramic objects. The aim of this study was to demonstrate the feasibility of using SLS to fabricate novel solid dosage forms with accelerated drug release properties, and with a view to create orally disintegrating formulations. Two polymers (hydroxypropyl methylcellulose (HPMC E5) and v...
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Overcoming the polycation dilemma – Explorative studies to characterise the efficiency and biocompatibility of newly designed lipofection reagents
Publication date: 25 April 2018 Source:International Journal of Pharmaceutics, Volume 541, Issues 1–2 Author(s): Julia Giselbrecht, Christopher Janich, Shashank Reddy Pinnapireddy, Gerd Hause, Udo Bakowsky, Christian Wölk, Andreas Langner In this explorative study of the novel cationic lipid OO4 in two different formulations the complex formation with DNA, the biopharmaceutical stability of the lipid/DNA complexes in physiological media, and the transfection efficiency were analysed. We investigated liposomes composed of two binary mixtures of OO4 with either DOPE or DPPE as co-lipids in the molar ratio of 1:3....
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Lipid-based nanosuspensions for oral delivery of peptides, a critical review
This article details different techniques used to produce SLN and NLC with potential or effective peptide encapsulation. Basic principles of covalent and non-covalent lipidization are described and discussed as a prerequisite to improve hydrophilic peptide encapsulation in lipid-based nanosuspensions. The last part of this review provides the key evaluation techniques to assay SLN and NLC for peptide oral bioavailability enhancement. Methods to assess the protective effects of the carriers are described as well as the techniques to evaluate peptide release upon lipid digestion by lipases. Furthermore, this review suggests ...
Source: International Journal of Pharmaceutics - February 22, 2018 Category: Drugs & Pharmacology Source Type: research

Flexible and precise dosing of enalapril maleate for all paediatric age groups utilizing orodispersible minitablets
In this study, a dilution method has been developed by dispersing the lowest dose strength ODMTs to enable flexible and precise EM dosing during the dose titration phase of the therapy. Furthermore, the physicochemical stability of the ODMTs has been investigated in child-friendly beverages and the administration of ODMTs via nasogastric tubes (NGT) of different sizes and materials has been evaluated. The results for the ODMT dilution procedure reveal that dispersion within an oral syringe is preferred over dispersion in a separate container, leading to flexible and precise dosing down to 0.025 mg EM. Although ODMTs were s...
Source: International Journal of Pharmaceutics - February 21, 2018 Category: Drugs & Pharmacology Source Type: research

Aqueous injection of quercetin: an approach for confirmation of its direct in vivo cardiovascular effects
This study reports for the first time an injectable water-soluble formulation of quercetin suitable for confirmation of its vascular effect in vivo. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 21, 2018 Category: Drugs & Pharmacology Source Type: research

DoE based Olanzapine loaded poly-caprolactone nanoparticles decreases extrapyramidal effects in rodent model
Publication date: Available online 21 February 2018 Source:International Journal of Pharmaceutics Author(s): Emil Joseph, Satish Reddi, Vibhu Rinwa, Garima Balwani, Ranendra Saha The purpose of present investigation was to nano-encapsulate atypical antipsychotic such as Olanzapine in polymeric nanoparticles in order to explore the possibility of minimizing drug associated extrapyramidal adverse effects. The polymeric nanoparticulate systems were prepared using FDA approved polymer, polycaprolactone, by simple technique of nanoprecipitation using factorial design by DoE approach. The significant factors selected for the op...
Source: International Journal of Pharmaceutics - February 21, 2018 Category: Drugs & Pharmacology Source Type: research

Protective effect of sodium stearate on the moisture-induced deterioration of hygroscopic spray-dried powders
In this study, disodium cromoglycate (DSCG) powder was chosen as a model drug because it is amorphous and highly hygroscopic after spray drying. Sodium stearate (NaSt) was co-spray dried with DSCG at various concentrations (10, 50 and 90% w/w) to investigate its effect against moisture-induced deterioration on the in vitro aerosolization performance of DSCG. Particle size distribution and morphology were measured by laser diffraction and scanning electron microscopy (SEM). Physicochemical properties of the powders were analysed by X-ray powder diffraction (XRPD) and dynamic vapour sorption (DVS). Particle surface chemistry...
Source: International Journal of Pharmaceutics - February 21, 2018 Category: Drugs & Pharmacology Source Type: research

Photostabilization strategies of photosensitive drugs
Conclusions A gold standard strategy suitable for all compounds cannot be proposed. Instead, case-by-case evaluation, supported on the photodegradation mechanism is recommended. Systematic studies that compare different photostabilization strategies undertaken with the same irradiation conditions are also needed. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 21, 2018 Category: Drugs & Pharmacology Source Type: research

Establishment of an Evaluation Method to Detect Drug Distribution in Hair Follicles
Publication date: Available online 19 February 2018 Source:International Journal of Pharmaceutics Author(s): Akinari Abe, Miyuki Saito, Wesam R. Kadhum, Hiroaki Todo, Kenji Sugibayashi Development of an appropriate method to evaluate drug disposition or targeting ability in hair follicles (HFs) is urgently needed in order to develop useful pharmaceutical products with pharmacological effects in HFs. In the present study, a cyanoacrylate biopsy (CB) method was used to measure drug disposition in HFs using a model hydrophilic drug, caffeine (CAF), and a lipophilic drug, 4-butylresorcinol (BR), in excised porcine skin. As a ...
Source: International Journal of Pharmaceutics - February 20, 2018 Category: Drugs & Pharmacology Source Type: research

Intestinal Absorption and Activation of Decitabine Amino Acid Ester Prodrugs Mediated by Peptide Transporter PEPT1 and Enterocyte Enzymes
Publication date: Available online 19 February 2018 Source:International Journal of Pharmaceutics Author(s): Wenhui Tao, Dongyang Zhao, Mengchi Sun, Ziyu Wang, Bin Lin, Yu Bao, Yingying Li, Zhonggui He, Yinghua Sun, Jin Sun Decitabine (DAC), a potent DNA methyltransferase (DNMT) inhibitor, has a limited oral bioavailability. Its 5′-amino acid ester prodrugs could improve its oral delivery but the specific absorption mechanism is not yet fully understood. The aim of this present study was to investigate the in vivo absorption and activation mechanism of these prodrugs using in situ intestinal perfusion and pharmacoki...
Source: International Journal of Pharmaceutics - February 20, 2018 Category: Drugs & Pharmacology Source Type: research

Transdermal delivery of vitamin K using dissolving microneedles for the prevention of vitamin K deficiency bleeding
The objective of our study was to investigate the manufacture of microneedles for the delivery of vitamin K. Following microneedle fabrication, we performed insertion studies to assess the microneedle’s mechanical properties. Results indicate that vitamin K in a microneedle array was successfully delivered in vitro across neonatal porcine skin with 1.80 ± 0.08 mg delivered over 24 hours. Therefore, this initial study shows that microneedles do have the potential to prevent vitamin K deficiency bleeding. Future work will assess delivery of vitamin K in microneedle array in vivo. Graphical abstract (Source: Inte...
Source: International Journal of Pharmaceutics - February 20, 2018 Category: Drugs & Pharmacology Source Type: research

Co-spray drying of hygroscopic kanamycin with the hydrophobic drug rifampicin to improve the aerosolization of kanamycin powder for treating respiratory infections
Publication date: Available online 17 February 2018 Source:International Journal of Pharmaceutics Author(s): Mohammad A.M. Momin, Ian G. Tucker, Colin S. Doyle, John A. Denman, Shubhra Sinha, Shyamal C. Das High dose delivery of drugs to the lung using a dry powder inhaler (DPI) is an emerging approach to combat drug-resistant local infections. To achieve this, highly aerosolizable powders are required. We hypothesized that co-spray-drying kanamycin, a hydrophilic hygroscopic antibiotic, with rifampicin, a hydrophobic antibiotic, would produce inhalable particles with surfaces enriched in rifampicin. Such particles would ...
Source: International Journal of Pharmaceutics - February 18, 2018 Category: Drugs & Pharmacology Source Type: research

Topical bio(in)equivalence of metronidazole formulations in vivo
Publication date: Available online 17 February 2018 Source:International Journal of Pharmaceutics Author(s): Thalita Pedon de Araujo, Isabelle Moura Fittipaldi, Danilo Cesar Galindo Bedor, Maira Ludna Duarte, Sarah F. Cordery, Richard H. Guy, M. Begonã Delgado-Charro, Davi Pereira de Santana, Leila Bastos Leal The topical bioavailabilities of metronidazole from a commercially available ‘reference’ product (Rozex®) and two extemporaneous test formulations were compared. With the reference drug product, a full skin pharmacokinetic profile, in vivo in human volunteers (following a 6-hour uptake and cle...
Source: International Journal of Pharmaceutics - February 18, 2018 Category: Drugs & Pharmacology Source Type: research

PLGA nanoformulation of Sparfloxacin enhanced antibacterial activity with photoprotective potential under ambient UV-R exposure
Publication date: Available online 17 February 2018 Source:International Journal of Pharmaceutics Author(s): Jyoti Singh, Ashish Dwivedi, Lipika Ray, Deepti Chopra, Divya Dubey, Ajeet K. Srivastva, Smita Kumari, Randheer Kumar, Saroj Kumar Amar, Chandana Haldar, Ratan Singh Ray Sparfloxacin (SPFX) is a broad spectrum antibiotic which inhibits bacterial DNA gyrase enzyme activity. However, photodegradation in the presence of UVA limits its antibacterial activity and induces phototoxicity. Thus, to encounter this problem, we have developed poly d,l-lactic-co- glycolic acid (PLGA) loaded SPFX nanoparticles. Here, we have per...
Source: International Journal of Pharmaceutics - February 18, 2018 Category: Drugs & Pharmacology Source Type: research

Dermal anti-oxidant, anti-inflammatory and anti-aging effects of Compritol ATO-based Resveratrol colloidal carriers prepared using mixed surfactants.
In this study, Compritol ATO-based Resveratrol colloidal carriers (CCCs) were prepared. In most formulae, the use of a binary-mixture of surfactants improved the physicochemical properties. CCC6 (containing P407/P188 as bi-surfactants) attained the highest drug loading, release efficiency during 24 hr and occlusive effect for 48 hr; in addition to, a uniform particle size distribution within the desired range. In-vivo studies were done based on the analysis of anti-oxidant markers [catalase (CAT), reduced glutathione (GSH) and superoxide dismutase (SOD)], anti-inflammatory markers [interleukin 6 (IL-6), interleukin 8 (IL-8...
Source: International Journal of Pharmaceutics - February 18, 2018 Category: Drugs & Pharmacology Source Type: research

Overcoming the polycation dilemma - Explorative studies to characterise the efficiency and biocompatibility of newly designed lipofection reagents
Publication date: Available online 17 February 2018 Source:International Journal of Pharmaceutics Author(s): Julia Giselbrecht, Christopher Janich, Shashank Reddy Pinnapireddy, Gerd Hause, Udo Bakowsky, Christian Wölk, Andreas Langner In this explorative study of the novel cationic lipid OO4 in two different formulations the complex formation with DNA, the biopharmaceutical stability of the lipid/DNA complexes in physiological media, and the transfection efficiency were analysed. We investigated liposomes composed of two binary mixtures of OO4 with either DOPE or DPPE as co-lipids in the molar ratio of 1:3. These for...
Source: International Journal of Pharmaceutics - February 18, 2018 Category: Drugs & Pharmacology Source Type: research

Self-microemulsifying drug delivery system for camptothecin using new bicephalous heterolipid with tertiary-amine as branching element
Publication date: Available online 17 February 2018 Source:International Journal of Pharmaceutics Author(s): Dinesh M. Dhumal, K.G. Akamanchi Camptothecin (CPT) has a potent and broad-spectrum anti-tumor activity but its clinical use is limited due to its poor water solubility, stability at physiological conditions and toxicity. The aim of our study was to evaluate bicephalous heterolipid E1E for enhancing the solubility and stability of CPT through the development of a selfmicroemulsifying drug delivery system (SMEDDS). The solubility of CPT in heterolipid E1E was found to be 82 and 5.86 folds higher than oleic acid and ...
Source: International Journal of Pharmaceutics - February 18, 2018 Category: Drugs & Pharmacology Source Type: research

Impact of Formulation Excipients on the Thermal, Mechanical, and Electrokinetic Properties of Hydroxypropyl methylcellulose acetate succinate (HPMCAS)
This study facilitated the understanding of the HPMCAS aggregation mechanism, in addition to identifying suitable stabilizing agents. These stabilizing excipients could potentially be used to develop a stable aqueous coating formulation that does not exhibit polymer aggregation and nozzle clogging during the coating process. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 17, 2018 Category: Drugs & Pharmacology Source Type: research

The use of fatty acids as absorption enhancer for pulmonary drug delivery
In this study, the potential of sodium decanoate (Na dec), docosahexaenoic acid (DHA) and eicosapentaenoic acid (EPA) as absorption enhancers has been investigated to increase pulmonary paracellular permeability by modulating epithelial cells’ tight junctions. By incorporating Na dec, DHA and EPA, separately, into a nebulising formulation, the aim was to enhance the absorption of a fluorescent marker (flu-Na, used as model drug) across pulmonary epithelial cells (Calu-3). Results indicate that the aerosol performance of all the nebulizing formulations containing absorption enhancers was significantly better than cont...
Source: International Journal of Pharmaceutics - February 17, 2018 Category: Drugs & Pharmacology Source Type: research

Mucoadhesive Self-Emulsifying Delivery Systems for Ocular Administration of Econazole
Conclusion Accordingly, these mucoadhesive SEDDS can be considered as promising ocular delivery system for EN. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 17, 2018 Category: Drugs & Pharmacology Source Type: research

Preparation of a solid self-microemulsifying drug delivery system by hot-melt extrusion
This study sought to prepare enteric S-SMEDDS by HME and evaluate the effects of the process and formulation variables on S-SMEDDS properties via Box-Behnken design. Liquid SMEDDS were developed, and carvedilol was used as a class II model drug. Mean size, polydispersity index (PdI) and zeta potential of the resulting microemulsions were determined. The extrudates were then obtained by blending the lipid mixture and HPMCAS using a twin-screw hot-melt extruder. SEM, optical microscopy and PXRD were used to characterize the extrudates. In vitro microemulsion reconstitution and drug release were also studied. L-SMEDDS gave ri...
Source: International Journal of Pharmaceutics - February 17, 2018 Category: Drugs & Pharmacology Source Type: research

Developing a Stable Aqueous Enteric Coating Formulation with Hydroxypropyl methylcellulose acetate succinate (HPMCAS-MF) and Colloidal Silicon Dioxide as Anti-tacking Agent
Publication date: Available online 16 February 2018 Source:International Journal of Pharmaceutics Author(s): Tanvi M. Deshpande, Anisul Quadir, Sakae Obara, Ahmed Ibrahim, Stephen W. Hoag The purpose of this study was to use statistical design of experiments to develop a stable aqueous enteric coating formulation containing stabilizing excipients, such as polyethylene glycol that can minimize hydroxypropyl methylcellulose acetate succinate aggregation and minimize spray-nozzle clogging at elevated processing temperatures. The mechanisms of stabilization (i.e. charge stabilization and molecular interactions) were studied b...
Source: International Journal of Pharmaceutics - February 17, 2018 Category: Drugs & Pharmacology Source Type: research

A Review of Implantable Biosensors for Closed-Loop Glucose Control and Other Drug Delivery Applications
Publication date: Available online 16 February 2018 Source:International Journal of Pharmaceutics Author(s): Kee Scholten, Ellis Meng Closed-loop drug delivery promises autonomous control of pharmacotherapy through the continuous monitoring of biomarker levels. For decades, researchers have strived for portable closed-loop systems, capable of treating ambulatory patients with chronic conditions such as diabetes mellitus. After years of development, the first of these systems have left the laboratory and entered commercial use. This long-awaited advance reflects recent development of chronically stable implantable biosenso...
Source: International Journal of Pharmaceutics - February 17, 2018 Category: Drugs & Pharmacology Source Type: research

Influence of ligands property and particle size of gold nanoparticles on the protein adsorption and corresponding targeting ability
In this study, two common used ligands were chosen as the model: transferrin and RGD peptide. Gold nanoparticles were utilized as model particles. Sodium dodecyl sulfate polyacrylamide gel electrophoresis data demonstrated that higher PEG modification and smaller particle size could reduce the plasma protein adsorption, while ligand modification could increase. The cellular uptake results showed that the targeting ability of smaller ligand RGD peptide would be more easily influenced by the proteins corona. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 4, 2018 Category: Drugs & Pharmacology Source Type: research

Isomalt and its diastereomer mixtures as stabilizing excipients with freeze-dried lactate dehydrogenase
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Anna-Kaisa Tuderman, Clare J. Strachan, Anne M. Juppo The purpose of this research was to study isomalt as a protein-stabilizing excipient with lactate dehydrogenase (LDH) during freeze-drying and subsequent storage and compare it to sucrose, a standard freeze-drying excipient. Four different diastereomer mixtures of isomalt were studied. The stability of the protein was studied with a spectrophotometric enzyme activity test and circular dichroism after freeze-drying and after 21 days of storage at 16% R...
Source: International Journal of Pharmaceutics - February 4, 2018 Category: Drugs & Pharmacology Source Type: research

Proliposome tablets manufactured using a slurry-driven lipid-enriched powders: Development, characterization and stability evaluation
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Iftikhar Khan, Sakib Yousaf, Sneha Subramanian, Mohamed Albed Alhnan, Waqar Ahmed, Abdelbary Elhissi Proliposome powders were prepared via a slurry method using sorbitol or D-mannitol as carbohydrate carriers in 1:10 or 1:15 w/w lipid phase to carrier ratios. Soya phosphatidylcholine (SPC) and cholesterol were employed as a lipid phase and Beclometasone dipropionate (BDP) was incorporated as a model drug. Direct compaction using a Minipress was applied on the lipid-enriched powder in order to manufacture p...
Source: International Journal of Pharmaceutics - February 4, 2018 Category: Drugs & Pharmacology Source Type: research

Improving release completeness from PLGA-based implants for the acid-labile model protein ovalbumin
The objectives of this study were to assess the feasibility of hot melt extrusion (HME) for the preparation of PLGA-based ovalbumin-loaded implants as well as to characterize and improve protein release from the implants. Ovalbumin (OVA) was stable during extrusion, which was attributed to a protective effect of the biodegradable matrix. OVA release was characterized by a low burst, a slow release up to day 21, which plateaued thereafter resulting in incomplete release for all evaluated protein loadings. Release incompleteness was accompanied by the formation of an insoluble residual mass. Further characterization of this ...
Source: International Journal of Pharmaceutics - February 4, 2018 Category: Drugs & Pharmacology Source Type: research

A drop penetration method to measure powder blend wettability
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Yifan Wang, Zhanjie Liu, Fernando Muzzio, German Drazer, Gerardo Callegari Water wettability of pharmaceutical blends affects important quality attributes of final products. We investigate the wetting properties of a pharmaceutical blend lubricated with Magnesium Stearate (MgSt) as a function of the mechanical shear strain applied to the blend. We measure the penetration dynamics of sessile drops deposited on slightly compressed powder beds. We consider a blend composed of 9% Acetaminophen 90% Lactose and ...
Source: International Journal of Pharmaceutics - February 4, 2018 Category: Drugs & Pharmacology Source Type: research

Development and pre-clinical evaluation in the swine model of a mucosal vaccine tablet for human influenza viruses: A proof-of-concept study
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): V. Busignies, G. Simon, G. Mollereau, O. Bourry, V. Mazel, M. Rosa-Calatrava, P. Tchoreloff Liquid vaccine formulations present some disadvantages such as stability problems, cold chain requirement or administration by trained personnel. Vaccine formulated as tablets would present a wide range of progress such as an increase stability that would facilitate the administration, the distribution and the storage of vaccine formulations. This work investigates the possibility to develop a mucosal tablet vaccine...
Source: International Journal of Pharmaceutics - February 4, 2018 Category: Drugs & Pharmacology Source Type: research

Recent trends of nanomedicinal approaches in clinics
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Fahima Dilnawaz, Sarbari Acharya, Sanjeeb Kumar Sahoo Nanotechnology has become the indispensable cutting edge science providing solutions to many problems associated with human being. The application of nanotechnology associated to human health “nanomedicine” has revolutionized the drug delivery system by providing improved pharmacological and therapeutic properties of drugs. These advantageous effects of drug loaded nanocarrier systems are embraced by the pharmaceutical industries for the dev...
Source: International Journal of Pharmaceutics - February 4, 2018 Category: Drugs & Pharmacology Source Type: research

Trends in insect repellent formulations: A review
Publication date: 25 March 2018 Source:International Journal of Pharmaceutics, Volume 539, Issues 1–2 Author(s): Melanie Tavares, Márcio Robert Mattos da Silva, Luciana Betzler de Oliveira de Siqueira, Raphaela Aparecida Schuenck Rodrigues, Lolita Bodjolle-d'Almeira, Elisabete Pereira dos Santos, Eduardo Ricci-Júnior The use of natural and synthetic repellents, marketed in different pharmaceutical forms, is growing in the world due to the emerging vector-borne viral diseases as Dengue, Zika, Chikungunya, Yellow Fever and Malaria. The choice of the ideal formulation will depend on a series of factors to...
Source: International Journal of Pharmaceutics - February 4, 2018 Category: Drugs & Pharmacology Source Type: research

Dual-responsive lidocaine in situ gel reduces pain of intrauterine device insertion
In conclusion, lidocaine dual-responsive in situ gel can be effectively used in prevention of pain during IUD insertion. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 3, 2018 Category: Drugs & Pharmacology Source Type: research

Is there a correlation between the glass forming ability of a drug and its supersaturation propensity?
In this study, a potential correlation between GFA and supersaturation propensity is investigated. The GFA of 23 different drugs was determined by melt quenching or milling the crystalline drugs to obtain their respective amorphous forms. The inherent propensity of the drug to supersaturate, i.e. the maximal apparent degree of supersaturation (aDS), and the time until precipitation at a given aDS were determined. Supersaturation was induced via a solvent shift method where the drug was initially dissolved in dimethyl sulfoxide and then added to a biorelevant medium (fasted state simulated intestinal fluid).The study showed...
Source: International Journal of Pharmaceutics - February 3, 2018 Category: Drugs & Pharmacology Source Type: research

A mesoporous silica based platform to enable tablet formulations of low dose drugs by direct compression
Publication date: 25 March 2018 Source:International Journal of Pharmaceutics, Volume 539, Issues 1–2 Author(s): Wei-Jhe Sun, Aktham Aburub, Changquan Calvin Sun Achieving adequate content uniformity (CU) is a significant challenge in the development and manufacturing of low dose oral tablets. Using four model active pharmaceutical ingredients (APIs), we show that loading APIs into a grade of mesoporous silica, Aeroperl®, is effective for achieving excellent CU. All APIs in the Aeroperl® composites were amorphous. After six months under accelerated stability conditions, the drug-Aeoperl composites exhibited ...
Source: International Journal of Pharmaceutics - February 3, 2018 Category: Drugs & Pharmacology Source Type: research

Liquid crystalline drug delivery vehicles for oral and IV/subcutaneous administration of poorly soluble (and soluble) drugs
Publication date: Available online 31 January 2018 Source:International Journal of Pharmaceutics Author(s): Andrew Otte, Bong-Kwan Soh, Gwangheum Yoon, Kinam Park Poorly soluble drug molecules often have low bioavailability issues and absorption problems in the clinical setting. As the number of poorly soluble drugs increases from discovery, developing technologies to enhance their solubility, while also controlling their release is one of the many challenges facing the pharmaceutical industry today. Liquid crystalline systems, nanoparticulate or macro-matrix, self-assemble in the presence of an aqueous environment and ca...
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

Asymmetric flow field flow fractionation for the characterization of globule size distribution in complex formulations: A cyclosporine ophthalmic emulsion case
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Haiou Qu, Jiang Wang, Yong Wu, Jiwen Zheng, Yellela S.R. Krishnaiah, Mohammad Absar, Stephanie Choi, Muhammad Ashraf, Celia N. Cruz, Xiaoming Xu Commonly used characterization techniques such as cryogenic-transmission electron microscopy (cryo-TEM) and batch-mode dynamic light scattering (DLS) are either time consuming or unable to offer high resolution to discern the poly-dispersity of complex drug products like cyclosporine ophthalmic emulsions. Here, a size-based separation and characterization method f...
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

Self-emulsifying peptide drug delivery systems: How to make them highly mucus permeating
Conclusion Small droplet size and negative zeta potential of SEDDS could be identified as key parameters for their mucus permeating properties. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

Induction of Au-methotrexate conjugates by sugar molecules: production, assembly mechanism, and bioassay studies
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Wei-Yuan Wang, Xiu-Fen Zhao, Xiao-Han Ju, Ping Liu, Jing Li, Ya-Wen Tang, Shu-Ping Li, Xiao-Dong Li, Fu-Gui Song Au-methotrexate (Au-MTX) conjugates induced by sugar molecules were produced by a simple, one-pot, hydrothermal growth method. Herein, the Au(III)-MTX complexes were used as the precursors to form Au-MTX conjugates. Addition of different types of sugar molecules with abundant hydroxyl groups resulted in the formation of Au-MTX conjugates featuring distinct characteristics that could be explained...
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

Process analytical technology in continuous manufacturing of a commercial pharmaceutical product
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Jenny M. Vargas, Sarah Nielsen, Vanessa Cárdenas, Anthony Gonzalez, Efrain Y. Aymat, Elvin Almodovar, Gustavo Classe, Yleana Colón, Eric Sanchez, Rodolfo J. Romañach The implementation of process analytical technology and continuous manufacturing at an FDA approved commercial manufacturing site is described. In this direct compaction process the blends produced were monitored with a Near Infrared (NIR) spectroscopic calibration model developed with partial least squares (PLS) regressio...
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

Hydrogels based on poly(methyl vinyl ether-co-maleic acid) and Tween 85 for sustained delivery of hydrophobic drugs
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Eneko Larrañeta, Laura Barturen, Michael Ervine, Ryan F. Donnelly Hydrogels based on poly(methyl vinyl ether-co-maleic acid) and Tween 85 were prepared for hydrophobic drug delivery. The hydrogels were synthesized following a simple procedure carried out in solid state. The process did not require the use of any solvent and, as it is based on an esterification reaction, no toxic by-products were obtained. The resulting hydrogels contained Tween 85 inside the structure and due to the amphiphilic natu...
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

Performance of an acoustically mixed pharmaceutical dry powder delivered from a novel inhaler
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Ryoma Tanaka, Naoyuki Takahashi, Yasuaki Nakamura, Yusuke Hattori, Kazuhide Ashizawa, Makoto OtsukaGraphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

Semifluorinated alkane based systems for enhanced corneal penetration of poorly soluble drugs
This study evaluated the potential of two SFAs to act as vehicle for topical ocular drug delivery. After confirming ocular safety, an ex vivo corneal penetration model was developed to determine drug distribution and corneal bioavailability. Hydrophobic dye distribution in the different corneal layers was visualised under a confocal microscope. Corneal bioavailability of cyclosporine A (CsA) dissolved in perfluorobutylpentane (F4H5) or perfluorohexyloctane (F6H8) was compared to commercially available CsA ophthalmic emulsions, Restasis® and Ikervis®. Precorneal residence of the four test vehicles containing the hyd...
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research