Nanoparticles formulation and in vitro efficacy testing of the mitoNEET ligand NL-1 for drug delivery in a brain endothelial model of ischemic reperfusion-injury
This study lays the preliminary work for potential use of mitoNEET as a target and NL-1 as a therapeutic for the treatment of cerebral ischemia and reperfusion injury.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 29, 2020 Category: Drugs & Pharmacology Source Type: research

A Comparison of Background Membrane Imaging versus Flow Technologies for Subvisible Particle Analysis of Biologics
Publication date: Available online 27 January 2020Source: International Journal of PharmaceuticsAuthor(s): Stephanie K. Vargas, Aydin Eskafi, Eric Carter, Natalie CiaccioAbstractA recently developed high-throughput background membrane imaging (BMI) technique, the HORIZON, was assessed for its ability to quantify subvisible particles (SVP) generated during protein therapeutic development. The HORIZON platform method was optimized and compared to three well-characterized SVP counting techniques: light obscuration, micro-flow imaging (MFI), and FlowCam®. A head-to-head comparison was performed for precision, linearity, SV...
Source: International Journal of Pharmaceutics - January 28, 2020 Category: Drugs & Pharmacology Source Type: research

Simultaneous taste-masking and oral bioavailability enhancement of Ligustrazine by forming sweet salts
Publication date: Available online 27 January 2020Source: International Journal of PharmaceuticsAuthor(s): Xinghua Zhao, Qiang Li, Chenguang Wang, Shenye Hu, Xin He, Changquan Calvin SunAbstractLigustrazine (or Tetramethylpyrazine, TMP) is an active pharmaceutical ingredient that faces the challenges of bitter taste and low oral bioavailability by the commercial phosphate salt (TMP-Pho). We tackled these challenges by forming salts with two sweeteners, acesulfame (Acs) and saccharine (Sac). Both salts effectively masked the bitter taste of TMP. Compared to TMP-Pho, TMP-Sac shows 43% lower solubility and 11% lower permeabil...
Source: International Journal of Pharmaceutics - January 28, 2020 Category: Drugs & Pharmacology Source Type: research

Enhanced anti-tumor and anti-metastasis therapy for triple negative breast cancer by CD44 receptor-targeted hybrid self-delivery micelles
Publication date: Available online 27 January 2020Source: International Journal of PharmaceuticsAuthor(s): Yiliang Yang, Yang Long, Yashi Wang, Kebai Ren, Man Li, Zhirong Zhang, Bing Xiang, Qin HeAbstractTumor growth and metastasis are multistep processes regulated by multiple signaling pathways. The successful treatment of cancer largely depends on the ability to inhibit metastatic process. Multiphase inhibition of metastasis is a promising approach. Here, we described a targeting delivery system which was constructed by mixing hyaluronic acid-D-α-tocopheryl succinate (HA-TOS, HT) and low molecular weight heparin-TO...
Source: International Journal of Pharmaceutics - January 28, 2020 Category: Drugs & Pharmacology Source Type: research

Gellan gum and its methacrylated derivatives as in situ gelling mucoadhesive formulations of pilocarpine: in vitro and in vivo studies
Publication date: Available online 28 January 2020Source: International Journal of PharmaceuticsAuthor(s): Laura E. Agibayeva, Daulet B. Kaldybekov, Natalia N. Porfiryeva, Venera Garipova, Rauash A. Mangazbayeva, Rouslan I. Moustafine, Irina I. Semina, Grigoriy A. Mun, Sarkyt E. Kudaibergenov, Vitaliy V. KhutoryanskiyAbstractGellan gum was chemically modified by the reaction with methacrylic anhydride to produce derivatives with 6, 14 and 49 % methacrylation. The structure and substitutions degrees of these derivatives were confirmed by 1H NMR- and FTIR-spectroscopy. These derivatives are more hydrophobic compared to prist...
Source: International Journal of Pharmaceutics - January 28, 2020 Category: Drugs & Pharmacology Source Type: research

Exploration of Docetaxel Palmitate and its Solid Lipid Nanoparticles as a Novel Option for Alleviating the Rising Concern of Multi-Drug Resistance
Publication date: Available online 27 January 2020Source: International Journal of PharmaceuticsAuthor(s): Lokesh Kaushik, Shubham Srivastava, Anshul Panjeta, Dasharath Chaudhari, Rohan Ghadi, Kaushik Kuche, Ruchi Malik, Simran Preet, Sanyog Jain, Kaisar RazaAbstractDocetaxel (DTX), a widely prescribed anticancer agent, is now associated with increased instances of multidrug resistance. Also, being a problematic BCS class IV drug, it poses challenges for the formulators. Henceforth, it was envisioned to synthesize an analogue of DTX with a biocompatible lipid, i.e., palmitic acid. The in-silico studies (molecular docking a...
Source: International Journal of Pharmaceutics - January 28, 2020 Category: Drugs & Pharmacology Source Type: research

Prolonged Melittin Release from Polyelectrolyte-Based Nanocomplexes Decreases Acute Toxicity and Improves Blood Glycemic Control in a Mouse Model of Type II Diabetes
Publication date: Available online 25 January 2020Source: International Journal of PharmaceuticsAuthor(s): Zaizhi Gui, Jinchang Zhu, Song Ye, Juan Ye, Jiao Chen, Yuanyuan Ling, Xueting Cai, Peng Cao, Zhiyu He, Chunping HuAbstractGating modifier toxins (GMTs) from animal venom have shown great potential in controlling blood glucose levels in type II diabetes (T2D), but their high acute toxicity and quick clearance in the body hamper their potential therapeutic use. Inspired by their highly positive charge, we have developed a nanocomplex system based on polyelectrolytes, in which strong interactions form between positively ...
Source: International Journal of Pharmaceutics - January 26, 2020 Category: Drugs & Pharmacology Source Type: research

Structural Characterization by Scattering and Spectroscopic Methods and Biological Evaluation of Polymeric Micelles of Poloxamines and TPGS as Nanocarriers for Miltefosine Delivery
Publication date: Available online 25 January 2020Source: International Journal of PharmaceuticsAuthor(s): Joan Puig-Rigall, Celia Fernandez-Rubio, Javier González-Benito, Judith E. Houston, Aurel Radulescu, Paul Nguewa, Gustavo González-GaitanoAbstractMiltefosine (MF), an alkylphospholipid originally developed for breast cancer treatment, is a highly active drug for the treatment against leishmaniasis, a neglected tropical disease considered the world’s second leading cause of death by a parasitic agent after malaria. MF exhibits dose-limiting gastrointestinal side effects in patients and its penetrati...
Source: International Journal of Pharmaceutics - January 26, 2020 Category: Drugs & Pharmacology Source Type: research

Correlation between drug dissolution and resistance to water-induced phase separation in solid dispersion formulations revealed by solid-state NMR spectroscopy
Publication date: Available online 25 January 2020Source: International Journal of PharmaceuticsAuthor(s): Hitomi Okada, Keisuke Ueda, Yuki Yasuda, Kenjirou Higashi, Motoki Inoue, Masataka Ito, Shuji Noguchi, Kohsaku Kawakami, Kunikazu MoribeAbstractWe aimed to elucidate the dissolution mechanism of solid dispersions (SDs) according to the carrier polymers used. Nifedipine (NIF) and polymers dissolved simultaneously from NIF/Eudragit® S (EUD-S), NIF/Eudragit® L (EUD-L), and NIF/hypromellose (HPMC)/EUD-S spray-dried samples (SPDs). In contrast, NIF dissolved separately from polymers from NIF/HPMC and NIF/HPMC/EUD-L ...
Source: International Journal of Pharmaceutics - January 26, 2020 Category: Drugs & Pharmacology Source Type: research

CD13-specific Ligand Facilitates Xanthatin Nanomedicine Targeting Dendritic Cells for Therapy of Refractory Allergic Rhinitis
Publication date: Available online 25 January 2020Source: International Journal of PharmaceuticsAuthor(s): Xue Zheng, Chao Sun, Rilei Yu, Xin Chu, Jiahao Xu, Chengcheng Liu, Miaoqing Zhao, Xuelian Xu, Ming Xia, Cheng WangAbstractRelapse in Allergic Rhinitis (AR) is triggered by various unclear mechanisms. Xanthium strumarium L. as a traditional folk medicine can inhibit inflammatory responses through multiple mechanisms. Xanthatin (XT) is a bioactive compound derived from Xanthium strumarium L, and we developed a polymeric micelle (PM) that is dendritic cells (DCs)-specific targeting delivery system loading XT (NGR-XT-PM) ...
Source: International Journal of Pharmaceutics - January 26, 2020 Category: Drugs & Pharmacology Source Type: research

Quantification of Phospholipid Degradation Products in Liposomal Pharmaceutical formulations by Ultra Performance Liquid Chromatography-Mass Spectrometry (UPLC-MS)
Publication date: Available online 24 January 2020Source: International Journal of PharmaceuticsAuthor(s): Dumindika A. Siriwardane, Changguang Wang, Wenlei Jiang, Thilak MudaligeAbstractIdentification and quantification of excipient related degradation products in the liposomal formulation is important, as they may impact the safety and efficacy of the drug. Phospholipids are one of the major excipients in liposome drugs composing the lipid bilayer, and they are vulnerable to oxidation and hydrolysis reactions. Since phospholipids with saturated fatty acid chain were preferred in most of liposome drug products, the major ...
Source: International Journal of Pharmaceutics - January 26, 2020 Category: Drugs & Pharmacology Source Type: research

Effect of an upstream grid on the fluidization of pharmaceutical carrier powders
This study contributes towards a better understanding of fluidization processes as relevant to dry powder inhaler devices and sheds light on how simple design alterations, such as adding an upstream grid, can be incorporated to optimise device effectiveness.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 26, 2020 Category: Drugs & Pharmacology Source Type: research

An Industrially Viable Technique for Fabrication of Docetaxel NLCs for Oncotherapy
Publication date: Available online 24 January 2020Source: International Journal of PharmaceuticsAuthor(s): Kharkar Prachi Balaram, Talkar Swapnil Sunil, Patravale Vandana BharatAbstractThe aim of this study is to formulate thermodynamically stable docetaxel loaded nanostructured lipid carriers (DTX-NLCs) for parenteral cancer therapy with improved long term stability and better pharmacokinetic performance. DTX-NLCswere formulated using microemulsion(ME) template technique and characterized for particle size,entrapment efficiency (EE%), drug content and in vitro release kinetics. Further evaluation of NLCs was carried out b...
Source: International Journal of Pharmaceutics - January 26, 2020 Category: Drugs & Pharmacology Source Type: research

Surface dissolution UV Imaging for characterization of superdisintegrants and their impact on drug dissolution
Publication date: Available online 24 January 2020Source: International Journal of PharmaceuticsAuthor(s): P. Zarmpi, T. Flanagan, E. Meehan, J. Mann, N. FotakiAbstractSuperdisintegrants are a key excipient used in immediate release formulations to promote fast tablet disintegration, therefore understanding the impact of superdisintegrant variability on product performance is important. The current study examined the impact of superdisintegrant critical material attributes (viscosity for sodium starch glycolate (SSG), particle size distribution (PSD) for croscarmellose sodium (CCS)) on their performance (swelling) and on d...
Source: International Journal of Pharmaceutics - January 26, 2020 Category: Drugs & Pharmacology Source Type: research

Cholic acid-based mixed micelles as siRNA delivery agents for gene therapy
In this study, we demonstrate the use of lipids as co-surfactants for the preparation of mixed micelles to improve the siRNA delivery of cholic acid-based block copolymers. Poly(allyl glycidyl ether) (PAGE) and poly(ethylene glycol) (PEG) were polymerized on the surface of cholic acid to afford a star-shaped block copolymer with four arms (CA-PAGE-b-PEG)4. The allyl groups of PAGE were functionalized to bear primary or tertiary amines and folic acid was grafted onto the PEG chain end to increase cell uptake. (CA-PAGE-b-PEG)4 functionalized with either primary or tertiary amines show high siRNA complexation with close to 10...
Source: International Journal of Pharmaceutics - January 26, 2020 Category: Drugs & Pharmacology Source Type: research

Combination of Paclitaxel and R-flurbiprofen loaded PLGA nanoparticles suppresses glioblastoma growth on systemic administration
In conclusion, PLGA NPs can efficiently carry their payloads to glioma tissue and the combined use of anticancer and anti-inflammatory drugs may exert additional anti-tumor activity.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 26, 2020 Category: Drugs & Pharmacology Source Type: research

Creation of novel large dataset comprising several granulation methods and the prediction of tablet properties from critical material attributes and critical process parameters using regularized linear regression models including interaction terms
In this study, we focused on the following three points: (1) creation of a dataset comprising several tablet production methods, (2) the influence of interaction terms of MAs and/or PPs, and (3) comparison of regularized linear regression models with partial least squares (PLS) regression. First, we prepared 44 kinds of tablets using direct compression and five kinds of granulation methods. We then measured 12 MAs and two model CQAs (tensile strength and disintegration time of tablet). Principal component analysis showed that the constructed dataset comprised a wide variety of particles. We applied regularized linear regre...
Source: International Journal of Pharmaceutics - January 26, 2020 Category: Drugs & Pharmacology Source Type: research

Phase behavior of pharmaceutically relevant polymer/solvent mixtures
Publication date: Available online 24 January 2020Source: International Journal of PharmaceuticsAuthor(s): Stefanie Dohrn, Christian Luebbert, Kristin Lehmkemper, Samuel O. Kyeremateng, Matthias Degenhardt, Gabriele SadowskiAbstractIn the pharmaceutical industry, polymers are used as excipients for formulating poorly water–soluble active pharmaceutical ingredients (APIs) in so-called “amorphous solid dispersions” (ASDs). ASDs can be produced via solvent-based processes, where API and polymer are both dissolved in a solvent, followed by a solvent evaporation step (e.g. spray drying). Aiming at a homogeneou...
Source: International Journal of Pharmaceutics - January 26, 2020 Category: Drugs & Pharmacology Source Type: research

A designed supramolecular cross-linking hydrogel for the direct, convenient, and efficient administration of hydrophobic drugs
Publication date: Available online 25 January 2020Source: International Journal of PharmaceuticsAuthor(s): Bohong Yu, Aiyan Zhan, Qi Liu, Hao Ye, Xiuqing Huang, Yue Shu, Yang Yang, Hongzhuo LiuAbstractHydrogels formed through reversible supramolecular interactions may attain self-healing in the in situ environment. However, the low grafting degree of functional groups and steric hindrance effect of polymer backbones significantly reduced the self-healing efficacy and kinetics. To overcome these deficiencies, we designed a novel hydrogel via non-covalent host-guest interaction between β-cyclodextrin modified hyaluronic...
Source: International Journal of Pharmaceutics - January 26, 2020 Category: Drugs & Pharmacology Source Type: research

Formulation development and in vitro evaluation of transferrin-conjugated liposomes as a carrier of ganciclovir targeting the retina
Publication date: Available online 25 January 2020Source: International Journal of PharmaceuticsAuthor(s): Rathapon Asasutjarit, Chittima Managit, Teva Phanaksri, Worapapar Treesuppharat, Asira FuongfuchatAbstractGanciclovir (GCV) is an antiviral drug approved for treatment of cytomegalovirus (CMV) retinitis. It can be delivered to the eye via systemic administrations. However, local delivery of GCV that targets the retina is considered as an alternative to increase efficacy of the treatment and lessen side effects. Thus, this study aimed to develop formulations of transferrin (Tf)-conjugated liposomes loaded GCV (Tf-GCV-L...
Source: International Journal of Pharmaceutics - January 26, 2020 Category: Drugs & Pharmacology Source Type: research

Quantification of porogen effect on the drug release from single- and multi-layered ethylcellulose coated pellets containing single or combined drugs
Publication date: Available online 25 January 2020Source: International Journal of PharmaceuticsAuthor(s): Anis Yohana Chaerunisaa, Rebaz Ali, Martin Körber, Roland BodmeierAbstractThe aim of this work was to develop a mathematical model to estimate the drug release from a conventional single-compartment reservoir pellet and extend its applicability to multi-compartment reservoir pellets. Conventional pellets were prepared by layering the drug onto starter-core then applying various ethylcellulose / HPC coatings for drug release control. Multi-layered pellets comprised a first drug layer of propranolol HCl (D1) follow...
Source: International Journal of Pharmaceutics - January 26, 2020 Category: Drugs & Pharmacology Source Type: research

An update on formulation strategies of benzoyl peroxide in efficient acne therapy with special focus on minimizing undesired effects
This article aims to give a comprehensive overview of the published experimental vehicle systems and to identify the fundamental rationales. With regard to the formulation, an increase in the tolerability of BPO can essentially be achieved by combining BPO with re-fattening and moisturizing substances, by incorporating it and controlling its release, as well as by targeted deposition of the active ingredient at the site of action, i.e. drug targeting. Recently, novel particulate formulations have been proposed that combine several of these design principles and are expected to bring new developments in this dynamic field o...
Source: International Journal of Pharmaceutics - January 24, 2020 Category: Drugs & Pharmacology Source Type: research

Engineered DNA nanodrugs alleviate inflammation in inflammatory arthritis
This study demonstrates that an engineered DNA nanodrug (TD-P-dODN) enhances the efficacy of nucleic acid drugs and represents a promising strategy for RA treatment.Graphical abstractThe intracellular NF-κB pathway is activated in the inflamed synovium. The degradation of IκB results in the release of the P50/P65 complex that can translocate into the nucleus and initiate the transcription of inflammatory protein. TD-P-dODNs insert across the P50/P65 complex in cytoplasm and inhibit its downstream activities, which ultimately reduces inflammation in vitro and in vivo. (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 24, 2020 Category: Drugs & Pharmacology Source Type: research

Transdermal delivery enhancement of carvacrol from Origanum vulgare L. essential oil by microemulsion
Publication date: Available online 23 January 2020Source: International Journal of PharmaceuticsAuthor(s): Natnaree Laothaweerungsawat, Waranya Neimkhum, Songyot Anuchapreeda, Jakkapan Sirithunyalug, Wantida ChaiyanaAbstractCarvacrol has been reported for analgesic and anti-inflammatory activity by cyclooxygenase inhibition but it could induce gastrointestinal toxicity because of its non-selective inhibition. Therefore, the present study aimed to develop transdermal microemulsion from Origanum vulgare essential oil to deliver carvacrol into and through the skin which would overwhelm the gastrointestinal problems. O. vulgar...
Source: International Journal of Pharmaceutics - January 24, 2020 Category: Drugs & Pharmacology Source Type: research

Facile Nose-to-brain delivery of Rotigotine-loaded Polymer Micelles Thermosensitive Hydrogels: in vitro Characterization and in vivo Behavior Study
In conclusion, the ROT-PM-TSG system has proven to be a potential application prospect as a ROT nose-to-brain delivery system.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 24, 2020 Category: Drugs & Pharmacology Source Type: research

Corrigendum to “Apoferritin nanocages loading mertansine enable effective eradiation of cancer stem-like cells in vitro” [Int. J. Pharm. 553 (2018) 201–209]
Publication date: Available online 22 January 2020Source: International Journal of PharmaceuticsAuthor(s): Tao Tan, Yuqi Wang, Hong Wang, Haiqiang Cao, Zhiwan Wang, Jing Wang, Jie Li, Yaping Li, Zhiwen Zhang, Siling Wang (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 23, 2020 Category: Drugs & Pharmacology Source Type: research

Highly Stabilized Nanocrystals Delivering Ginkgolide B in Protecting against the Parkinson’s Disease
In this study, Ginkgolide B (GB), a potent anti-Parkinsonism compound, was selected to verify the utility of NCs to effectively accumulate GB in both the blood and brain. Highly stabilized GB-NCs had small sizes, high rates of dissolution, enhanced cellular uptake and permeability. The GB-NCs could protect neurons against cytotoxicity induced by MPP+, and showed no toxicity in zebrafish. Fluorescent imaging in zebrafish indicated high levels of the NCs in both the gut and brain. When orally administrated to rats, the GB-NCs showed higher drug plasma levels and neuronal drug distributions when compared to control groups. Im...
Source: International Journal of Pharmaceutics - January 23, 2020 Category: Drugs & Pharmacology Source Type: research

Electrospun anti-inflammatory patch loaded with essential oils for wound healing
Publication date: Available online 22 January 2020Source: International Journal of PharmaceuticsAuthor(s): Sara García-Salinas, Michael Evangelopoulos, Enrique Gámez-Herrera, Manuel Arruebo, Silvia Irusta, Francesca Taraballi, Gracia Mendoza, Ennio TasciottiAbstractWound healing is a complex process that consists of three overlapping phases: inflammation, proliferation, and remodeling. A bacterial infection can increase inflammation and delay this process. Microorganisms are closely related to the innate immune system, such as macrophages and neutrophils, as they can start an inflammatory cascade. Essential o...
Source: International Journal of Pharmaceutics - January 23, 2020 Category: Drugs & Pharmacology Source Type: research

Formation of ciprofloxacin nanocrystals within liposomes by spray drying for controlled release via inhalation
Publication date: Available online 22 January 2020Source: International Journal of PharmaceuticsAuthor(s): Isra Khatib, Patricia Tang, Juanfang Ruan, David Cipolla, Francis Dayton, James D. Blanchard, Hak-Kim ChanAbstractThe present study was conducted to harness spray drying technology as a novel method of producing Ciprofloxacin nanocrystals inside liposomes (CNL) for inhalation delivery. Liposomal ciprofloxacin dispersions were spray dried with sucrose as a lyoprotectant in different mass ratios (0.5:1, 1:1 and 2:1 sucrose to lipids), along with 2% w/w magnesium stearate and 5% w/w isoleucine as aerosolization enhancers...
Source: International Journal of Pharmaceutics - January 23, 2020 Category: Drugs & Pharmacology Source Type: research

Non-destructive dose verification of two drugs within 3D printed polyprintlets
Publication date: Available online 23 January 2020Source: International Journal of PharmaceuticsAuthor(s): Sarah J Trenfield, Hui Xian Tan, Alvaro Goyanes, David Wilsdon, Martin Rowland, Simon Gaisford, Abdul W BasitAbstractThree-dimensional printing (3DP) is a revolutionary technology in pharmaceuticals, enabling the personalisation of flexible-dose drug products and 3D printed polypills (polyprintlets). A major barrier to entry of this technology is the lack of non-destructive quality control methods capable of verifying the dosage of multiple drugs in polyprintlets at the point of dispensing. In the present study, 3D pr...
Source: International Journal of Pharmaceutics - January 23, 2020 Category: Drugs & Pharmacology Source Type: research

Colon-targeting of progesterone using hybrid polymeric microspheres improves its bioavailability and in vivo biological efficacy
This study aims to enhance progesterone (PG) oral bioavailability via its incorporation into hybrid colon-targeted pectin/NaCMC microspheres (MS) cross-linked with Zn2+ and Al3+. The MS were characterized for particle morphology, encapsulation efficiency, swelling behavior, drug release, mucoadhesivity and colon-specific degradability. Response-surface methodology was adopted to optimize the fabrication conditions. Enhancement of in vivo drug performance was evaluated through pharmacokinetic and pharmacodynamic studies. The optimized formulation was typically spherical with a mean diameter of 1031 µm and drug entrapm...
Source: International Journal of Pharmaceutics - January 23, 2020 Category: Drugs & Pharmacology Source Type: research

Vitamin E-based Prodrug Self-delivery for Nanoformulated Irinotecan with Synergistic Antitumor Therapeutics
In this study, a novel vitamin E succinate-based formulation of Ir (VES-Ir) combined with nanoscaled characteristics and synergistic combination was constructed through esterification. The conjugation makes amphiphilic VES-Ir prodrug self-assemble into nanoparticles with a fine diameter (VES-Ir NPs, 75.4 nm) of spherical morphology. Furthermore, VES-Ir NPs with a 1:1 drug-to-drug ratio was demonstrated to possess respectable physiological stability within 72 h test, while can react to pH/esterase-sensitive drug release in lysosomes internalized into tumor cells, potentially highlighting their alleviating side effects. Comp...
Source: International Journal of Pharmaceutics - January 23, 2020 Category: Drugs & Pharmacology Source Type: research

Boosting Transdermal delivery of Atorvastatin Calcium via o/w Nanoemulsifying System: Two-step optimization, ex vivo and in vivo evaluation
In conclusion, data revealed no correlation between ex vivo and in vivo studies explained by the collapse of the follicles in ex vivo skin permeation study, leaving only the lipoidal pathway for NE to pass through, thus only NE components, neither nanosizing nor other reported mechanisms, are the main influencing factors. In vivo experiments suggested that o/w NE changed ATOR pathway to follicular delivery leading to accumulation of NE in follicles and consequently a prolonged plasma profile.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 23, 2020 Category: Drugs & Pharmacology Source Type: research

Drug-loaded implantable surgical cavity-adaptive hydrogels for prevention of local tumor recurrence
Publication date: Available online 21 January 2020Source: International Journal of PharmaceuticsAuthor(s): Bo Zhuang, Ting Chen, Zhimei Xiao, Yiguang JinAbstractHigh local post-surgical cancer recurrence severely impairs the patients’ prognosis and survival rates. Here, an injectable in situ forming hydrogel was designed to locally controlled release gemcitabine (GEM) and doxorubicin (DOX) to prevent local cancer recurrence. The hydrogel was rapidly formed at the post-surgical cavity after the aldehyde hyaluronic acid (HA-CHO) and the carboxymethyl chitosan (CM-CS) were mixed and immediately injected. Meanwhile, DOX ...
Source: International Journal of Pharmaceutics - January 22, 2020 Category: Drugs & Pharmacology Source Type: research

Continuous twin screw granulation: impact of binder addition method and surfactants on granulation of a high-dosed, poorly soluble API
Publication date: Available online 22 January 2020Source: International Journal of PharmaceuticsAuthor(s): Christoph Portier, Tamas Vigh, Giustino Di Pretoro, Thomas De Beer, Chris Vervaet, Valérie VanhoorneAbstractDespite the recent commercialization of several drug products manufactured through continuous manufacturing techniques, knowledge on the formulation aspect of these techniques, such as twin screw wet granulation, is still rather limited. Previous research identified lactose/MCC/HPMC as a robust platform formulation for several model formulations, although granulation of the high-dosed, poorly soluble API ...
Source: International Journal of Pharmaceutics - January 22, 2020 Category: Drugs & Pharmacology Source Type: research

Synthesis of cationic quaternized pullulan derivatives for miRNA delivery
In conclusion, the formation of polyplexes using cationic derivatives of pullulan with miRNA provided an easy and versatile method for polysaccharide nanoparticle production in aqueous media and could be a new promising platform for gene delivery.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 22, 2020 Category: Drugs & Pharmacology Source Type: research

Oral formulation strategies to improve the bioavailability and mitigate the food effect of abiraterone acetate
Publication date: Available online 22 January 2020Source: International Journal of PharmaceuticsAuthor(s): Hayley B. Schultz, Tahlia R. Meola, Nicky Thomas, Clive A. PrestidgeAbstractAbiraterone acetate, marketed as Zytiga®, is an antiandrogen medication used in the treatment of prostate cancer. Abiraterone acetate is a BCS Class IV compound associated with several oral delivery challenges. Its low solubility and high lipophilicity lead to poor oral bioavailability (
Source: International Journal of Pharmaceutics - January 22, 2020 Category: Drugs & Pharmacology Source Type: research

Crystallo-co-spray drying as a new approach to manufacturing of drug/excipient agglomerates: impact of processing on the properties of paracetamol and lactose mixtures
Publication date: Available online 22 January 2020Source: International Journal of PharmaceuticsAuthor(s): Alan F. McDonagh, Lidia TajberAbstractThe novel process of crystallo-co-spray drying of paracetamol and α-lactose monohydrate was investigated by varying the spray dryer inlet temperature and inlet feed solvent composition. A crystalline agglomerate was obtained with no change to the physical structure of either component throughout both investigations and with possible interactions between the hydroxyl groups of the α-lactose monohydrate and the amide and hydroxyl groups of the paracetamol detected. The p...
Source: International Journal of Pharmaceutics - January 22, 2020 Category: Drugs & Pharmacology Source Type: research

Prediction of drug dissolution from Toremifene 80 mg tablets by NIR spectroscopy
Publication date: 15 March 2020Source: International Journal of Pharmaceutics, Volume 577Author(s): Krista Ojala, Mika Myrskyranta, Anni Liimatainen, Hanna Kortejärvi, Anne JuppoAbstractThe aim of our study was to justify substitution of dissolution analysis for NIR measurement of Toremifene 80 mg tablets. We studied implementation of a NIRS method by integrating the method development to discrimination power of the dissolution method. Hence, we analyzed 20 DoE tablet batches and studied which of the critical formulation factors affecting dissolution were statistically significant. To study if these factors can b...
Source: International Journal of Pharmaceutics - January 22, 2020 Category: Drugs & Pharmacology Source Type: research

Critical steps during the prilling process of molten lipids: Main stumbling blocks due to pharmaceutical excipient properties
Publication date: 25 February 2020Source: International Journal of Pharmaceutics, Volume 576Author(s): F. Séquier, V. Faivre, J.-Y. Lanne, G. Daste, M. Renouard, S. LesieurAbstractPrilling by ultrasonic jet break-up is an efficient process to produce perfectly spherical microparticles homogeneous in size. However, the material properties could affect the manufacturability and the final product properties especially with lipid-based excipients which often exhibit complex structural properties. This work presents the characterisation of six lipid-based excipients differing by their melting point and polymorphic behavi...
Source: International Journal of Pharmaceutics - January 21, 2020 Category: Drugs & Pharmacology Source Type: research

Evaluating supersaturation in vitro and predicting its performance in vivo with Biphasic Gastrointestinal Simulator: A case study of a BCS IIB drug
In conclusion, CoPVP and HPMC increased and prolonged the supersaturation of apatinib, and then improved its bioavailability. Moreover, BGIS was demonstrated to be a significant approach for simulating in vivo conditions for in vitro-in vivo correlation in a supersaturation study. This study presents a promising approach for evaluating supersaturation, screening precipitation inhibitors in vitro, and predicting their performances in vivo.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 19, 2020 Category: Drugs & Pharmacology Source Type: research

Sincere thanks to Véronique Préat and Thorsteinn Loftsson and a Warm Welcome to Carmen Alvarez-Lorenzo and Juan Manuel Irache
Publication date: Available online 17 January 2020Source: International Journal of PharmaceuticsAuthor(s): Juergen Siepmann (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 18, 2020 Category: Drugs & Pharmacology Source Type: research

Poorly soluble drugs
Publication date: Available online 17 January 2020Source: International Journal of PharmaceuticsAuthor(s): Juergen Siepmann, Thomas Rades, Anette Muellertz, Thorsteinn Loftsson (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 18, 2020 Category: Drugs & Pharmacology Source Type: research

Nanostructured lipid carriers-mediated brain delivery of carbamazepine for improved in vivo anticonvulsant and anxiolytic activity
Publication date: Available online 16 January 2020Source: International Journal of PharmaceuticsAuthor(s): Namrah Khan, Fawad Ali Shah, Isra Rana, Muhammad Mohsin Ansari, Fakhar ud Din, Syed Zaki Husain Rizvi, Waqar Aman, Gwan-Yeong Lee, Eun-Sun Lee, Jin-Ki Kim, Alam ZebAbstractThe limited brain delivery of carbamezapine (CBZ) presents a major hurdle in the successful epilepsy treatment. The potential of carbamezapine-loaded nanostructured lipid carriers (CBZ-NLCs) for improved brain delivery is investigated in the current study. CBZ-NLCs were prepared by using binary mixture of trilaurin and oleic acid as a lipid core sta...
Source: International Journal of Pharmaceutics - January 16, 2020 Category: Drugs & Pharmacology Source Type: research

Efficacy of SPM-NONOate following intrapulmonary delivery in promoting absorptions of poorly absorbed macromolecules in rats and the underling mechanism
Publication date: Available online 16 January 2020Source: International Journal of PharmaceuticsAuthor(s): Yang Gao, Guangli Liao, Shucong Wang, Ya Sun, Xin Long, Yan Ma, Hailong ZhangAbstractThis research aims to investigate the potential of N-[4-[1-(3-Aminopropyl)-2-hydroxy-2-nitrosohydrazino]butyl]-1,3-propanediamine (SPM-NONOate) for promoting the absorption of poorly absorbed macromolecules delivered by intrapulmonary route. Influence of SPM-NONOate on the drug absorption was characterized by using a series of fluorescein isothiocyanate-labeled dextrans (FDs) as affordable models of hydrophilic macromolecules with est...
Source: International Journal of Pharmaceutics - January 16, 2020 Category: Drugs & Pharmacology Source Type: research

Prediction of drug dissolution from Toremifene 80 mg tablets using NIR spectroscopy
Publication date: Available online 16 January 2020Source: International Journal of PharmaceuticsAuthor(s): Krista Ojala, Mika Myrskyranta, Anni Liimatainen, Hanna Kortejärvi, Anne JuppoAbstractThe aim of our study was to justify substitution of dissolution analysis for NIR measurement of Toremifene 80 mg tablets. We studied implementation of a NIRS method by integrating the method development to discrimination power of the dissolution method. Hence, we analyzed 20 DoE tablet batches and studied which of the critical formulation factors affecting dissolution were statistically significant. To study if these factors can...
Source: International Journal of Pharmaceutics - January 16, 2020 Category: Drugs & Pharmacology Source Type: research

Application of machine learning to predict monomer retention of therapeutic proteins after long term storage
Publication date: Available online 15 January 2020Source: International Journal of PharmaceuticsAuthor(s): Lorenzo Gentiluomo, Dierk Roessner, Wolfgang FrießAbstractAn important aspect of initial developability assessments as well formulation development and selection of therapeutic proteins is the evaluation of data obtained under accelerated stress condition, i.e. at elevated temperatures. We propose the application of artificial neural networks (ANNs) to predict long term stability in real storage condition from accelerated stability studies and other high-throughput biophysical properties e.g. the first apparent ...
Source: International Journal of Pharmaceutics - January 16, 2020 Category: Drugs & Pharmacology Source Type: research

Formulation of simvastatin chitosan nanoparticles for controlled delivery in bone regeneration: optimization using Box-Behnken design, stability and in vivo study
This study aims to formulate and optimize simvastatin loaded chitosan-tripolyphosphate nanoparticle (SIM CS-TPP NPs) using ionic gelation method to provide a local delivery system that control and sustain the release of simvastatin in the desired dose to promote bone regeneration. Box-Behnken design was adopted for optimization of the formulation variables of the prepared nanoparticles namely, CS percentage, TPP percentage and homogenization time. The optimized formula was selected and characterized by transmission electronic microscopy, in-vitro release, swelling index and storage stability. The ability of the optimum for...
Source: International Journal of Pharmaceutics - January 16, 2020 Category: Drugs & Pharmacology Source Type: research

Novel ultrasmall nanomicelles based on rebaudioside A: A potential nanoplatform for the ocular delivery of pterostilbene
Publication date: Available online 15 January 2020Source: International Journal of PharmaceuticsAuthor(s): Kaichao Song, Meng Xin, Fan Zhang, Wenjing Xie, Mingyue Sun, Xianggen WuAbstractRebaudioside A (RA) self-assembled into ultrasmall nanomicelles can be utilized as ocular drug delivery system; nevertheless, the therapeutic efficacy of RA micelles has not evaluated thus far. In this manuscript, the RA micelles are thought to strengthen the therapeutic effects of pterostilbene (Pt). Results showed that Pt can be highly encapsulated into RA micelles with ultrasmall particle sizes (3.99 ± 0.03 nm) with a uniform dis...
Source: International Journal of Pharmaceutics - January 16, 2020 Category: Drugs & Pharmacology Source Type: research

ChABC-Loaded PLGA Nanoparticles: A Comprehensive Study on Biocompatibility, Functional Recovery, and Axonal Regeneration in Animal Model of Spinal Cord Injury
According to this study, the loaded particles can potentially serve as a suitable candidate for spinal cord repair, functional recovery and axonal regeneration.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 16, 2020 Category: Drugs & Pharmacology Source Type: research