Delivery of docetaxel using pH-sensitive liposomes based on D-?-tocopheryl poly(2-ethyl-2-oxazoline) succinate: comparison with PEGylated liposomes
This study aimed to investigate the ability of the novel materials d-α-tocopheryl poly(2-ethyl-2-oxazoline) succinate (TPOS) to construct pH-sensitive liposomes. TPOS was initially synthesized and characterized by thin-layer chromatography (TLC), fourier transform infrared spectroscopy, and 1H-NMR. The buffering capacity of polyethylene glycol- distearoyl phosphatidylethanolamine (PEG-DSPE) and TPOS was determined by acid-base titration, and TPOS displayed a slower downtrend and gentler slope of titration curve than PEG-DSPE within pH 7.4-5.0. Studies on the in vitro drug release demonstrated that TPOS modified docetaxel ...
Source: Asian Journal of Pharmaceutical Sciences - September 20, 2018 Category: Drugs & Pharmacology Source Type: research

Triphenylphosphonium-modified mitochondria-targeted paclitaxel nanocrystals for overcoming multidrug resistance
Publication date: Available online 18 September 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Xue Han, Ruijuan Su, Xiuqing Huang, Yingli Wang, Xiao Kuang, Shuang Zhou, Hongzhuo LiuAbstractMitochondria are currently known as novel targets for treating cancer, especially for tumors displaying multidrug resistance (MDR). This present study aimed to develop a mitochondria-targeted delivery system by using triphenylphosphonium cation (TPP+)-conjugated Brij 98 as the functional stabilizer to modify paclitaxel (PTX) nanocrystals (NCs) against drug-resistant cancer cells. Evaluations were performed on 2D monolayer...
Source: Asian Journal of Pharmaceutical Sciences - September 20, 2018 Category: Drugs & Pharmacology Source Type: research

Cooperative effect of polyvinylpyrrolidone and HPMC E5 on dissolution and bioavailability of nimodipine solid dispersions and tablets
In this study, SD of nimodipine (NMP) and corresponding tablets were prepared through solvent method and fluid bed granulating one step technique respectively. Discriminatory dissolution media were used to obtain reliable dissolution results. Meanwhile, the stability study of SDs was investigated with storage under high temperature and humidity conditions. Moreover, the solubility of SDs was measured to explore the effect of carriers. The preparations were characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and Fourier-transform infrared spectroscopy (FTIR). Dramatical improvements in...
Source: Asian Journal of Pharmaceutical Sciences - September 20, 2018 Category: Drugs & Pharmacology Source Type: research

MSNCs and MgO-MSNCs as drug delivery systems to control the adsorption kinetics and release rate of indometacin
Publication date: Available online 20 September 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Xin Zheng, Shuang Feng, Xiudan Wang, Zhenning Shi, Yuling Mao, Qinfu Zhao, Siling WangAbstractMesoporous silica cocoon materials (MSNCs) and MgO doped mesoporous silica cocoons (MgO-MSNCs) with the cocoon-like hierarchical morphology and different alkalinities were synthesized as carriers for acidic drugs. Indomethacin (IMC) was selected as a model drug and loaded into carriers. All materials and the drug-loaded samples were characterized by nitrogen adsorption, FTIR spectroscopy, transmission electron microscopy ...
Source: Asian Journal of Pharmaceutical Sciences - September 20, 2018 Category: Drugs & Pharmacology Source Type: research

Effects of granulation process variables on the physical properties of dosage forms by combination of experimental design and principal component analysis
Publication date: Available online 18 September 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Prakash Thapa, Du Hyung Choi, Min-Soo Kim, Seong Hoon JeongAbstractThe current study was to understand how process variables of high shear wet granulations affect physical properties of granules and tablets. The knowledge gained was intended to be used for Quality-by-Design based process design and optimization. The variables were selected based on the risk assessment as impeller speed, liquid addition rate, and wet massing time. Formulation compositions were kept constant to minimize their influence on granules p...
Source: Asian Journal of Pharmaceutical Sciences - September 18, 2018 Category: Drugs & Pharmacology Source Type: research

The appliances and prospects of aurum nanomaterials in biodiagnostics, imaging, drug delivery and combination therapy
Publication date: Available online 14 September 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Dan Yang, Feiyang Deng, Dechun Liu, Bo He, Bing He, Xing Tang, Qiang ZhangAbstractAurum nanomaterials (ANM), combining the features of nanotechnology and metal elements, have demonstrated enormous potential and aroused great attention on biomedical applications over the past few decades. Particularly, their advantages, such as controllable particle size, flexible surface modification, higher drug loading, good stability and biocompatibility, especially unique optical properties, promote the development of ANM in b...
Source: Asian Journal of Pharmaceutical Sciences - September 15, 2018 Category: Drugs & Pharmacology Source Type: research

The development of a method to quantify total and free irinotecan and 7-ethyl-10-hydroxycamptothecin (SN-38) for pharmacokinetic and bio-distribution studies after administration of irinotecan liposomal formulation
This study focuses on separation of non-liposomal CPT-11, evaluation of the pharmacokinetics of free CPT-11 and total CPT-11 and bio-distribution after intravenous administration of CPT-11 liposome. Free CPT-11 in plasma was separated by solid-phase extraction (SPE). The amount of total CPT-11 and main metabolite 7-ethyl-10-hydroxycamptothecin (SN-38) in plasma was quantified by ultra-performance liquid chromatography–MS/MS. The calibration curves fitted well and lower limit of quantitation for SN-38, free CPT-11, total CPT-11 and CPT-11 in tissue and were 5 ng/ml, 10 ng/ml, 4.44 ng/ml and 25 ng/ml respectively. The reco...
Source: Asian Journal of Pharmaceutical Sciences - September 12, 2018 Category: Drugs & Pharmacology Source Type: research

A hybrid genipin-crosslinked dual-sensitive hydrogel /nanostructured lipid carrier ocular drug delivery platform
In conclusion, the hybrid NLC-based hydrogel has a promising potential for application in ocular drug delivery.Graphical Abstract. An innovative hybrid drug delivery platform: genipin-crosslinked dual pH- and thermo-sensitive hydrogel/nanostructured lipid carrier has been exploited for ocular delivery of baicalin (BN). (Source: Asian Journal of Pharmaceutical Sciences)
Source: Asian Journal of Pharmaceutical Sciences - September 11, 2018 Category: Drugs & Pharmacology Source Type: research

Extended Tacrolimus Release via the Combination of Lipid-based Solid Dispersion and HPMC Hydrogel Matrix Tablets
The objective of this study is to evaluate the feasibility of obtaining extended release of tacrolimus by a novel combination of lipid-based solid dispersion and matrix-type extended release tablet techniques. Tacrolimus solid dispersion was prepared using glycerylbehenate (Compritol® ATO888) and Pluronic F127 as the carrier materials with hot-melt method, which was then blended with hydrogel matrix materials, such as HPMC and lactose, the powders were directly compressed into tablets. In vitro drug release tests were carried out to evaluate the performance of the solid dispersions and the tablets. The dissolution rate of...
Source: Asian Journal of Pharmaceutical Sciences - September 8, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of Kupffer cells depletion on ABC phenomenon induced by Kupffer cells-targeted liposomes
In this study, the correlation between Kupffer cells (KCs) and ABC phenomenon has been studied by KCs-targeted liposomes inducing ABC phenomenon and KCs depletion. In other words, the 4-aminophenyl-α-D-mannopyranoside (APM) lipid derivative DSPE-PEG2000-APM (DPM), and 4-aminophenyl-β-L-fucopyranoside (APF) lipid derivative DSPE-PEG2000-APF (DPF) were conjugated and modified on alendronate sodium (AD) liposomes to specifically target and deplete KCs. The dual-ligand modified PEGylated liposomes (MFPL) showed stronger ability to damage KCs in vitro and in vivo, which also could indirectly illustrate that dual-ligand mod...
Source: Asian Journal of Pharmaceutical Sciences - September 5, 2018 Category: Drugs & Pharmacology Source Type: research

Cyclodextrin/chitosan nanoparticles for oral ovalbumin delivery: Preparation, characterization and intestinal mucosal immunity in mice
In conclusion, our data suggested that CD/CS nanoparticles could serve as a promising antigen-delivery system for oral vaccination.Graphical abstract (Source: Asian Journal of Pharmaceutical Sciences)
Source: Asian Journal of Pharmaceutical Sciences - September 1, 2018 Category: Drugs & Pharmacology Source Type: research

Optimizing pH-sensitive and time-dependent polymer formula of colonic pH-responsive pellets to achieve precise drug release
In conclusion, ES100-ERS NCO colonic delivery system achieved reduced coating thickness and improved colonic targeting compared with traditional delivery system (ERS-ES100 TCO). In addition, the similarity factors (f2) value of sophoridine and matrine for investigated formulation were within 50-100 and> 80, demonstrating that sophoridine and matrine in all formulations achieved a synchronous release.Graphical abstractTASA(total alkaloids of sophora alopecuroides) pH-sensitive and time-dependent pellets were prepared by extrusion-spheronization coating with Eudragit RS30D and Eudragit S100. In order to achieve precise colon...
Source: Asian Journal of Pharmaceutical Sciences - August 28, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of raw material variability of glipizide on the in vitro dissolution rate and in vivo bioavailability performance: the importance of particle size
The objective of this study was to understand the impact of active pharmaceutical ingredients (API) particle size on a re-developed generic product of glipizide and to improve its formulation so that it exhibits bioequivalent to that of the reference listed drug (RLD). Two commercial batches of APIs (API-1 and API-2) with the same polymorphism and one batch of home-made APIs (API-3) with super-small particle size were used in the present study. The in vitro dissolution profiles of the tested formulations were compared with the RLD in a series of dissolution media. Then, the impact of particle size on in vivo absorption was...
Source: Asian Journal of Pharmaceutical Sciences - August 28, 2018 Category: Drugs & Pharmacology Source Type: research

Nanomaterials for modulating innate immune cells in cancer immunotherapy
Publication date: Available online 23 August 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Quoc-Viet Le, Geon Yang, Yina Wu, Ho Won Jang, Mohammadreza Shokouhimehr, Yu-Kyoung OhAbstractCancer immunotherapy has been intensively investigated in both preclinical and clinical studies. Whereas chemotherapies use cytotoxic drugs to kill tumor cells, cancer immunotherapy is based on the ability of the immune system to fight cancer. Tumors are intimately associated with the immune system: they can suppress the immune response and/or control immune cells to support tumor growth. Immunotherapy has yielded promising ...
Source: Asian Journal of Pharmaceutical Sciences - August 24, 2018 Category: Drugs & Pharmacology Source Type: research

Double-layered osmotic pump controlled release tablets of actarit: In vitro and in vivo evaluation
Publication date: Available online 19 August 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Yuenan Li, Hao Pan, Hongliang Duan, Jianting Chen, Zhihong Zhu, Jingxin Fan, Pingfei Li, Xinggang Yang, Weisan PanAbstractThe aim of the study was to develop actarit double-layered osmotic pump tablets to overcome the weak points of actarit common tablets, such as short half-life and large plasma concentration fluctuations. Single factor experiment and orthogonal test were applied to optimize the formulation; the pharmacokinetic study was performed in beagle dogs adopting actarit common tablets as reference tablets. ...
Source: Asian Journal of Pharmaceutical Sciences - August 20, 2018 Category: Drugs & Pharmacology Source Type: research