Improved Dissolution and Oral Absorption by Co-grinding Active Drug Probucol and Ternary Stabilizers Mixtures with Planetary Beads-Milling Method
The objective of this work is to construct a nanosuspension drug delivery system of probucol, a BCS II drug, in order to improve its dissolution and oral bioavailability. The wet milling procedure using planetary beads-milling equipment was utilized to grind the raw probucol to ultrafine nanoparticle/nanocrystal aqueous suspension that was further solidified by freeze-drying process. Cellulose derivatives of different substitution groups and molecular weights, including HPMC, HPC, and MC, were evaluated as the primary stabilizer of probucol nanosuspension. Ternary stabilizers system composed of a primary stabilizer (cellul...
Source: Asian Journal of Pharmaceutical Sciences - December 12, 2018 Category: Drugs & Pharmacology Source Type: research

Investigation of molecular aggregation mechanism of glipizide/cyclodextrin complexation by combined experimental and molecular modeling approaches
Publication date: Available online 8 December 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Tianhe Huang, Qianqian Zhao, Yan Su, Defang OuyangAbstractCyclodextrin complexation is a wise strategy to enhance aqueous solubility of water-insoluble drugs. However, the aggregation mechanism of drug-cyclodextrin complexes is still unclear. This research aimed to investigate the molecular aggregation mechanism of glipizide/cyclodextrin complexation by the combination of experimental and modeling methods. Binding free energies between glipizide and cyclodextrins from modeling calculations were higher than those by ...
Source: Asian Journal of Pharmaceutical Sciences - December 8, 2018 Category: Drugs & Pharmacology Source Type: research

Exploring the Relationship of Hyaluronic acid Molecular Weight and Active Targeting Efficiency for Designing Hyaluronic acid-modified Nanoparticles
In this study, we constituted three HA-functionalized Dox-loaded NPs (Dox/HCVs) different HA MWs (7, 63, and 102 kDa) and attempted to illustrate the effects of HA MW on the targeting efficiency. The three Dox/HCVs had similar physiochemical and pharmaceutical characteristics, but showed different affinity to CD44 receptor. Furthermore, Dox/HCV-63 exerted the best targeting effect and the highest cytotoxicity compared with Dox/HCV-7 and Dox/HCV-102. It was interesting to found that both the HA-CD44 binding affinity and induced CD44 clustering by HA-based NPs were HA MW-dependent, the two of which determine the apparent tar...
Source: Asian Journal of Pharmaceutical Sciences - December 7, 2018 Category: Drugs & Pharmacology Source Type: research

Piperacillin enhances the inhibitory effect of tazobactam on β-lactamase through inhibition of organic anion transporter 1/3 in rats
Publication date: Available online 7 December 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Shilei Yang, Zhihao Liu, Changyuan Wang, Shijie Wen, Qiang Meng, Xiaokui Huo, Huijun Sun, Xiaodong Ma, Jinyong Peng, Zhonggui He, Kexin LiuAbstractTo assess the mechanism of the pharmacokinetic interaction between piperacillin and tazobactam, renal excretion and pharmacokinetic studies of piperacillin/tazobactam were investigated in normal and bacteremia rats. A bacteremia model was established to investigate the pharmacokinetic properties of piperacillin and tazobactam under different conditions. Renal slices were ...
Source: Asian Journal of Pharmaceutical Sciences - December 7, 2018 Category: Drugs & Pharmacology Source Type: research

Magnetic and CD44 Receptor Dual Targeting Redox-Responsive Polymeric Micelle for Precise Delivery of Gambogic Acid to Triple-Negative Breast Cancer
In conclusion, the tumor magnetic and CD44 receptor dual targeting redox-responsive multifunctional magnetic polymeric micelle (mPEG-HA/CSO-SS-Hex/Fe3O4/GA) has the potential to be an effective carrier in targeted drug delivery for the TNBC chemotherapy.Graphical abstractScheme of mPEG-HA/CSO-SS-Hex/Fe3O4/GA micelle preparation and magnetism-enhanced EPR in vivo and in vitro trafficking pathway of the polymeric micelles. The intracellular trafficking pathway includes receptor-meditated cellular internalization and redox-responsive triggered micelle disassembly and drug release. (Source: Asian Journal of Pharmaceutical Sciences)
Source: Asian Journal of Pharmaceutical Sciences - December 5, 2018 Category: Drugs & Pharmacology Source Type: research

Redox-Sensitive, PEG-Shielded Carboxymethyl PEI Nanogels Silencing MicroRNA-21, Sensitizes Resistant Ovarian Cancer Cells to Cisplatin
Publication date: Available online 1 December 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Sanaz Javanmardi, Ali Mohammad Tamaddon, Mahmoud Reza Aghamaali, Ladan Ghahramani, Samira Sadat AbolmaaliAbstractA series of branched polyethylenimine (PEI) modifications including PEGylation (PEG2k-PEI) for steric shielding, redox-sensitive crosslinking for synthesis PEG2k-PEI-ss nanogels and subsequent carboxymethylation (PEG2k-CMPEI-ss) for modulation of the polymer pka have been introduced for cellular delivery of Anti-miR-21. The synthesis was characterized using 1H-NMR, FTIR, TNBS, potentiometric titration, pa...
Source: Asian Journal of Pharmaceutical Sciences - December 2, 2018 Category: Drugs & Pharmacology Source Type: research

Apoptosis of A549 cells by small interfering RNA targeting survivin delivery using poly-β-amino ester/guanidinylated O-carboxymethyl chitosan nanoparticles
This study focuses on guanidinylated O-carboxymethyl chitosan (GOCMCS) along with poly-β-amino ester(PBAE) for siRNA delivery. Binding efficiency of PBAE/siRNA/GOCMCS nanoparticles were characterized by gel electrophoresis. The siRNA-loaded nanoparticles were found to be stable in the presence of RNase A, serum and BALF respectively. Fine particle fraction (FPF) which was determined by a two-stage impinger (TSI) was 57.8% ± 2.6%. The particle size and zeta potential of the nanoparticles were 153.8 ± 12.54 nm and +12.2 ± 4.94 mV. In vitro cell transfection studies were carried out with A549 cells. The cellular uptake wa...
Source: Asian Journal of Pharmaceutical Sciences - November 28, 2018 Category: Drugs & Pharmacology Source Type: research

Special issue on “Formulation strategies and manufacturing technologies to enhance non-invasive drug delivery”
Publication date: November 2018Source: Asian Journal of Pharmaceutical Sciences, Volume 13, Issue 6Author(s): Korbinian Löbmann, Adam Bohr, Mingshi Yang (Source: Asian Journal of Pharmaceutical Sciences)
Source: Asian Journal of Pharmaceutical Sciences - November 23, 2018 Category: Drugs & Pharmacology Source Type: research

The application of nitric oxide delivery in nanoparticle-based tumor targeting drug delivery and treatment
Publication date: Available online 22 November 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Lin Qin, Huile GaoAbstractNitric oxide (NO) shows great role in tumor biology. Recent years, more and more researches utilized NO donor in tumor targeting drug delivery and treatment. In this review, we summarized the NO donors by their endogenous and exogenous stimuli. Then the application of NO donors, which was the main aim of the review, was discussed in detailed according to their functions, including inducing tumor cell apoptosis, reversing tumor multidrug resistance, inhibiting tumor metastasis and improving...
Source: Asian Journal of Pharmaceutical Sciences - November 23, 2018 Category: Drugs & Pharmacology Source Type: research

Integration of Phospholipid-Drug Complex into Self-Nanoemulsifying Drug Delivery System to Facilitate Oral Delivery of Paclitaxel
Publication date: Available online 20 November 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Dawei Ding, Bingjun Sun, Weiping Cui, Qin Chen, Xuanbo Zhang, Haotian Zhang, Zhonggui He, Jin Sun, Cong LuoAbstractSelf-nanoemulsifying drug delivery system (SNEDDS) has emerged as a promising platform to improve oral absorption of drugs with poor solubility and low permeability. However, large polarity molecules with insufficient lipid solubility, such as paclitaxel (PTX), would suffer from inferior formulation of SNEDDS due to poor compatibility. Herein, phospholipid-drug complex (PLDC) and SNEDDS were integrated...
Source: Asian Journal of Pharmaceutical Sciences - November 21, 2018 Category: Drugs & Pharmacology Source Type: research

A cabazitaxel liposome for increased solubility, enhanced antitumor effect and reduced systemic toxicity
In this study, a PEG-modified liposome was developed for efficiently encapsulating CBZ, thus enhancing its specific tumor inhibition effect and reducing the systemic toxicity. It was found that the loading efficiency of CBZ into the liposome could be improved with the increase of lipophilic materials, as it could be over 80% under the weight ratio of 20:1 (total lipid: CBZ). The diameter of CBZ loaded liposome (CBZ@Lipo) was ∼100 nm. And the liposome suspending in aqueous medium was stable at 4 °C for at least one month, according to the change of its size distribution. The killing ability of CBZ@Lipo to cancer cells wa...
Source: Asian Journal of Pharmaceutical Sciences - November 21, 2018 Category: Drugs & Pharmacology Source Type: research

Co-amorphous solid dispersion systems of lacidipine-spironolactone with improved dissolution rate and enhanced physical stability
This study demonstrated the novel drug-drug C-ASDs systems is a promising formulation strategy for improved dissolution rate and enhanced physical stability of poorly soluble drugs.Graphical Abstract (Source: Asian Journal of Pharmaceutical Sciences)
Source: Asian Journal of Pharmaceutical Sciences - November 14, 2018 Category: Drugs & Pharmacology Source Type: research

A thorough analysis of the effect of surfactant/s on the solubility and pharmacokinetics of (S) -zaltoprofen
Publication date: Available online 2 November 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Cuong Viet Pham, Jong-Suep Baek, Jong-Hun Park, Sang-Hun Jung, Jong-Seong Kang, Cheong-Weon ChoAbstractUntil now, there are no publications about the preformulation studies on (S)-zaltoprofen ((S)-ZPF). Hence, we first investigated the solubility of (S)-ZPF, screened solubilizers and performed the pharmacokinetic study of (S)-ZPF in the presence of the solubilizers. The measurement of the solubility of (S)-ZPF in 26 different solvents was carried out, including D-alpha tocopheryl polyethylene glycol 1000 succinate (...
Source: Asian Journal of Pharmaceutical Sciences - November 3, 2018 Category: Drugs & Pharmacology Source Type: research

Monitoring film coalescence from aqueous polymeric dispersions using atomic force microscopy: surface topographic and nano-adhesion studies
Publication date: Available online 3 November 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Ziyi Yang, Duncan Q.M. CraigAbstractThe aim of the investigation was to develop the use of topographic and nano-adhesion atomic force microscopy (AFM) studies as a means of monitoring the coalescence of latex particles within films produced from a pharmaceutically relevant aqueous dispersion (Eudragit®NE30D). Films were prepared via spin coating and analysed using AFM, initially via tapping mode for topographic assessment followed by force-distance measurements which allowed assessment of site-specific adhesion. Th...
Source: Asian Journal of Pharmaceutical Sciences - November 3, 2018 Category: Drugs & Pharmacology Source Type: research

Improving the protective effects of aFGF for peripheral nerve injury repair using sulfated chitooligosaccharides
Publication date: Available online 1 November 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Yanmei Liu, Fenglin Yu, Beibei Zhang, Meng Zhou, Yu Bei, Yifan Zhang, Jianzhong Tang, Yan Yang, Yadong Huang, Qi Xiang, Yueping Zhao, Qian Liang, Yang LiuAbstractInjury to the peripheral nerves can result in temporary or life-long neuronal dysfunction and subsequent economic or social disability. Acidic fibroblast growth factor (aFGF) promotes the growth and survival of neurons and is a possible treatment for peripheral nerve injury. Yet, the actual therapeutic utility of aFGF is limited by its short half-life and i...
Source: Asian Journal of Pharmaceutical Sciences - November 2, 2018 Category: Drugs & Pharmacology Source Type: research