Current developments in drug delivery with thermosensitive liposomes
Publication date: Available online 31 October 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Hongshu Bi, Jianxiu Xue, Hong Jiang, Shan Gao, Dongjuan Yang, Yan Fang, Kai ShiAbstractThermosensitive liposomes (TSLs) have been an important research area in the field of tumor targeted chemotherapy. Since the first TSLs appeared that using 1,2-dipalmitoyl-sn-glyce-ro-3-phosphocholine (DPPC) as the primary liposomal lipid, many studies have been done using this type of liposome from basic and practical aspects. While TSLs composed of DPPC enhance the cargo release near the phase transition temperature, it has been...
Source: Asian Journal of Pharmaceutical Sciences - November 1, 2018 Category: Drugs & Pharmacology Source Type: research

Preparation and in vitro-in vivo evaluation of intestinal retention pellets of Berberine chloride to enhance hypoglycemic and lipid-lowing efficacy
Publication date: Available online 25 October 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Guofei Li, Mingming Zhao, Xianying Su, Lin Song, Limei ZhaoAbstractBerberine chloride (BBR) is a pharmacokinetic profile of drug with poor bioavailability but good therapeutic efficacy, which is closely related to the discovery of BBR intestinal target. The major aim of this paper is to develop BBR intestinal retention type sustained-release pellets and evaluate their in vivo and in vitro behaviors base on the aspect of local action on intestinal tract. Here, wet milling technology is used to improve dissolution and...
Source: Asian Journal of Pharmaceutical Sciences - October 25, 2018 Category: Drugs & Pharmacology Source Type: research

Nanocarriers as a powerful vehicle to overcome blood-brain barrier in treating neurodegenerative diseases: focus on recent advances
Publication date: Available online 22 October 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Xiaoqian Niu, Jiejian Chen, Jianqing GaoAbstractNeurodegenerative diseases including Alzheimer's disease, Parkinson's disease, Huntington disease and amyotrophic lateral sclerosis throw a heavy burden on families and society. Related scientific researches make tardy progress. One reason is that the known pathogeny is just the tip of the iceberg. Another reason is that various physiological barriers, especially blood-brain barrier (BBB), hamper effective therapeutic substances from reaching site of action. Drugs in c...
Source: Asian Journal of Pharmaceutical Sciences - October 23, 2018 Category: Drugs & Pharmacology Source Type: research

Folate-targeted nanostructured chitosan/chondroitin sulfate complex carriers for enhanced delivery of bortezomib to colorectal cancer cells
In this study, we successfully incorporated a hydrophobic drug, bortezomib (Bor), into folic acid (FA)-conjugated Cs/Chs self-assembled NPs (Bor/Cs/Chs-FA) for colorectal cancer therapy. The particle size and polydispersity index of Bor/Cs/Chs-FA were ∼196.5 ± 1.2 nm and ∼0.21 ± 0.5, respectively. A pH-dependent release profile was observed, facilitating cancer cell-targeted drug release under an acidic tumor microenvironment. Moreover, in vitro data revealed enhanced cellular uptake and apoptosis in folate receptor-expressing colorectal cancer cells (HCT-116 and HT-29) as compared to that in lung cancer cells (A549)...
Source: Asian Journal of Pharmaceutical Sciences - October 21, 2018 Category: Drugs & Pharmacology Source Type: research

Cellulose based polymers in development of amorphous solid dispersions
Publication date: Available online 18 October 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Rahul B Chavan, Sneha Rathi, Vaskuri G S Sainaga Jyothi, Nalini R ShastriAbstractCellulose derivatives have gained immense popularity as stabilizers for amorphous solid dispersion owing to their diverse physicochemical properties. More than 20 amorphous solid dispersion-based products that have been approved for marketing consist of cellulose derivatives as stabilizers, thus highlighting their importance in generation of amorphous solid dispersions. These polymers offer numerous advantages like drug solubilization, ...
Source: Asian Journal of Pharmaceutical Sciences - October 19, 2018 Category: Drugs & Pharmacology Source Type: research

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. ...
Source: Asian Journal of Pharmaceutical Sciences - October 16, 2018 Category: Drugs & Pharmacology Source Type: research

Delivery of docetaxel using pH-sensitive liposomes based on D-α-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 TLC, FTIR, 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 (DOC) liposomes (TPOS-DOC-L) had a slower drug-release rate a...
Source: Asian Journal of Pharmaceutical Sciences - October 16, 2018 Category: Drugs & Pharmacology Source Type: research

Development of polyurethane foam dressing containing silver and asiaticoside for healing of dermal wound
In conclusion, this innovative foam dressing had potential to be a good candidate for wound treatment.Graphical abstractThe developed foam dressing consisted of three parts; natural polyols, silver nanoparticles and asiaticoside. Adding the natural polyols in polyurethane foam preparation was to increase hydrophilic properties and their characteristics were evaluated. The silver and asiaticoside were then impregnated and their releasing profiles were determined. The animal studies were performed to evaluate the efficacy and safety of the prepared foam dressings. (Source: Asian Journal of Pharmaceutical Sciences)
Source: Asian Journal of Pharmaceutical Sciences - October 16, 2018 Category: Drugs & Pharmacology Source Type: research

Preparation, characterization, and in vitro/vivo evaluation of polymer-assisting formulation of atorvastatin calcium based on solid dispersion technique
Publication date: Available online 12 October 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Wenxiang Dong, Xitong Su, Meng Xu, Mingming Hu, Yinghua Sun, Peng ZhangAbstractDue to low solubility and bioavailability, atorvastatin calcium is confronted with challenge in conceiving appropriate formulation. Solid dispersion of atorvastatin calcium was prepared through the solvent evaporation method, with Poloxamer 188 as hydrophilic carriers. This formulation was then characterized by scanning electron microscopy, differential scanning calorimetry, powder X-ray diffraction and fourier transform infrared spectros...
Source: Asian Journal of Pharmaceutical Sciences - October 13, 2018 Category: Drugs & Pharmacology Source Type: research

Modulating intestinal mucus barrier for nanoparticles penetration by surfactants
Publication date: Available online 12 October 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Xin Zhang, Wei Dong, Hongbo Cheng, Meixia Zhang, Yongqiang Kou, Jian Guan, Qiaoyu Liu, Mingyue Gao, Xiuhua Wang, Shirui MaoAbstractImproving peroral delivery efficiency is always a persistent goal for both small-molecule and macromolecular drug development. However, intestinal mucus barrier which greatly impedes drug-loaded nanoparticles penetration is commonly overlooked. Therefore, in this study, taking fluorescent labeled PLGA (poly (lactic-co-glycolic acid)) nanoparticles as a tool, the influence of anionic and ...
Source: Asian Journal of Pharmaceutical Sciences - October 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 abstractAn innovative hybrid drug delivery platform: genipin-crosslinked dual pH- and thermo-sensitive hydrogel/nanostructured lipid carrier has been exploited for ocular delivery of baicalin. (Source: Asian Journal of Pharmaceutical Sciences)
Source: Asian Journal of Pharmaceutical Sciences - October 10, 2018 Category: Drugs & Pharmacology Source Type: research

Formulation of a film-coated dutasteride tablet bioequivalent to a soft gelatin capsule (Avodart®): Effect of γ-cyclodextrin and solubilizers
Publication date: Available online 5 October 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Mi-Hong Min, Jin-Hyong Park, Mi-Ran Choi, Jong-Hyun Hur, Byung-Nak Ahn, Dae-DuK KimABSTRACTThe aim of this study was to optimize a tablet formulation of dutasteride that is bioequivalent to a commercially available soft gelatin capsule (Avodart®). The effect of cyclodextrin on enhancing the aqueous solubility of dutasteride was investigated, after which the formulation was further optimized with solubilizing polymer and surfactant. Among the cyclodextrins tested, the highest solubility was observed when dutasteride ...
Source: Asian Journal of Pharmaceutical Sciences - October 6, 2018 Category: Drugs & Pharmacology Source Type: research

Redox-sensitive micelles for targeted intracellular delivery and combination chemotherapy of paclitaxel and all-trans-retinoid acid
Publication date: Available online 24 September 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Lingfei Han, Lejian Hu, Fulei Liu, Xin Wang, Xiaoxian Huang, Bowen Liu, Feng Feng, Wenyuan Liu, Wei QuAbstractThe application of paclitaxel (PTX) in clinic has been restricted due to its poor solubility. Several traditional nano-medicines have been developed to improve this defect, while they are still lack of tumor targeting ability and rapid drug release. In this work, an amphiphilic polymeric micelle of hyaluronic acid (HA) - all-trans-retinoid acid (ATRA) with a disulfide bond, was developed successfully for t...
Source: Asian Journal of Pharmaceutical Sciences - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Development of PLGA micro- and nanorods with high capacity of surface ligand conjugation for enhanced targeted delivery
In this study, we prepared anisotropic PLGA nanoparticles with abundant conjugatable surface functional groups by a film stretching-based fabrication method with poly (ethylene-alt-maleic acid) (PEMA). Scanning electron microscopy images showed that microrods and nanorods were successfully fabricated by the PEMA-based film stretching method. The presence of surface carboxylic acid groups was confirmed by confocal microscopy and zeta potential measurements. Using the improved film-stretching method, the amount of protein conjugated to the surface of nanorods was increased three-fold. Transferrin-conjugated, nanorods fabrica...
Source: Asian Journal of Pharmaceutical Sciences - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

PEPT1-mediated prodrug strategy for oral delivery of peramivir
Publication date: Available online 3 October 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Yongbing Sun, Wei Gan, Mingdao Lei, Wei Jiang, Meng Cheng, Junwei He, Qi Sun, Wan Liu, Lvjiang Hu, Yi JinAbstractPeramivir was a novel and highly potent neuraminidase (NA) inhibitor for the treatment of influenza A and B. However, it exhibited a very low oral bioavailability (only 3%) due to the high polarity (log P of −1.4) and the low membrane permeability across the intestine. To utilize the PEPT1-mediated prodrug strategy to improve the oral absorption and develop the oral alternative, seven amino acid ester pr...
Source: Asian Journal of Pharmaceutical Sciences - October 5, 2018 Category: Drugs & Pharmacology Source Type: research