Development of a novel L-sulpiride-loaded quaternary microcapsule: Effect of TPGS as an absorption enhancer on physicochemical characterization and oral bioavailability

Title
Development of a novel L-sulpiride-loaded quaternary microcapsule: Effect of TPGS as an absorption enhancer on physicochemical characterization and oral bioavailability
Author
김경수
Keywords
Administered drug dose; L-sulpiride; Quaternary microcapsule; D-alpha-tocopheryl polyethylene glycol 1000;; succinate; Oral absorption; MODEL-DRUG; IN-VIVO EVALUATION; BIOPHARMACEUTICS CLASSIFICATION-SYSTEM; DRUG-DELIVERY SYSTEM; VITAMIN-E TPGS; SOLID LIPID NANOPARTICLES; INTESTINAL-ABSORPTION; AQUEOUS SOLUBILITY; PARTICLE-SIZE; SOLUBLE DRUG
Issue Date
2016-11
Publisher
Elsevier
Citation
Colloids and Surfaces B: Biointerfaces, v. 147, Page. 250-257
Abstract
The aim of this study was to assess the effect of D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) on the physicochemical characterization and oral bioavailability of a novel L-sulpiride-loaded quaternary microcapsule (QMC). The effect of carriers on drug solubility was investigated. Among the carriers tested, polyvinyl pyrrolidone (PVP), sodium lauryl sulphate (SLS) and TPGS were selected as polymer, surfactant and absorption enhancer, respectively, due to their high drug solubility. Using the solvent evaporation method, numerous QMCs with different ratios of L-sulpiride, PVP, SLS and TPGS were prepared, and their physicochemical properties, solubility and release were evaluated. In addition, the influence of TPGS concentration on the oral bioavailability of various drug doses was evaluated. All QMCs converted the crystalline drug to the amorphous form and remarkably improved the solubility, release and oral bioavailability of the drug. Furthermore, the TPGS concentration in the QMCs hardly affected the crystallinity, particle size and release, but considerably increased the solubility and oral bioavailability of the drug. In particular, as the dose of administered drug was increased, TPGS provided a greater improvement in oral drug bioavailability. Thus, TPGS played an important role in improving the oral bioavailability of L-sulpiride. Moreover, the QMC with a drug/PVP/SLS/TPGS weight ratio of 5:12:1 :20 with approximately 3.3-fold improved oral bioavailability would be recommended as a commercial pharmaceutical product for oral administration of L-sulpiride.
URI
https://www.sciencedirect.com/science/article/pii/S0927776516305872http://repository.hanyang.ac.kr/handle/20.500.11754/71335
ISSN
0927-7765
DOI
10.1016/j.colsurfb.2016.08.010
Appears in Collections:
RESEARCH INSTITUTE[E](부설연구소) > INSTITUTE OF PHARMACEUTICAL SCIENCE AND TECHNOLOGY(약학기술연구소) > Articles
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