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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
최한곤
Keywords
L-sulpiride; Quaternary microcapsule; D-alpha-tocopheryl polyethylene glycol 1000; succinate; Oral absorption; Administered drug dose; IN-VIVO EVALUATION; BIOPHARMACEUTICS CLASSIFICATION-SYSTEM; DRUG-DELIVERY SYSTEM; VITAMIN-E TPGS; SOLID LIPID NANOPARTICLES; INTESTINAL-ABSORPTION; AQUEOUS SOLUBILITY; PARTICLE-SIZE; SOLUBLE DRUG; MODEL-DRUG
Issue Date
2016-08
Publisher
ELSEVIER SCIENCE BV
Citation
COLLOIDS AND SURFACES B-BIOINTERFACES, v. 147, Page. 250-257
Abstract
The aim of this study was to assess the effect of n-alpha-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. (C) 2016 Elsevier B.V. All rights reserved.
URI
https://www.sciencedirect.com/science/article/pii/S0927776516305872http://hdl.handle.net/20.500.11754/68042
ISSN
0927-7765; 1873-4367
DOI
10.1016/j.colsurfb.2016.08.010
Appears in Collections:
COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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