title: Development of a novel l-sulpiride-loaded quaternary microcapsule: Effect of TPGS as an absorption enhancer on physicochemical characterization and oral bioavailability.
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.
authors: College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 426-791, South Korea, South Korea.
authors: Dong Shik
authors: DS
authors: Kim
authors: College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 426-791, South Korea, South Korea.
authors: Dong Wuk
authors: DW
authors: Kim
authors: College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 426-791, South Korea, South Korea.
authors: Kyeong Soo
authors: KS
authors: Kim
authors: College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 426-791, South Korea, South Korea.
authors: Jong Seo
authors: JS
authors: Choi
authors: College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyongsan 712-749, South Korea, South Korea.
authors: Youn Gee
authors: YG
authors: Seo
authors: School of Pharmacy, Sungkyunkwan University, 300 Cheoncheon-dong, Jangan-gu, Suwon 440-746, South Korea, South Korea.
authors: Yu Seok
authors: YS
authors: Youn
authors: College of Pharmacy, Chung-Ang University, 221 Heuksuk-dong Dongjak-gu, Seoul 156-756, South Korea, South Korea.
authors: Kyung Taek
authors: KT
authors: Oh
authors: College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyongsan 712-749, South Korea, South Korea.
authors: Chul Soon
authors: CS
authors: Yong
authors: College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyongsan 712-749, South Korea, South Korea. Electronic address: jongohkim@yu.ac.kr.
authors: Jong Oh
authors: JO
authors: Kim
authors: College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 426-791, South Korea, South Korea. Electronic address: sklover777@gmail.com.
authors: Sung Giu
authors: SG
authors: Jin
authors: College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 426-791, South Korea, South Korea. Electronic address: hangon@hanyang.ac.kr.
authors: Han-Gon
authors: HG
authors: Choi
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002214:Capsules / Q000737:chemistry*; D004337:Drug Carriers / Q000008:administration & dosage* / Q000737:chemistry; D016503:Drug Delivery Systems; D008297:Male; D011108:Polymers / Q000008:administration & dosage / Q000737:chemistry; D011205:Povidone / Q000008:administration & dosage / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D012967:Sodium Dodecyl Sulfate / Q000008:administration & dosage / Q000737:chemistry; D012995:Solubility; D013469:Sulpiride / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D013501:Surface-Active Agents; D014018:Tissue Distribution; D014810:Vitamin E / Q000008:administration & dosage* / Q000737:chemistry
chemical_list: D002214:Capsules; D004337:Drug Carriers; D011108:Polymers; D013501:Surface-Active Agents; D014810:Vitamin E; D012967:Sodium Dodecyl Sulfate; D013469:Sulpiride; D011205:Povidone; C014225:tocophersolan
keywords: Administered drug dose; Oral absorption; Quaternary microcapsule; d-α-tocopheryl polyethylene glycol 1000 succinate; l-sulpiride