Ketoprofen-loaded polymer carriers in bigel formulation: an approach to enhancing drug photostability in topical application forms

被引：36

作者：

Andonova, Velichka ^{[1
,2
]}

Peneva, Petya ^{[1
,2
]}

Georgiev, George S. ^{[3
]}

Toncheva, Vencislava T. ^{[3
]}

Apostolova, Elisaveta ^{[4
]}

Peychev, Zhivko ^{[5
]}

Dimitrova, Stela ^{[6
]}

Katsarova, Mariana ^{[6
]}

Petrova, Nadia ^{[7
]}

Kassarova, Margarita ^{[1
,2
]}

机构：

[1] Med Univ Plovdiv, Fac Pharm, Dept Pharmaceut Sci, 15A Vassil Aprilov Blvd, Plovdiv 4002, Bulgaria

[2] Technol Ctr Emergency Med TCEMED, Plovdiv, Bulgaria

[3] Sofia Univ St Kliment Ohridski, Fac Chem & Pharm, Sofia, Bulgaria

[4] Med Univ Plovdiv, Fac Pharm, Dept Pharmacol & Drug Toxicol, Plovdiv, Bulgaria

[5] Med Univ Plovdiv, Fac Publ Hlth, Dept Med Informat Biostat & E Learning, Plovdiv, Bulgaria

[6] Med Univ Plovdiv, Fac Pharm, Dept Chem & Biochem, Plovdiv, Bulgaria

[7] Bulgarian Acad Sci, Inst Mineral & Crystallog, Sofia, Bulgaria

来源：

INTERNATIONAL JOURNAL OF NANOMEDICINE | 2017年 / 12卷

关键词：

antihyperalgesic effect; antinociceptive activity; biphasic systems; carrageenan-induced edema; emulsifier-free radical polymerization; NANOSTRUCTURED LIPID CARRIERS; IN-VITRO; DELIVERY-SYSTEMS; OIL; VIVO; GEL; SURFACTANTS; DISSOLUTION; CONSISTENCY; PERMEATION;

D O I：

10.2147/IJN.S140934

中图分类号：

TB3 [工程材料学];

学科分类号：

0805 ; 080502 ;

摘要：

The purpose of the study was to investigate the stability and biopharmaceutical characteristics of ketoprofen, loaded in polymeric carriers, which were included into a bigel in a semisolid dosage form. The polymer carriers with in situ-included ketoprofen were obtained by emulsifier-free emulsion polymerization of the monomers in aqueous medium or a solution of the polymers used. The morphological characteristics of the carriers, the in vitro release and the photochemical stability of ketoprofen were evaluated. The model with optimal characteristics was included in a bigel formulation. The bigel was characterized in terms of pH, rheological behavior, spreadability, and in vitro drug release. Acute skin toxicity, antinociceptive activity, anti-inflammatory activity, and antihyperalgesic effects of the prepared bigel with ketoprofen-loaded polymer carrier were evaluated. The carriers of ketoprofen were characterized by a high yield and drug loading. The particle size distribution varied widely according to the polymer used, and a sustained release was provided for up to 6 hours. The polymer mixture poly(vinyl acetate) and hydroxypropyl cellulose as a drug carrier, alone or included in the bigel composition, improved the photostability of the drug compared with unprotected ketoprofen. The bigel with ketoprofen-loaded particles provided sustained release of the drug and had optimal rheological parameters. In vivo experiments on the bigel showed no skin inflammation or irritation. Four hours after its application, a well-defined analgesic, anti-inflammatory, and antihyperalgesic effect was registered. The polymer mixture of poly(vinyl acetate) and hydroxypropyl cellulose as a carrier of ketoprofen and the bigel in which it was included provided an enhanced photostability and sustained drug release.

引用

页码：6221 / 6238

页数：18

共 53 条

[1] Preparation, characterization and biocompatibility studies of thermoresponsive eyedrops based on the combination of nanostructured lipid carriers (NLC) and the polymer Pluronic F-127 for controlled delivery of ibuprofen [J].