Alkyl polyglucoside vs. ethoxylated surfactant-based microemulsions as vehicles for two poorly water-soluble drugs: physicochemical characterization and in vivo skin performance

被引:12
作者
Pajic, Natasa Z. Bubic [1 ]
Todosijevic, Marija N. [2 ]
Vuleta, Gordana M. [2 ]
Cekic, Nebojsa D. [3 ,4 ]
Dobricic, Vladimir D. [5 ]
Vucen, Sonja R. [6 ]
Calija, Bojan R. [2 ]
Lukic, Milica Z. [2 ]
Ilic, Tanja M. [2 ]
Savic, Snezana D. [2 ]
机构
[1] Univ Banja Luka, Fac Med, Dept Pharmaceut Technol & Cosmetol, Fac Med, Banja Luka 78000, Bosnia & Herceg
[2] Univ Belgrade, Fac Pharm, Dept Pharmaceut Technol & Cosmetol, Belgrade 11221, Serbia
[3] Univ Nis, Fac Technol, Leskovac 16000, Serbia
[4] DCP Hemigal, Leskovac 16000, Serbia
[5] Univ Belgrade, Fac Pharm, Dept Pharmaceut Chem, Belgrade, Serbia
[6] Univ Coll Cork, Sch Pharm, Cork, Ireland
关键词
alkyl polyglucoside; ethoxylated surfactant; adapalene; sertaconazole nitrate; biocompatible microemulsion; in vivo skin irritation; PHASE-BEHAVIOR; DELIVERY; FORMULATION; PARAMETERS; TRANSPORT; SYSTEMS; ACID;
D O I
10.1515/acph-2017-0036
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Two types of biocompatible surfactants were evaluated for their capability to formulate skin-friendly/non-irritant microemulsions as vehicles for two poorly water-soluble model drugs differing in properties and concentrations: alkyl polyglucosides (decyl glucoside and caprylyl/capryl glucoside) and ethoxylated surfactants (glycereth-7-caprylate/caprate and polysorbate 80). Phase behavior, structural inversion and microemulsion solubilization potential for sertaconazole nitrate and adapalene were found to be highly dependent on the surfactants structure and HLB value. Performed characterization (polarized light microscopy, pH, electrical conductivity, rheological, FTIR and DSC measurements) indicated a formulation containing glycereth-7-caprylate/caprate as suitable for incorporation of both drugs, whereas alkyl polyglucoside-based systems did not exhibit satisfying solubilization capacity for sertaconazole nitrate. Further, monitored parameters were strongly affected by sertaconazole nitrate incorporation, while they remained almost unchanged in adapalene-loaded vehicles. In addition, results of the in vivo skin performance study supported acceptable tolerability for all investigated formulations, suggesting selected microemulsions as promising carriers worth exploring further for effective skin delivery of model drugs.
引用
收藏
页码:415 / 439
页数:25
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