Patil Pradeep, Paradkar Anant
Department of Pharmaceutics, Bharati Vidyapeeth Deemed University, Poona College of Pharmacy, Erandwane, 411 038, Pune, Maharashtra State, India.
AAPS PharmSciTech. 2006 Mar;7(1):E199-E205. doi: 10.1208/pt070128. Epub 2017 Mar 8.
The aim of this study was to formulate a self-emulsifying system (SES) containing a lipophilic drug, loratadine, and to explore the potential of preformed porous polystyrene beads (PPB) to act as carriers for such SES. Isotropic SES was formulated, which comprised Captex 200 (63% wt/wt), Cremophore EL (16% wt/wt), Capmul MCM (16% wt/wt), and loratadine (5% wt/wt). SES was evaluated for droplet size, drug content, and in vitro drug release. SES was loaded into preformed and characterized PPB using solvent evaporation method. SES-loaded PPB were evaluated using scanning electron microscopy (SEM) for density, specific surface area (S), loading efficiency, drug content, and in vitro drug release. After SES loading, specific surface area reduced drastically, indicating filling of PPB micropores with SES. Loading efficiency was least for small size (SS) and comparable for medium size (MS) and large size (LS) PPB fractions. In vitro drug release was rapid in case of SS beads due to the presence of SES near to surface. LS fraction showed inadequate drug release owing to presence of deeper micropores that resisted outward diffusion of entrapped SES. Leaching of SES from micropores was the rate-limiting step for drug release. Geometrical features such as bead size and pore architecture of PPB were found to govern the loading efficiency and in vitro drug release from SES-loaded PPB.
本研究的目的是制备一种包含亲脂性药物氯雷他定的自乳化系统(SES),并探索预制多孔聚苯乙烯珠(PPB)作为此类SES载体的潜力。制备了各向同性的SES,其由Captex 200(63%重量/重量)、聚氧乙烯蓖麻油EL(16%重量/重量)、Capmul MCM(16%重量/重量)和氯雷他定(5%重量/重量)组成。对SES的液滴大小、药物含量和体外药物释放进行了评估。使用溶剂蒸发法将SES载入预制并表征的PPB中。使用扫描电子显微镜(SEM)对载入SES的PPB的密度、比表面积(S)、载入效率、药物含量和体外药物释放进行了评估。载入SES后,比表面积急剧降低,表明PPB微孔被SES填充。小尺寸(SS)PPB的载入效率最低,中尺寸(MS)和大尺寸(LS)PPB级分的载入效率相当。由于表面附近存在SES,SS珠的体外药物释放很快。由于存在较深的微孔,阻碍了包封的SES向外扩散,LS级分的药物释放不足。SES从微孔中的浸出是药物释放的限速步骤。发现PPB的珠尺寸和孔结构等几何特征决定了载入SES的PPB的载入效率和体外药物释放。