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Effect of additives on encapsulation efficiency,stability and bioactivity of entrapped lysozyme from biodegradable polymer particles

机译:添加剂对可生物降解聚合物颗粒包埋的溶菌酶的包封率,稳定性和生物活性的影响

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摘要

Low encapsulation efficiency,incomplete and erratic release profiles are the most common features of controlled released protein delivery systems employing biodegradable polymers.In the present study,lysozyme as a model protein was encapsulated in biodegradable microspheres using solvent evaporation method and the effect of amphiphilic stabilizer,a basic salt and a lyoprotectant on microparticle formulation was evaluated.Incorporation rat serum albumin (RSA) in the internal aqueous phase during emulsion increased the encapsulation efficiency of lysozyme and maintained the bioactivity.Use of NaHCO_3 improved the encapsulation efficiency of lysozyme from 15-94%,but at the cost of reduced in vitro release characteristics.Incorporation of both RSA and NaHCO_3 improved the bioactivity of lysozyme 'and decreased burst release of the protein from the polymer particle,but reduced the encapsulation efficiency from 90-70%.Addition of sucrose in the internal aqueous phase lowered the encapsulation efficiency which was restored by its addition in the external aqueous phase.Maintenance of internal aqueous phase pH close to the iso-electric point of the protein and osmotic balance between the internal aqueous phase and the external aqueous phase during solvent evaporation method helped in better encapsulation of the protein drug.In vitro release of the lysozyme correlated with the effect of different excipients on entrapment in polymer matrix.Entrapment efficiency as high as 76%,low burst effect and high bioactivity of the entrapped lysozyme was observed from the polymer particles.Use of RSA,sucrose and NaHCO_3 helped in a co-operative way towards the formulation of particles entrapping bioactive lysozyme.
机译:低包封率,不完全和不规则的释放曲线是采用可生物降解的聚合物的控释蛋白递送系统的最常见特征。在乳剂中将大鼠血清白蛋白(RSA)掺入内部水相提高了溶菌酶的包封效率并保持了生物活性。NaHCO_3的使用从15-94提高了溶菌酶的包封效率。 %,但以降低体外释放特性为代价。RSA和NaHCO_3的结合改善了溶菌酶的生物活性,并减少了蛋白质从聚合物颗粒中的突释,但将包封效率从90-70%降低了。内部水相中的蔗糖降低了胶囊化n通过在外部水相中添加而恢复的效率。内部水相pH的维持接近蛋白质的等电点,并且在溶剂蒸发法中内部水相与外部水相之间的渗透平衡有助于更好地溶菌酶的体外释放与不同赋形剂对聚合物基质中包封的影响有关。从聚合物颗粒中观察到包埋的溶菌酶的包埋率高达76%,低突释效果和高生物活性。 RSA,蔗糖和NaHCO_3的使用以合作方式有助于形成包埋生物活性溶菌酶的颗粒。

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