Laboratory of Pharmaceutical Technology, Department of Pharmaceutical Sciences, School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Ribeirão Preto, São Paulo, Brazil.
J Microencapsul. 2009 May;26(3):243-50. doi: 10.1080/02652040802305105.
Chitosan treated alginate microparticles were prepared with the purpose of incorporating all-trans retinoic acid (ATRA) using an inexpensive, simple and fast method, enhancing dermal localization and sustaining the release of ATRA into the skin. Microparticles characterization, drug-polymer interaction, release profile and in vitro skin retention were investigated. Microparticles presented spherical shape and drug loading capacity of 47%. The drug content of these microparticles was affected by ATRA concentration and by the solvent used and it was more weakly affected by chitosan concentration. The release of ATRA was also affected by chitosan concentration. Microparticles prepared with 0.4% chitosan (w/w) resulted in drug release with a more sustained profile. The results of in vitro retention studies showed that chitosan treated alginate microparticles decreased the drug retention in the stratum corneum (SC), where occur the skin irritation, but maintained the ATRA concentration in the deeper skin layers, where occur the pathologies treated with ATRA. Then, the microparticles developed in this work can be a good candidate to improve the topical therapy with retinoid.
壳聚糖处理的海藻酸钠微球的制备目的是使用一种廉价、简单和快速的方法将全反式视黄酸(ATRA)包埋在内,增强其在皮肤中的定位和持续释放 ATRA。对微球的特性、药物-聚合物相互作用、释放曲线和体外皮肤保留进行了研究。微球呈现球形,载药量为 47%。这些微球的药物含量受 ATRA 浓度、溶剂的影响,受壳聚糖浓度的影响较弱。壳聚糖浓度也影响 ATRA 的释放。用 0.4%(w/w)壳聚糖制备的微球导致药物释放呈现更持久的曲线。体外保留研究的结果表明,壳聚糖处理的海藻酸钠微球减少了药物在引起皮肤刺激的角质层(SC)中的保留,但维持了在更深层皮肤中发生 ATRA 治疗的病变处的 ATRA 浓度。因此,本文开发的微球可以成为改善维甲酸局部治疗的良好候选物。