Zafar Nadiah, Robin Sophie, Viennet Céline, Humbert Philippe, Valour Jean Pierre, Agusti Geraldine, Fessi Hatem, Elaissari Abdelhamid
Univ Lyon, University Claude Bernard Lyon-1, CNRS, LAGEP-UMR 5007, F-69622 Lyon, France.
Laboratory of Engineering and Cutaneous Biology, UMR 1098, Medicine and Pharmaceutical University, 19 rue Ambroise Paré, 25000, Besançon, France.
Int J Pharm. 2017 Oct 30;532(1):623-634. doi: 10.1016/j.ijpharm.2017.08.122. Epub 2017 Sep 1.
This unique work is targeted to achieve three main goals: i) to enhance the aqueous solubility of three specifically selected hydrophobic active agents, ii) to prepare such polymeric biodegradable microparticles which can encapsulate actives-cyclodextrin complexes and iii) to functionalize a polyamide base textile with active loaded microparticles and active-cyclodextrin loaded microparticles. To achieve this objective, biodegradable cationic microparticles were prepared via double emulsion solvent evaporation process and were loaded with hydroxypropyl-beta-cyclodextrin based complexes of Indomethacin, α-tocopheroland Lauryl Isoquinolinium Bromide during the formulation process. Inclusion complex based particles were evaluated for their morphology, size distribution, zeta potential, skin penetration aptitude and adsorption onto a selected textile. It was observed that active-cyclodextrin complex encapsulation do not affect the morphology, size and zeta potential of the microparticles as well as adsorption of the microparticles onto textile remains unaltered. However such active-cyclodextrin complex encapsulated particles provided the enhancement in the aqueous solubility of hydrophobic agents and also provided prolonged release formulations.
i)提高三种特定选择的疏水性活性剂的水溶性;ii)制备能够包封活性剂 - 环糊精复合物的可生物降解聚合物微粒;iii)用负载有活性剂的微粒和负载有活性剂 - 环糊精的微粒对聚酰胺基纺织品进行功能化处理。为实现这一目标,通过双乳液溶剂蒸发法制备了可生物降解的阳离子微粒,并在配方过程中用吲哚美辛、α - 生育酚和月桂基异喹啉溴化物的羟丙基 - β - 环糊精基复合物对其进行负载。对基于包合物的微粒进行了形态、尺寸分布、zeta电位、皮肤渗透能力以及在选定纺织品上的吸附等方面的评估。观察到活性剂 - 环糊精复合物的包封不影响微粒的形态、尺寸和zeta电位,并且微粒在纺织品上的吸附也保持不变。然而,这种包封有活性剂 - 环糊精复合物的微粒提高了疏水性活性剂的水溶性,并提供了缓释制剂。