Nawaz Asif, Latif Muhammad Shahid, Shah Muhammad Khurshid Alam, Elsayed Tarek M, Ahmad Saeed, Khan Hamid Ali
Advanced Drug Delivery Lab, Gomal Centre of Pharmaceutical Sciences, Faculty of Pharmacy, Gomal University, Dera Ismail Khan 29050, Pakistan.
Pharmaceutical Technology Department, Faculty of Pharmacy, Sultan Zainal Abidin University, Besut Kampus, Besut 22200, Malaysia.
Gels. 2023 Mar 6;9(3):201. doi: 10.3390/gels9030201.
Curcumin, a natural phenolic compound, exhibits poor absorption and extensive first pass metabolism after oral administration. In the present study, curcumin-chitosan nanoparticles (cur-cs-np) were prepared and incorporated into ethyl cellulose patches for the management of inflammation via skin delivery. Ionic gelation method was used for the preparation of nanoparticles. The prepared nanoparticles were evaluated for size, zetapotential, surface morphology, drug content, and % encapsulation efficiency. The nanoparticles were then incorporated into ethyl cellulose-based patches using solvent evaporation technique. ATR-FTIR was used to study/assess incompatibility between drug and excipients. The prepared patches were evaluated physiochemically. The in vitro release, ex vivo permeation, and skin drug retention studies were carried out using Franz diffusion cells and rat skin as permeable membrane. The prepared nanoparticles were spherical, with particle size in the range of 203-229 nm, zetapotential 25-36 mV, and PDI 0.27-0.29 Mw/Mn. The drug content and %EE were 53% and 59%. Nanoparticles incorporated patches are smooth, flexible, and homogenous. The in vitro release and ex vivo permeation of curcumin from nanoparticles were higher than the patches, whereas the skin retention of curcumin was significantly higher in case of patches. The developed patches deliver cur-cs-np into the skin, where nanoparticles interact with skin negative charges and hence result in higher and prolonged retention in the skin. The higher concentration of drug in the skin helps in better management of inflammation. This was shown by anti-inflammatory activity. The inflammation (volume of paw) was significantly reduced when using patches as compared to nanoparticles. It was concluded that the incorporation of cur-cs-np into ethyl cellulose-based patches results in controlled release and hence enhanced anti-inflammatory activity.
姜黄素是一种天然酚类化合物,口服后吸收较差且首过代谢广泛。在本研究中,制备了姜黄素-壳聚糖纳米粒(cur-cs-np),并将其掺入乙基纤维素贴剂中,通过皮肤给药来治疗炎症。采用离子凝胶法制备纳米粒。对制备的纳米粒进行粒径、zeta电位、表面形态、药物含量和包封率的评估。然后使用溶剂蒸发技术将纳米粒掺入乙基纤维素基贴剂中。采用衰减全反射傅里叶变换红外光谱(ATR-FTIR)研究/评估药物与辅料之间的不相容性。对制备的贴剂进行理化性质评估。使用Franz扩散池和大鼠皮肤作为渗透膜进行体外释放、离体渗透和皮肤药物滞留研究。制备的纳米粒呈球形,粒径范围为203-229nm,zeta电位为25-36mV,多分散指数(PDI)为0.27-0.29Mw/Mn。药物含量和包封率分别为53%和59%。掺入纳米粒的贴剂光滑、柔韧且均匀。姜黄素从纳米粒中的体外释放和离体渗透高于贴剂,而姜黄素在贴剂中的皮肤滞留量显著更高。所开发的贴剂将cur-cs-np递送至皮肤,纳米粒与皮肤负电荷相互作用,因此在皮肤中的滞留量更高且持续时间更长。皮肤中较高的药物浓度有助于更好地控制炎症。这通过抗炎活性得以证明。与纳米粒相比,使用贴剂时炎症(爪体积)显著减轻。得出的结论是,将cur-cs-np掺入乙基纤维素基贴剂可实现控释,从而增强抗炎活性。