Department of Pharmaceutical Technology, Faculty of Pharmacy, Gazi University, Ankara, Turkey.
Department of Pharmacology, Faculty of Pharmacy, Gazi University, Ankara, Turkey.
J Microencapsul. 2021 Jun;38(4):218-232. doi: 10.1080/02652048.2021.1895344. Epub 2021 Mar 23.
The objective of this study was to develop dermal nanosuspension (NS) based gel formulation of etodolac (ETD).
Etodolac nanosuspension (ETD-NS) was prepared by wet milling method and dispersed in hydroxypropyl methylcellulose (NS-HPMC) or hydroxyethyl cellulose (NS-HEC) gels. Rheologic and mechanical properties were investigated. and permeability studies were performed. Topical anti-inflammatory and analgesic activity were evaluated in regard to carrageenan-induced inflammatory paw oedema and radiant heat tail-flick method, respectively.
The ETD-NS with approximately 190 nm particle size (PS), 0.16 polydispersity index (PDI), and -15 mV zeta potential (ZP) values were obtained. The work of bioadhesion values of NS-HEC and NS-HPMC gels were 0.229 mJ/cm for both gels. Dermal permeation of ETD from NS-HEC gel (7.18%) was found significantly higher than the NS-HPMC gel (4.56%). Enhanced anti-inflammatory and analgesic activity of NS-HEC gels were observed in comparison with micronised ETD.
ETD-NS based gel formulation is promising for topical delivery of ETD.
本研究旨在开发依托考昔（ETD）的透皮纳米混悬剂（NS）凝胶制剂。
采用湿磨法制备依托考昔纳米混悬剂（ETD-NS），并将其分散在羟丙甲纤维素（NS-HPMC）或羟乙基纤维素（NS-HEC）凝胶中。考察了流变学和力学性能，并进行了渗透性研究。通过角叉菜胶诱导的炎性足肿胀和辐射热尾 flick 法分别评价了局部抗炎和镇痛活性。
得到了粒径约为 190nm（PS）、0.16 多分散指数（PDI）和-15mV 动电电势（ZP）的 ETD-NS。NS-HEC 和 NS-HPMC 凝胶的生物粘附功值均为 0.229mJ/cm。从 NS-HEC 凝胶中渗透的 ETD（7.18%）明显高于 NS-HPMC 凝胶（4.56%）。与微米化 ETD 相比，NS-HEC 凝胶表现出增强的抗炎和镇痛活性。
依托考昔 NS 凝胶制剂有望成为依托考昔的局部递药系统。
