Drug-in-mucoadhesive type film for ocular anti-inflammatory potential of amlodipine: Effect of sulphobutyl-ether-beta-cyclodextrin on permeation and molecular docking characterization

被引：43

作者：

Nanda, Ashirbad ^{[1
]}

Sahoo, Rudra Narayan ^{[1
]}

Pramanik, Arunima ^{[1
]}

Mohapatra, Rajaram ^{[1
]}

Pradhan, Sukanta Kumar ^{[2
]}

Thirumurugan, Arun ^{[3
]}

Das, Debajyoti ^{[1
]}

Mallick, Subrata ^{[1
]}

机构：

[1] Siksha O Anusandhan, Sch Pharmaceut Sci, Dept Pharmaceut, Bhubaneswar, Odisha, India

[2] Orissa Univ Agr & Technol, Dept Bioinfonnat, Bhubaneswar, Odisha, India

[3] Inst Phys, Bhubaneswar, Odisha, India

来源：

COLLOIDS AND SURFACES B-BIOINTERFACES | 2018年 / 172卷

关键词：

Drug-in-mucoadhesive film; Sulphobutyl-ether-beta-cyclodextrin; Amlodipine; Binary and ternary docking; Ocular permeation; Anti-inflammatory activity; INTRAOCULAR-PRESSURE; INCLUSION COMPLEXES; DELIVERY; VITRO; TEMPERATURE; FORMULATION; SOLUBILITY; DICLOFENAC; IBUPROFEN; RELEASE;

D O I：

10.1016/j.colsurfb.2018.09.011

中图分类号：

Q6 [生物物理学];

学科分类号：

071011 ;

摘要：

Mucoadhesive type ocular film has been prepared for studying the anti-inflammatory potential of amlodipine (AML) on carrageenan-induced rabbit model and the effect of sulphobutyl-ether-beta-cyclodextrin on corneal permeation was tested. Hydroxypropyl methylcellulose (HPMC) ocular film was prepared after complexation of amlodipine with beta-cyclodextrin, (BCD), hydroxypropyl beta-cyclodextrin (HPCD), and sulfobutylether beta-cyclodextrin (SBCD). The film without cyclodextrin showed a maximum swelling, and erosion to the highest extent. Both drug release and permeation were highly diffusion controlled and highest improvement was observed with SBCD due to increased dissolution, compared to other formulations with or without cyclodextrin. Highest binding energy and highest extent of amorphization were noticed in the SBCD film formulation. Improved amlodipine release in-vitro and ocular permeation were found by the HPMC film formulation after complexation of the drug with cyclodextrin wherein SBCD exhibited both to the highest extent. Binary and ternary systems molecular docking studies confirmed the lowest energy of binding between amlodipine and BCD compared to HBCD and SBCD. Signs of acute inflammation were mitigated within 2 h of film application in the cul-de-sac. Presence of sulphobutyl-ether beta-cyclodextrin in the amlodipine-HPMC film can improve ocular permeation significantly and could be utilized as mucoadhesive type formulation for anti-inflammatory activity.

引用

页码：555 / 564

页数：10