Preparation and <i>in Vitro</i>, <i>in Vivo</i> Characterization of Elastic Liposomes Encapsulating Cyclodextrin-Colchicine Complexes for Topical Delivery of Colchicine

Abstract

In the present study, an attempt was made to develop a cyclodextrin-colchicine complex and to study its eŠect on skin permeation and deposition of colchicine. Colchicine b cyclodextrin (BCD) complex was prepared by freeze-drying method and complex formation was conˆrmed by NMR and in vitro drug release study. Formulation containing cyclodextrin-drug complex showed 6-fold increase in transdermal ‰ux in comparison with drug solution. Skin retention studies were carried out with the objective of determining the depot eŠect of elastic liposomes in skin. The amount of drug deposited was 12.4-fold higher in case of elastic liposomes of colchicine-cyclodextrin complex (567±1.5 mg) than drug solution (46±1.1 mg). The biological evaluation of various vesicular formulations and drug solution was carried out using monosodium urate-induced air pouch model. The results of anti-gout activity in rats showed better and sustained biological eŠects over 24 h measured in terms of exudate volume, reduction in leukocyte count, decrease in in‰ammatory cell accumulation, and collagen deposition with colchicine-BCD elastic liposomal formulation than drug solution. Hence the present study reveals that colchicine-cyclodextrin-elastic liposomes approach possesses good potential to enhance skin accumulation, prolong drug release, and improve the site-speciˆcity of colchicine.

Optimized permeation enhancer for topical delivery of 5-fluorouracil-loaded elastic liposome using Design Expert: part II

“…The accumulated EL (5-FU) has been observed with the slow and sustained release as depot which led to localized effect. A similar finding was observed using cyclodextrin as an enhancer to deliver hydrophilic colchicines in an EL (Singh et al, 2010).…”

Transethosomal gels as carriers for the transdermal delivery of colchicine: statistical optimization, characterization, and ex vivo evaluation

“…Although, EE% was improved (79.5%±1.6%), this was associated with a significant decrease in the flux (26.4±1.2 µg/cm 2 /h) and an increase in the vesicular size (152±14 nm). 12 , 13 Furthermore, no stability studies were reported for both the formulations. Stability study is important, because drug leakage from elastic liposomal vesicles commonly occurs during storage, especially when a hydrophilic drug like colchicine is incorporated.…”

“…Stability study is important, because drug leakage from elastic liposomal vesicles commonly occurs during storage, especially when a hydrophilic drug like colchicine is incorporated. 13 – 15 …”

Elastic liposomes as novel carriers: recent advances in drug delivery

“…13,59 Anti-psoriatic, anti-inflammatory, and antiacne drugs Currently, researchers have reported the management of acne, psoriasis, inflammation, and other cutaneous keratoses using colchicine, methotrexate, and tretinoin for topical delivery (Table 3). [59][60][61][62][63][64] with a desired set of goals. In brief, we have compiled limitations of these potent drugs in Table 3 that could be helpful for pharmaceutical scientists engaged in formulation design.…”

“…59 Table 3 summarizes some of the problems identified with MTX, tretinoin, and colchicines. [59][60][61][62][63][64][65][66] Topically delivered tretinoin was investigated for enhancing skin permeation in dermal delivery using different hydrophilic penetration enhancers such as labrasol, transcutol P, PG, and commercially available Oramix ® NS 10 (OrNS10). All of these surfactants showed increased cutaneous accumulation and transdermal delivery of the tretinoin except PG.…”