Elastic liposomes bearing meloxicam-beta-cyclodextrin for transdermal delivery.
The ultra-flexible lipid vesicles, the elastic liposomes bearing meloxicam-beta-cyclodextrin complex were prepared for its topical administration with the aim of simultaneously exploiting the favorable properties of both the carriers. The prepared meloxicam-beta-cyclodextrin complex was evaluated using DSC, XRD and FT-IR, which indicates the formation of inclusion complex in a molar ratio of 1:2 of meloxicam and beta-cyclodextrin (beta-CD). The elastic liposomes were prepared by conventional rotary evaporation method and characterized for various parameters such as vesicle shape and surface morphology, size and size distribution, entrapment efficiency, elasticity, stability and in-vitro release pattern. Permeability studies of meloxicam and meloxicam-beta-cyclodextrin complex, as such or incorporated in elastic liposomes performed both across artificial membranes and rat skin highlighted a favorable effect of cyclodextrin on drug permeation rate, due to its solubilizing action. Moreover skin-permeation enhancer property of elastic liposomes has been evidenced. Skin permeation potential of the developed formulation was assessed using confocal laser scanning microscopy (CLSM), which revealed an enhanced permeation of the formulation to the deeper layers of the skin (up to 160 microm) following channel like pathways. Skin permeation profile of elastic liposomal formulation bearing meloxicam-beta-cyclodextrin complex was observed and the investigations revealed an enhanced transdermal flux (12.48+/-0.9 microg/cm(2)/h) and decreased lag time (0.7 h) for meloxicam. The obtained flux was nearly 1.4 and 9.1 times higher than elastic liposomal formulation bearing meloxicam and plain drug solution, respectively (P<0.005). The results indicate that the elastic liposomes may be promising vehicles for the transdermal delivery of meloxicam.
Jain
Sanjay K
SK
Pharmaceutics Research Projects Laboratory, Department of Pharmaceutical Sciences, Dr. Hari Singh Gour Vishwavidyalaya, Sagar [M. P.] 470003, India. drskjainsagar@rediffmail.com
Gupta
Yashwant
Y
Jain
Anekant
A
Amin
Sadia
S
D000279:Administration, Cutaneous; D000818:Animals; D002152:Calorimetry, Differential Scanning; D052246:Cyclooxygenase 2 Inhibitors / Q000008:administration & dosage* / Q000737:chemistry; D004337:Drug Carriers; D004339:Drug Compounding; D004355:Drug Stability; D004548:Elasticity; D008081:Liposomes; D000077239:Meloxicam; D017551:Microdialysis; D010316:Particle Size; D051381:Rats; D054772:Rats, Hairless; D017207:Rats, Sprague-Dawley; D012869:Skin Absorption; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013843:Thiazines / Q000008:administration & dosage* / Q000737:chemistry; D013844:Thiazoles / Q000008:administration & dosage* / Q000737:chemistry; D014961:X-Ray Diffraction; D047392:beta-Cyclodextrins / Q000008:administration & dosage* / Q000737:chemistry
D052246:Cyclooxygenase 2 Inhibitors; D004337:Drug Carriers; D008081:Liposomes; D013843:Thiazines; D013844:Thiazoles; D047392:beta-Cyclodextrins; C031215:betadex; D000077239:Meloxicam