Proultraflexible lipid vesicles for effective transdermal delivery of levonorgestrel: Development, characterization, and performance evaluation

Abstract

The present investigation aimed at formulation, performance evaluation, and stability studies of new vesicular drug carrier system protransfersomes for transdermal delivery of the contraceptive agent, levonorgestrel. Protransfersome gel (PTG) formulations of levonorgestrel were prepared and characterized for vesicle shape, size, entrapment efficiency, turbidity, and drug permeation across rat skin and were evaluated for their stability. The system was evaluated in vivo for biological assay of progestational activity including endometrial assay, inhibition of the formation of corpora lutea, and weight gain of uterus. The effects of different formulation variables (type of alcohol, type and concentration of surfactant) on transdermal permeability profile were assessed. The optimized PTG formulation showed enhanced in vitro skin permeation flux of 15.82 ± 0.37 μg/cm 2 /hr as compared to 0.032 ± 0.01 μg/cm 2 /hr for plain drug solution. PTG also showed good stability and after 2 months of storage there was no change in liquid crystalline nature, drug content, and other characteristic parameters. The peak plasma concentration of levonorgestrel (0.139 ± 0.05 μg/mL) was achieved within 4 hours and maintained until 48 hours by a single topical application of optimized PTG formulation. In vivo performance of the PTG formulation showed increase in the therapeutic efficacy of drug. Results indicated that the optimized protransfersomal formulation of levonorgestrel had better skin permeation potential, sustained release characteristic, and better stability than proliposomal formulation.

Mannan-coated gelatin nanoparticles for sustained and targeted delivery of didanosine: In vitro and in vivo evaluation

“…Results of the cellular uptake study were well correlated with those reported by Cui et al The better cellular uptake of the nanoparticle formulation was further confirmed by fluorescence microscopy. Marker selected for the present study was 6-CF because it has a similar hydrophilic nature to didanosine (17). Fluorescence photomicrographs (not shown) reveal better qualitative uptake and localization of fluorescence marker loaded plain nanoparticles and mannan-coated nanoparticles in brain, spleen and lymph nodes as compared to its solution.…”

“…Third and fourth groups received subcutaneous injection of 1.0 mL of the optimized plain nanoparticle formulation (N-C3) and mannan--coated nanoparticle formulation (N-C3-M) loaded with 6-CF (0.16%, m/V), respectively, in the dorsal part of hind paw. Rats were sacrificed after 12 h of administration and selected tissues (spleen, liver and lymph nodes) were excised, cut into small pieces and fixed using the conventional method (17). Paraffin blocks were made, 5-mm thick sections were cut using a microtome (Erma Optical Works, Japan) and examined under a fluorescence microscope (Leica, DMRBE, Germany).…”

Experimental design and optimization of raloxifene hydrochloride loaded nanotransfersomes for transdermal application

“…The vesicular formulations were mixed with deionized water, in a ratio of 0.4 mL in 10 mL of deionized water, before taking the measurement using the particle size analyser in a multimodal mode. 18,23 The polydispersity index (PDI) was used as a measure of size distribution, which was measured in triplicate. A PDI value of less than 0.1 was considered as a homogeneous distribution of vesicles, whereas a PDI value of greater than 0.3 was of higher heterogeneity.…”

Reduction in cisplatin genotoxicity (micronucleus formation) in non target cells of mice by protransfersome gel formulation used for management of cutaneous squamous cell carcinoma

“…liposomes, miosomes, etc. (5,6). Squamous cell carcinoma is a malignant tumor of squamous epithelium.…”