Procedure for Preparation of Lipid Vesicles (Liposomes) Using the Coacervation (Phase Separation) Technique

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.

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“…Transfersomes formed from PTG formulation were also characterized for vesicle size and drug content. 20 …”

Section: Stability Studiesmentioning

confidence: 99%

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

et al. 2005

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“…Since phospholipids are nontoxic and biodegradable, they are in many respects regarded as ideal biological surfactants for use in food and pharmaceutical industries. Phospholipid aggregates in organic solvents have been studied by several groups, and various structures have been reported (16,17). Phospholipid-based reversed micellar systems have also been studied (12,13,18,19).…”

Section: Introductionmentioning

confidence: 99%

Formation and Characterization of Reversed Micelles Composed of Phospholipids and Fatty Acids

Sugiura

Ichikawa

Sano

et al. 2001

Journal of Colloid and Interface Science

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“…The larger size with ethanol is due to the slower phase separation because of its greater solubility in water. The smaller size with isopropanol may be due to its branched chain 13,15 . The transdermal dose of CXB is lower than the oral dose since Transdermal dose = Oral dose (mg/day) × Bioavailability (%) 16 .…”

Section: Resultsmentioning

confidence: 99%

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Alam¹,

Baboota²,

Kohli³

et al. 2010

ScienceAsia

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A low dose proniosomal gel containing celecoxib was developed for the treatment of osteoarthritis. All the prepared formulations were subjected to physicochemical evaluations and anti-inflammatory studies. The entrapment was > 90%. The vesicle shape was determined with the help of transmission electron microscopy. The vesicle size, sizedistribution, and polydispersity studies were performed using photon correlation spectroscopy. Anti-inflammatory studies were performed using the rat hind-paw oedema induced by carrageenan (1% w/v). The selected proniosomal gel (N1LE3) produced 100% inhibition of paw oedema in rats up to 8 h after carrageenan injection. It produced 95% and 92% inhibition after 12 h and 24 h, respectively. These results indicate that proniosomes are a promising carrier for the transdermal delivery of celecoxib. Thus celecoxib can be formulated into a low dose proniosomal gel that can save the recipient from the adverse effects of large doses.

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Procedure for Preparation of Lipid Vesicles (Liposomes) Using the Coacervation (Phase Separation) Technique

Cited by 63 publications

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

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

Formation and Characterization of Reversed Micelles Composed of Phospholipids and Fatty Acids

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