Lamivudine Liposomes for Transdermal Delivery - Formulation, Characterization, Stability and In vitro Evaluation
DOI:
https://doi.org/10.37285/ijpsn.2008.1.4.1Abstract
: Lamivudine, an antiretroviral is commonly used in the treatment of HIV infections. Upon oral administration, it exhibits dose dependent toxic effects such as hepatotoxicity, hyperglycemia, hyperlipidemia, lactic acidosis, lipodystropy, osteonecrosis. These side effects often require dosage reduction or even cessation of treatment. Thus, the problems associated with oral administration led us to explore the possibilities of designing novel drug delivery system for lamivudine with an alternative route of administration. In the present study, liposomes of lamivudine were prepared by thin film hydration and their potential for transdermal drug delivery has been evaluated in vitro. In the preparation of liposomes, process and formulation parameters were standardized. Liposomes were evaluated for their physicochemical properties such as appearance, particle size, particle size distribution and drug entrapment. Liposomes stored at lower temperature conditions, retained 96 % of the incorporated drug. Residual solvents in the formulation were determined by Gas Chromatography and content of lipids was estimated by Stewart assay. Permeation studies of liposomal formulations were carried out across rat abdominal skin using modified Franz diffusion cells. The lamivudine liposomes with good stability and appreciably controlled skin permeation with minimal retention of drug in the skin were successfully prepared
Downloads
Metrics
Keywords:
Lamivudine, antiretroviral, liposomes,, transdermal, stability
Downloads
Published
How to Cite
Issue
Section
References
Anbazhagan S, Indumathy N, Shanmugapandiyan P, and Sridhar KS. Simultaneous quantification of stavudine,lamivudine and nevirapine by UV spectroscopy, reverse phase HPLC and HPTLC in tablets. J. Pharm. and Biomed. Ana. 39: 801-804 (2005).
Bhatia A, Kumar R, and Katare OP. Tamoxifen in topical liposomes: development, characterization and in-vitro evaluation. J. Pharm. Pharmaceut. Sci. 7(2): 252-259 (2004).
Betagiri GV, Jenkins SA and Ravis WR. Drug delivery using antibody-liposome conjugates. Drug. Dev. Ind. Pharm. 19(16): 2109-2116. (1993).
Betty JD, Herfindal TE. Text Book of Therapeutics Drug and Disease Management, 7th Edn., Lippincott Williams and Wilkins, USA,1555, (2000).Eds.,
Bouwstra JA, and Honeywell-Nguyen, PL. Skin structure and mode of action of vesicles. Adv. Drug. Del. Revs. 54(1): S 41-S 55 (2002).
Desormeaux, A, and Bergeron MG. Liposomes as drug delivery system: a strategic approach for the treatment of HIV infection. J. Drug. Target. 6(1): 1-15 (1998).
Dubey V, Mishra D, Asthana A and Jain NK. Transdermal delivery of a pineal hormone: Melatonin via elastic liposomes. Biomaterials. 27: 3491–3496 (2006).
Elsayed MMA, Abdallah OY, Naggar VF, and Khalafallah NM. Deformable liposomes and ethosomes: Mechanism of enhanced skin delivery. Int. J. Pharm. 322: 60–66 (2006).
El-Samaligy MS, Afifi N N and Mahmoud E A. Increasing bioavailability of silymarin using a buccal liposomal delivery system: Preparation and experimental design investigation. Int. J. Pharm. 308: 140-148 (2006).
Gøril Eide Flaten GE, Bunjes H, Luthman K, and Brandl M. Drug permeability across a phospholipids vesicle-based barrier 2.Characterization of barrier structure, storage stability and stability towards pH changes. Eur. J. Pharma. Sc.; 28: 336 –343 (2006).
Greenberg M, Cammack N, Salgo M, and Smiley L. HIV fusion and its inhibition in antiretroviral therapy. Rev. Med. Virol. 14(5): 321-337 (2004).
Joshi UJ, Indu TB, and Patil P. Aids and Approaches to Anti HIV Chemotherapy. Ind Drugs. 37(4): 160-176 (2000).
Karali TT, Kirchhoff CF, and Stanley CP. Enhancement of transdermal transport of azidothymidine (AZT) with novel terpene and terpene-like enhancers: in vivo-in vitro correlations. J. Cont. Rel. 34: 43-51 (1995).
Mahesh N, Padamwar V, and Pokharkar B. Development of vitamin loaded topical liposomal formulation using factorial design approach: Drug deposition and stability. Int. J. Pharm. 320: 37-44 (2006).
Manosroi A, Kongkaneramit L, and Manosroi J. Stability and transdermal absorption of topical amphotericin B liposome formulations. Int. J. Pharm. 270: 279–286 (2004).
Mirachandani H, and Chien YW. Drug delivery approaches for anti-HIV drugs. Int. J. Pharm. 95: 1-21 (1993).
Nagarsenker MS, and Londhe VY. Preparation and evaluation of a liposomal formulation of sodium cromoglicate. Int. J. Pharm. 251: 49 – 56 (2003).
Nii T, and Ishii F. Encapsulation efficiency of water – soluble and insoluble drgs in liposomes prepared by the microencapsulation vesicle method. Int. J. Pharm. 298: 198 – 205 (2005).
Notari S, Bocedi A, Ippolito G, Narciso P, Pucillo LP, Tossini G, Donnorso RF, Gasparrini F and Ascenzi P. Simultaneous determination of 16 anti-HIV drugs in human plasma by high-performance liquid chromatography. J. Chromo. B. 831: 258-266 (2006).
Palled MS, Rajesh PMN, Chatter M, and Bhat AR. Reverse Phase High Performance Liquid Chromatographic Determination of Zidovudine and Lamivudine in Tablet Dosage form, Ind. J. Pharm. Sci., 67: 96-97 (2005).
Panchagnula R, Bokalial R, Sharma P, and Khandavilli S. Transdermal delivery of naloxane: skin permeation, pharmacokinetic, irritancy and stability studies. Int. J. Pharm. 293: 213-223 (2005).
Pai NR, and Desai AS. Simultaneous Estimation of some Antiretroviral drugs from tablets by reverse phase High Performance Liquid Chromatography Method. Ind. Drugs. 42: 681- 687 (2005).
Prasad VG, Peter AC, and Ram BM. Gas chromatographic determination of residual levels of tert.-butanol from lyophilized liposomal formulations. J. Chrom. Biomedical. Appli. 620(1): 83-88 (1993).
Ricci M, Giovagnoli S, Blasi P, Schoubben A, Perioli L, and Rossi C. Development of liposomal capreomycin sulfate formulations: Effects of formulation variables on peptide encapsulation. Int. J. Pharm. 311: 172-181 (2006).
Sætern AM, Flaten GE, and Brandll MA. Method to Determine the Incorporation Capacity of Camptothecin in Liposomes. Pharm. Sci. Tech. 5(3):1-8 (2004).Stephen R, David WH, Gilman AG. Goodman and Gilman’s The Pharmacological Basis of Therapeutics, 8th Edn., Vol. II., Pergamom Press Inc., 1182, (1991).
Sarkar M, Khandavilli S, and Panchagnula R.. Development and validation of RP-HPLC and ultraviolet spectrophotometric methods of analysis for the quantitative estimation of antiretroviral drugs in pharmaceutical dosage forms. J. Chromo. B. 830: 349-354 (2006).
Stensrud G, Sande SA, Kristensen S, and Smistad G. Formulation and characterisation of primaquine loaded liposomes prepared by a pH gradient using experimental design. Int. J Pharm. 198: 213–228 (2000).
Stewart JCM. Colorimetric determination of phospholipids with ammonium ferrothiocyanate. Anal. Biochem. 104: 10–14 (1980).
Thomas NS, and Panchagnula R. Transdermal delivery of zidovudine: effect of vesicles on permeation across rat skin and their mechanism of action. Eur. J. Pharm. Sci. 18: 71-79 (2003).
Vemuri S, and Rhodes CT. Preparation and characterization of liposomes as therapeutic delivery systems:a review. Pharma. Acta. Hel., 70: 95-111 (1995).
Xiaomei M, and Zhensheng Z. Preparation and properties of poly(vinyl alcohol)-stabilized liposomes Int. J. Pharm. 318: 55–61 (2006).
