Dovepress Open Access to Scientific and Medical Research Open Access Full Text Article Preparation, Characterization, and in Vitro Release Study of Albendazole-encapsulated Nanosize Liposomes

The purpose of the present study was to formulate effective and controlled release albendazole liposomal formulations. Albendazole, a hydrophobic drug used for the treatment of hydatid cysts, was encapsulated in nanosize liposomes. Rapid evaporation method was used for the preparation of albendazole-encapsulated conventional and PEGylated liposomes consisting of egg phosphatidylcholine (PC) and cholesterol (CH) in the molar ratios of (6:4) and PC:CH: polyethylene glycol (PEG) (5:4:1), respectively. In this study, PEGylated and conventional liposomes containing albendazole were prepared and their characteristics, such as particle size, encapsulation efficiency, and in vitro drug release were investigated. The drug encapsulation efficiency of PEGylated and conventional liposomes was 81% and 72%, respectively. The biophysical characterization of both conventional and PEG-coated liposomes were done by transmission electron microscopy and UV-vis spectrophotometry. Efforts were made to study in vitro release of albendazole. The drug release rate showed decrease in albendazole release in descending order: free albendazole, albendazole-loaded conventional liposomes, and least with albendazole-loaded PEG-liposomes. Biologically relevant vesicles were prepared and in vitro release of liposome-entrapped albendazole was determined.

[1]  J. Graybill,et al.  Discrepancy between in vitro and in vivo antifungal activity of albendazole. , 1997, Journal of Medical and Veterinary Mycology.

[2]  B. C. Thanoo,et al.  Preparation, characterization and in vivo evaluation of 120-day poly(D,L-lactide) leuprolide microspheres. , 2001, Journal of controlled release : official journal of the Controlled Release Society.

[3]  S Singh,et al.  Study of azathioprine encapsulation into liposomes. , 1998, Journal of microencapsulation.

[4]  R. Schubert,et al.  Liposomal gels for vaginal drug delivery. , 2004, International journal of pharmaceutics.

[5]  N. Kiper,et al.  Treatment of Hydatid Disease , 2001, Paediatric drugs.

[6]  S. A. Sande,et al.  In vitro evaluation of drug release kinetics from liposomes by fractional dialysis , 1995 .

[7]  S. Mahor,et al.  Pegylated Protein Encapsulated Multivesicular Liposomes: A Novel Approach for Sustained Release of Interferon α , 2006, Drug development and industrial pharmacy.

[8]  M. Bally,et al.  The liposomal formulation of doxorubicin. , 2005, Methods in enzymology.

[9]  M. Newman,et al.  Pharmacokinetics, Biodistribution and Therapeutic Efficacy of Doxorubicin Encapsulated in Stealth® Liposomes (Doxil®) , 1994 .

[10]  A. Bangham,et al.  Cation Permeability of Phospholipid Model Membranes: Effect of Narcotics , 1965, Nature.

[11]  N. Oku,et al.  Antitumor activity of vincristine encapsulated in glucuronide-modified long-circulating liposomes in mice bearing Meth A sarcoma. , 1996, Biochimica et biophysica acta.

[12]  S. Vyas,et al.  Aerosolized liposome-based delivery of amphotericin B to alveolar macrophages. , 2005, International journal of pharmaceutics.

[13]  C. Ehrhardt,et al.  Assessing transferrin modification of liposomes by atomic force microscopy and transmission electron microscopy. , 2005, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[14]  Z. Pawłowski,et al.  Multicentre clinical trials of benzimidazole-carbamates in human cystic echinococcosis (phase 2). , 1989, Bulletin of the World Health Organization.

[15]  M. D. P. Guillermo Ramos,et al.  Hydatid Cyst of the Lung: Diagnosis and Treatment , 2001, World Journal of Surgery.

[16]  R N Zare,et al.  Rapid preparation of giant unilamellar vesicles. , 1996, Proceedings of the National Academy of Sciences of the United States of America.

[17]  J. Zhang,et al.  Development and characterization of a novel Cremophor EL free liposome-based paclitaxel (LEP-ETU) formulation. , 2005, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[18]  K. Maruyama,et al.  Intracellular targeting therapy of cisplatin‐encapsulated transferrin‐polyethylene glycol liposome on peritoneal dissemination of gastric cancer , 2002, International journal of cancer.

[19]  H. Baradaran,et al.  Albendazole versus placebo in treatment of echinococcosis. , 2001, Transactions of the Royal Society of Tropical Medicine and Hygiene.

[20]  Y. Tseng,et al.  Phase I and pharmacokinetic study of a stable, polyethylene‐glycolated liposomal doxorubicin in patients with solid tumors , 2001, Cancer.

[21]  M. Newman,et al.  Comparative pharmacokinetics, tissue distribution, and therapeutic effectiveness of cisplatin encapsulated in long-circulating, pegylated liposomes (SPI-077) in tumor-bearing mice , 1999, Cancer Chemotherapy and Pharmacology.

[22]  Taewon Hwang,et al.  Enhanced circulation time and antitumor activity of doxorubicin by comblike polymer-incorporated liposomes. , 2007, Journal of controlled release : official journal of the Controlled Release Society.

[23]  N. Oku,et al.  Therapeutic effect of adriamycin encapsulated in long‐circulating liposomes on meth‐a‐sarcoma‐bearing mice , 1994, International journal of cancer.

[24]  Rolf Schubert,et al.  Liposomal gels for vaginal drug delivery. , 2001, Methods in enzymology.

[25]  S. Law,et al.  Characterization of calcitonin-containing liposome formulations for intranasal delivery. , 2001, Journal of microencapsulation.

[26]  I. Antal,et al.  Gels and liposomes in optimized ocular drug delivery: studies on ciprofloxacin formulations. , 2007, International journal of pharmaceutics.

[27]  Chen Lin,et al.  Pharmacokinetic and cytotoxic studies of pegylated liposomal daunorubicin , 2006, Cancer Chemotherapy and Pharmacology.

[28]  R. Moreno-Esparza,et al.  Biopharmaceutics: Absorption Studies of Albendazole and Some Physicochemical Properties of the Drug and Its Metabolite Albendazole Sulphoxide , 1998, The Journal of pharmacy and pharmacology.

[29]  R. J. Horton.  Albendazole in treatment of human cystic echinococcosis: 12 years of experience. , 1997, Acta tropica.