Preparation and physicochemical characterization of poorly soluble drug-loaded lipid nanoparticles

Preparation and physicochemical characterization of poorly soluble drug-loaded lipid nanoparticles

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Title: Preparation and physicochemical characterization of poorly soluble drug-loaded lipid nanoparticles
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Article_Title: Preparation and physicochemical characterization of poorly soluble drug-loaded lipid nanoparticles
Authors: Răzvan Prisada, Cristina Dinu Pîrvu, Mariana Ferdeş, Alina Orţan, Corina Dalia Toderescu, Dumitru Lupuliasa
Affiliation: Physical and Colloidal Chemistry Department, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, Bucharest
University Polytechnic Bucharest
Analytical Chemistry Department, Faculty of Medicine, Pharmacy and Dental Medicine, ”Vasile Goldis” Western University, Arad, Romania
Pharmaceutical Technology and Biopharmacy Department, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, Bucharest, Romania
Abstract: This study presents the preparation and characterization of testosterone loaded lipid nanoparticles in order to obtain a topical system. The designed lipid nanostructures were prepared by conventional rotary evaporation method followed by mechanical dispersion in hydrating medium or by the method proposed by Touitou. The effects of formulation variables upon the liposomes` characteristics were also investigated. The experiments showed that the molar ratios of the drug, PC and Co influence the drug entrapment or, in the two case, the entrapment efficiency was affected by the percentage of ethanol, PC and TS in the formulation. The stability of the lipid vesicles was determined by the entrapment efficiency and size distribution. The studies were performed during a period of 2 months. Lipid vesicles prepared by Touitou method proved to be more stable than the first, in the same experimental conditions.
Keywords: lipid vesicles, topical application, entrapment efficiency, size distribution, stability
References: Barry B, Transdermal Drug Delivery in Pharmaceutics: The Science of Dosage Form Design, ed. Aulton E. M., Churchill Livingstone, 499 – 528, 2002.
Cevc G, Lipid vesicles and other colloids as drug carriers on the skin, in Advanced Drug Delivery Reviews 56, 675– 711, 2004.
Cevc G, Transfersomes: Innovative Transdermal Drug Carriers, in Modified Release Drug Delivery Technology, Rathbone J. M., Hadgraft J., Roberts M. S. (eds.), Marcel Dekker Inc., 533 – 547, 2003.
Elsayed M, Abdallah O, Naggar V, Khalafalah N: Deformable liposomes and ethosomes: Mechanism of enhanced skin delivery, International Jurnal of Pharmaceutics, 322, 60-66, 2006.
Godin B, Touitou E, Ethosomes: New prospects in transdermal delivery ,Therapeutic Drug Carriers Systems, 20, 63-102, 2003.
Honeywell-Nguyen PJ, Bouwstra JA ,Vesicles as a Tool for Transdermal and Dermal Delivery, Drug discovery Today: Technologies, 2,67-74, 2005.
Leucuţa SE, Biofarmacie şi farmacocinetică, Ed. Dacia, Cluj Napoca, 2002.
Ning M, Guo Y, Pan H, Chen X, Gu Z, Preparation and in-vitro and in vivo evaluation of liposomal/niosomal gel delivery systems for clotrimazole, Drug development and Industrial Pharmacy, 31, 375-383, 2005.
Solanki A, Parikh J, Parikh R, Preparation, Characterization, Optimization, and Stability Studies of Aceclofenac Proniosomes, Iranian Journal of Pharmaceutical Research., 7 (4), 237-246, 2008.
Touitou E., Godin B.,Weiss C., Enhanced Delivery of Drug Into and Across the Skin by Ethosomal Carriers, Drug Develop. Res., 50, 406-415, 2002
Vyas SP, Khar RK, Targeted and controlled drug delivery: Novel carrier systems ─Liposomes, CBS Publishers, 196-197, 2002.
Wen A H, Choi MK, Kim DD, Formulation of Liposome for Topical Delivery of Arbutin, Arch. Pharm. Res., 29(12), 1187-1192, 2006.
Read_full_article: pdf/22-2012/22-4-2012/SU22-4-2012-Prisada.pdf
Correspondence: Cristina Dinu Pîrvu, Colloidal and Physical Chemistry Department, “Carol Davila” University of Medicine and Pharmacy, Bucharest, no.6, Traian Vuia St., 020956, Tel. +40-(021)-3180751, Fax. +40-(021)-3180751, email: ecristinaparvu@yahoo.com

Read full article
Article Title: Preparation and physicochemical characterization of poorly soluble drug-loaded lipid nanoparticles
Authors: Răzvan Prisada, Cristina Dinu Pîrvu, Mariana Ferdeş, Alina Orţan, Corina Dalia Toderescu, Dumitru Lupuliasa
Affiliation: Physical and Colloidal Chemistry Department, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, Bucharest
University Polytechnic Bucharest
Analytical Chemistry Department, Faculty of Medicine, Pharmacy and Dental Medicine, ”Vasile Goldis” Western University, Arad, Romania
Pharmaceutical Technology and Biopharmacy Department, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, Bucharest, Romania
Abstract: This study presents the preparation and characterization of testosterone loaded lipid nanoparticles in order to obtain a topical system. The designed lipid nanostructures were prepared by conventional rotary evaporation method followed by mechanical dispersion in hydrating medium or by the method proposed by Touitou. The effects of formulation variables upon the liposomes` characteristics were also investigated. The experiments showed that the molar ratios of the drug, PC and Co influence the drug entrapment or, in the two case, the entrapment efficiency was affected by the percentage of ethanol, PC and TS in the formulation. The stability of the lipid vesicles was determined by the entrapment efficiency and size distribution. The studies were performed during a period of 2 months. Lipid vesicles prepared by Touitou method proved to be more stable than the first, in the same experimental conditions.
Keywords: lipid vesicles, topical application, entrapment efficiency, size distribution, stability
References: Barry B, Transdermal Drug Delivery in Pharmaceutics: The Science of Dosage Form Design, ed. Aulton E. M., Churchill Livingstone, 499 – 528, 2002.
Cevc G, Lipid vesicles and other colloids as drug carriers on the skin, in Advanced Drug Delivery Reviews 56, 675– 711, 2004.
Cevc G, Transfersomes: Innovative Transdermal Drug Carriers, in Modified Release Drug Delivery Technology, Rathbone J. M., Hadgraft J., Roberts M. S. (eds.), Marcel Dekker Inc., 533 – 547, 2003.
Elsayed M, Abdallah O, Naggar V, Khalafalah N: Deformable liposomes and ethosomes: Mechanism of enhanced skin delivery, International Jurnal of Pharmaceutics, 322, 60-66, 2006.
Godin B, Touitou E, Ethosomes: New prospects in transdermal delivery ,Therapeutic Drug Carriers Systems, 20, 63-102, 2003.
Honeywell-Nguyen PJ, Bouwstra JA ,Vesicles as a Tool for Transdermal and Dermal Delivery, Drug discovery Today: Technologies, 2,67-74, 2005.
Leucuţa SE, Biofarmacie şi farmacocinetică, Ed. Dacia, Cluj Napoca, 2002.
Ning M, Guo Y, Pan H, Chen X, Gu Z, Preparation and in-vitro and in vivo evaluation of liposomal/niosomal gel delivery systems for clotrimazole, Drug development and Industrial Pharmacy, 31, 375-383, 2005.
Solanki A, Parikh J, Parikh R, Preparation, Characterization, Optimization, and Stability Studies of Aceclofenac Proniosomes, Iranian Journal of Pharmaceutical Research., 7 (4), 237-246, 2008.
Touitou E., Godin B.,Weiss C., Enhanced Delivery of Drug Into and Across the Skin by Ethosomal Carriers, Drug Develop. Res., 50, 406-415, 2002
Vyas SP, Khar RK, Targeted and controlled drug delivery: Novel carrier systems ─Liposomes, CBS Publishers, 196-197, 2002.
Wen A H, Choi MK, Kim DD, Formulation of Liposome for Topical Delivery of Arbutin, Arch. Pharm. Res., 29(12), 1187-1192, 2006.
*Correspondence: Cristina Dinu Pîrvu, Colloidal and Physical Chemistry Department, “Carol Davila” University of Medicine and Pharmacy, Bucharest, no.6, Traian Vuia St., 020956, Tel. +40-(021)-3180751, Fax. +40-(021)-3180751, email: ecristinaparvu@yahoo.com