Liposomes as an ocular delivery system for acetazolamide: In vitro and in vivo studies
| Autor: | D M Patel, Nahed Mortada, Dr Awesh Yadav, Paul Wan Sia Heng, Gopal Rai, Celine Valeria Liew, Rania Hathout, Shyam S Pancholi |
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| Rok vydání: | 2007 |
| Předmět: |
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Surface Properties Administration Topical Drug Compounding Drug Evaluation Preclinical Pharmaceutical Science Aquatic Science Pharmacology Article Diffusion chemistry.chemical_compound In vivo Phosphatidylcholine Materials Testing Drug Discovery medicine Animals Particle Size Intraocular Pressure Ecology Evolution Behavior and Systematics Liposome Chromatography Ecology Chemistry Cholesterol General Medicine Phosphate Controlled release In vitro Acetazolamide Liposomes Rabbits Ophthalmic Solutions Pharmaceutical Vehicles Agronomy and Crop Science medicine.drug |
| Zdroj: | AAPS PharmSciTech. 8:E1-E12 |
| ISSN: | 1530-9932 |
| DOI: | 10.1208/pt0801001 |
| Popis: | The purpose of this study was to formulate topically effective controlled release ophthalmic acetazolamide liposomal formulations. Reverse-phase evaporation and lipid film hydration methods were used for the preparation of reverse-phase evaporation (REVs) and multilamellar (MLVs) acetazolamide liposomes consisting of egg phosphatidylcholine (PC) and cholesterol (CH) in the molar ratios of (7:2), (7:4), (7:6), and (7:7) with or without stearylamine (SA) or dicetyl phosphate (DP) as positive and negative charge inducers, respectively. The prepared liposomes were evaluated for their entrapment efficiency and in vitro release. Multilamellar liposomes entrapped greater amounts of drug than REVs liposomes. Drug loading was increased by increasing CH content as well as by inclusion of SA. Drug release rate showed an order of negatively chargedneutralpositively charged liposomes, which is the reverse of the data of drug loading efficiency. Physical stability study indicated that approximately 89%, 77%, and 69% of acetazolamide was retained in positive, negative, and neutral MLVs liposomal formulations up to a period of 3 months at 4 degrees C. The intraocular pressure (IOP)-lowering activity of selected acetazolamide liposomal formulations was determined and compared with that of plain liposomes and acetazolamide solution. Multilamellar acetazolamide liposomes revealed more prolonged effect than REVs liposomes. The positively charged and neutral liposomes exhibited greater lowering in IOP and a more prolonged effect than the negatively charged ones. The positive multilamellar liposomes composed of PC:CH:SA (7:4:1) molar ratio showed the maximal response, which reached a value of -7.8 +/- 1.04 mmHg after 3 hours of topical administration. |
| Databáze: | OpenAIRE |
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