PREPARATION AND EVALUATION OF MICROEMULSION CONTAINING ANTIHYPERTENSIVE DRUG
Keywords:Microemulsion, Surfactants, Solubility, Phase diagram
Objective: The aim of the present study was to design novel drug delivery system containing ramipril microemulsion. Ramipril is an antihypertensive drug having very low aqueous solubility and bioavailability. Ramipril microemulsion could be used as a possible alternative to the traditional oral formulation to improve dissolution rate and hence its bioavailability with avoidance of the first-pass metabolism.
Methods: The microemulsion existence region was determined by constructing pseudoternary phase diagram and prepared by using four components orange oil, tween 80 as a surfactant, propylene glycol as co-surfactant and distilled water as the aqueous phase. The water titration method was employed for its determination. All formulated microemulsion were subjected for visual inspection, centrifugation and stability test. The all stable formulations were selected for further study.
The optimized microemulsion formulation B-9 was subjected for various evaluation parameters such as, visual inspection, stability studies, pH, viscosity measurements, electrical conductivity, content uniformity and dye solubility test.
Results: Results revealed that construction of phase diagram and use of phase titration method was a suitable technique for the preparation of microemulsion as most of the formulations were transparent. It was found that the best microemulsion result was found for ratio 2:1. The results of stress tests conclude that the optimized formulation was both physically and chemically stable for 8 mo. Also, The Fourier transform infrared (FTIR) radiation measurement and Differential scanning calorimetry (DSC) of optimized formulation indicate the compatibility of ramipril with orange oil, surfactant-tween 80 and cosurfactant-propylene glycol. From electrical conductivity 0.283 Ïƒ and staining test the prepared optimized formulation B-9 was found to be o/w type of microemulsion. The optimized B-9 formulation showed good viscosity 13.52Â±0.01cps and pH 3.21Â±0.02 with highest drug content uniformity was found to be 84.98Â±0.02 %.
Conclusion: In the present study a satisfactory attempt was made to formulate a novel o/w microemulsion of ramipril which improves the gastrointestinal absorption by raising its water solubility and hence oral bioavailability is also enhanced.Â
C Srinivas, S Vanitha Sagar. Enhancing the bioavailability of simvastatin using microemulsion drug delivery system. Asian J Pharm Clin Res 2012;5:134-9.
Faizi Muzaffar, UK Singh, Lalit Chauhan. Review on microemulsion as futuristic drug delivery. Int J Pharm Pharm Sci 2013;5:39-53.
Ramaiyan Dhanapal. A review-microemulsion. Asian J Pharm Res 2012;2:23-9.
Sarkhejiya Naimish A, Nakum Mayur A, Patel Vipul P, Atara Samir A, Desai Thusarbindu R. Emerging trend of the microemulsion in formulation and research. Int Bull Drug Res 2010;1:54-83.
Tian Tian Tang, Xiong Bin Hu, De Hua Liao, Xin Yi Liu, Da Xiong Xiang. Mechanisms of microemulsion enhancing the oral bioavailability of puerarin: comparison between oil-in-water and water-in-oil microemulsions using the single-pass intestinal perfusion method and a chylomicron flow blocking approach. Int J Nanomed 2013;8:4415â€“26.
Sushama Talegaonkar, Adnan Azeem, Farhan J Ahmad, Roop K Khar, Shadab A Pathan, Zeenat I Khan. Microemulsions: a novel approach to enhanced drug delivery. J Korean Neurosurg Soc 2008;2:238-57.
M Joyce Nirmala, Srinivas Allankib, Amitava Mukherjeea, N Chandrasekarana. Enhancing the solubility of ramipril using a new essential oil based microemulsion system. Int J Pharm Pharm Sci 2013;5:322-3.
M Joyce Nirmala, N Chandrasekaran, Amitava Mukherjee. Enhanced solubilization of aqueous insoluble anti-hypertensive drug. Int J Pharm Pharm Sci 2012;4:366-8.
Divya A, Ch Praveen Kumar, K Gnanaprakash, M Gobinath. Design, formulation and characterization of tenofovir microemulsion as oral drug delivery. Int J Pharm Rev Res 2014;4:1-5.
Surjyanarayan Mandal, Snigdha S Mandal. Microemulsion drug delivery system: a platform for improving the dissolution rate of the poorly water-soluble drug. Int J Pharm Sci Nanotechnol 2011;3:1214-9.
Neha Tyagi, NV Sateesh Madhav. Formulation and evaluation of zidovudine microemulsion using a novel biopolymer from the seeds of buchanania llanzan. Int J Biopharm 2012;3:40-3.
Mandal Surjyanarayan, Mandal Snigdha S, Surti Naazneen, Patel Vandana B Parul, Arogya Seva Mandal. Design and development of squinavir microemulsion for the oral bioavailability enhancement. Int J Pharm Tech Res 2009;1:1442-8.
Jha SK, Dey S, Karki R. Department of Pharmaceutics, a microemulsions-potential carrier for improved drug delivery. Asian J Biomed Pharm Sci 2011;1:5-9.
Indian Pharmacopoeia, Government of India Ministry of Health and Family Welfare. Vol. III; 2014. p. 2639.
Shah RR, Magdum CS, Wadkar KA, Naikwade NS. Fluconazole topical microemulsion: preparation and evaluation. Res J Pharm Tech 2009;2:353-8.
Eskandar Moghimipour, Anayatollah Salimi, Soroosh Eftekhari. Design and characterization of microemulsion systems for naproxen. Adv Pharm Bull 2013;3:63-71.
Anindya Hana Iradhati, Mahdi Jufri. Formulation and physical stability test of griseofulvin microemulsion gel. Int J Appl Pharm 2017;9:23-6.
Vishal Yadav, Prakash Jadhav, Shailaja Dombe, Anjali Bodhe, Pranali Salunkhe. Formulation and evaluation of microsponge gel for topical delivery of the antifungal drug. Int J Appl Pharm 2017;9:30-7.