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Design and Optimization of Controlled Drug Delivery System of Losartan Potassium


Affiliations
1 Department of Pharmaceutics, Krupanidhi College of Pharmacy, Chikka Bellandur, Carmelaram Post, Varthur Hobli, Bangalore - 560035, India
 

Purpose: The objective of the study was to develop microspheres of Losartan potassium as controlled drug delivery system by using various polymer (HPMC and Ethylcellulose), evaluating the relationship and influence of different content levels of HPMC, and Ethylcellulose, in order to achieve a zero order release of Losartan potassium.

Approach: Microspheres were prepared by solvent evaporation process. Release kinetics was evaluated by using United States Pharmacopoeia (USP) type I dissolution apparatus. The release mechanism of microspheres loaded with Losartan potassium was determined by fitting the data in Korsmeryer peppas equation. The regression coefficient values for Peppas model was found to be high, indicating adequate fitting. The 'n' value was ranged from 0.548 to 0.963 indicating Non Fickian diffusion for all the formulations. Optimization was performed by using desirability function. To validate the model, the optimized formula was subjected to in vitro characterization.

Findings: Release kinetics of Losartan potassium from these microspheres was principally regulated by HPMC K4M and Ethylcellulose. Percentage yield, entrapment efficiency and particle size of optimized formula was found to be 91.42%, 68.01% and 310μm. Formulation (F1) release at the end of 12 hours of dissolution studies was found to be 79.81%.

Conclusion: It can be concluded that Losartan potassium loaded microspheres could be successfully formulated by using HPMC 4KM and Ethylcellulose by solvent evaporation method to obtain maximum percentage yield, entrapment efficiency, desired particle size.


Keywords

Microspheres, Losartan Potassium, HPMC K4M, Ethylcellulose, Percentage Yield, Drug Content, Entrapment Efficiency.
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  • Bakris GL, Ritz E. The Message for World Kidney Day: Hypertension and Kidney Disease. Int. J Nephrology. 2009; 5(1):1540-2665.
  • Selvam RP, Singh AK, Sivakumar T. Transdermal drug delivery systems for antihypertensive drugs - A review. Int J Pharm Biomed Res. 2010; 1(1):1-8.
  • New Strategic Focus: Controlled-release drug delivery. 2007: BIO113B0602. Available from : URL:http://www.biovail.com. [12/10/20106].
  • Jain NK. Controlled and novel drug delivery. 1st ed. New Delhi: CBS publishers & Distributors Pvt. Ltd.; 1997. p.1, 236-51.
  • Vyas SP, Khar RK. Targeted and controlled drug delivery: Novel carrier systems. 1st ed. New Delhi: CBS publishers & Distributors; 2002. p.13, 417-54.
  • Belgamwar VS, Surana SJ. Design and Development of Oral Mucoadhesive Multiparticulate System Containing Atenolol: in vitro in vivo Characterization. Chem Pharm Bul. 2010; 58(9): 1168—1175.
  • Lachman L, Lieberman HA, Kanig JL editors. The theory and practice of industrial pharmacy. 3rd ed. Bombay (India): Varghee publishing house; 1991; 293-430.
  • Dandagi PM, Mastiholimath VS, Gadad AP, Iliger SR. Mucoadhesive Microspheres of Propranolol hydrochloride for nasal delivery. Int J Pharm. Sci. 2007; 69(3): 402-07.
  • Levis GA, Matheieu D, Phan-Tan-Luu R editors. Pharmaceutical Experimental Design. Newyork: Marcel Dekker; 2005; 183-185.
  • Costa P, Manuel J, Lobo S. Modeling and Comparison of dissolution profiles. Eur J Pharm. Sci. 2001; 13: 123-133.
  • International conference on harmonization (ICH) guidelines. Stability testing of new drug substances and products. ICH Q1A (R2) 2003.

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  • Design and Optimization of Controlled Drug Delivery System of Losartan Potassium

Abstract Views: 195  |  PDF Views: 75

Authors

C. Ashoka
Department of Pharmaceutics, Krupanidhi College of Pharmacy, Chikka Bellandur, Carmelaram Post, Varthur Hobli, Bangalore - 560035, India
Bharani S. Sogali
Department of Pharmaceutics, Krupanidhi College of Pharmacy, Chikka Bellandur, Carmelaram Post, Varthur Hobli, Bangalore - 560035, India
Hamed Barzeh
Department of Pharmaceutics, Krupanidhi College of Pharmacy, Chikka Bellandur, Carmelaram Post, Varthur Hobli, Bangalore - 560035, India

Abstract


Purpose: The objective of the study was to develop microspheres of Losartan potassium as controlled drug delivery system by using various polymer (HPMC and Ethylcellulose), evaluating the relationship and influence of different content levels of HPMC, and Ethylcellulose, in order to achieve a zero order release of Losartan potassium.

Approach: Microspheres were prepared by solvent evaporation process. Release kinetics was evaluated by using United States Pharmacopoeia (USP) type I dissolution apparatus. The release mechanism of microspheres loaded with Losartan potassium was determined by fitting the data in Korsmeryer peppas equation. The regression coefficient values for Peppas model was found to be high, indicating adequate fitting. The 'n' value was ranged from 0.548 to 0.963 indicating Non Fickian diffusion for all the formulations. Optimization was performed by using desirability function. To validate the model, the optimized formula was subjected to in vitro characterization.

Findings: Release kinetics of Losartan potassium from these microspheres was principally regulated by HPMC K4M and Ethylcellulose. Percentage yield, entrapment efficiency and particle size of optimized formula was found to be 91.42%, 68.01% and 310μm. Formulation (F1) release at the end of 12 hours of dissolution studies was found to be 79.81%.

Conclusion: It can be concluded that Losartan potassium loaded microspheres could be successfully formulated by using HPMC 4KM and Ethylcellulose by solvent evaporation method to obtain maximum percentage yield, entrapment efficiency, desired particle size.


Keywords


Microspheres, Losartan Potassium, HPMC K4M, Ethylcellulose, Percentage Yield, Drug Content, Entrapment Efficiency.

References