DESIGN, OPTIMIZATION AND IN VITRO CHARACTERIZATION OF SELF NANO EMULSIFYING DRUG DELIVERY SYSTEM OF OLMESARTAN MEDOXOMIL

Authors

  • Sreenivas Patro Sisinthy School of Pharmacy, Taylors University, Malaysia
  • Nalamolu Koteswara Rao School of Medicine, Taylors University, Malaysia
  • Chin Yi Lynn Sarah School of Pharmacy, Taylors University, Malaysia

DOI:

https://doi.org/10.22159/ijpps.2017v9i1.15166

Keywords:

Olmesartan, SNEDDS, Dissolution, Box-Behnken, Optimization

Abstract

Objective: The objective of the present study was to design, optimise and characterise self nano emulsifying drug delivery systems (SNEDDS) for a poorly water soluble drug, olmesartan medoxomil (OLM) by Formulation by Design (FbD) approach with an aim to improve its solubility and dissolution.

Methods: The SNEDDS were systematically optimised using three factor Box-Behnken design. Concentration of formulation variables, namely, the oil phaseX1 (Capryol 90), the surfactant X2 (Cremophor EL), and the co-surfactant X3 (Transcutol P), was optimized for its impact on mean globule size (Y1), percentage drug release in 20 min (Y2) and turbidity (Y3) of the formulation. Ternary phase diagrams were constructed to select the areas of nanoemulsion and the amounts of oil, surfactant and cosurfactants as critical formulation variables. The prepared SNEDDS were characterised for globule size, dissolution studies, turbidity, and transmission electron microscopy (TEM).

Results: Following optimisation, the values of formulation variables were found to be 142.276 mg (Capryol P), 399.999 mg (Cremophor EL) and 598.871 mg (Transcutol P) which produced a globule size of 12.64 nm, percentage drug release of 93.34% and a turbidity of 0.02 FNU. TEM studies demonstrated spherical droplet morphology.

Conclusion: Thus, the present studies reveal that the SNEDDS is a promising drug delivery system approach for the enhancement of solubility and dissolution rate of OLM.

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References

Chabukswar AR, Kuchekar BS, Jagdale SC, Mehetre DM, More AS, Lokhande PD. Development and validation of an RP-HPLC method for simultaneous estimation of olmesartan medoxomil and amlodipine besylate in tablet dosage form. Arch Appl Sci Res 2010;2:307-12.

Raval C, Joshi N, Patel J, Upadhyay UM. Enhanced oral bioavailability of olmesartan by using novel solid self-emulsifying drug delivery system. Int J Adv Pharm 2012;2:82-92.

Kang MJ, Kim HS, Jeon HS, Park JH, Lee BS, Ahn BK, et al. In situ intestinal permeability and in vivo absorption characteristics of olmesartan medoxomil in self-micro emulsifying drug delivery system. Drug Dev Ind Pharm 2012;38:587-96.

Khade S, Pore Y. Formulation and evaluation of neusilin US2 adsorbed amorphous solid self-micro emulsifying delivery system of atorvastatin calcium. Asian J Pharm Clin Res 2016;9:93-100.

Date AA, Desai N, Dixit R, Nagarsenker M. Self-nanoemulsifying drug delivery systems: formulation insights, applications and advances. Nanomed 2010;5:1595-616.

Kallakunta VR, Bandari S, Jukanti R, Veerareddy PR. Oral self-emulsifying powder of lercanidipine hydrochloride: formulation and evaluation. J Powder Technol 2012;221:375-82.

Narang AS, Delmarre D, Gao D. Stable drug encapsulation in micelles and microemulsions. Int J Pharm 2007;345:9-25.

Gursoy RN, Benita S. Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs. Biomed Pharmacother 2004;58:173-82.

Anand S, Gupta R, Prajapati SK. Self-micro emulsifying drug delivery system. Asian J Pharm Clin Res 2016;9:1-6.

Nasr A, Gardouh A, Ghoniam H, Abdelghany E, Ghorab M. Effect of oils, surfactants and cosurfactants on phase behavior and physicochemical properties of self-nanoemulsifying drug delivery system (SNEDDS) for irbesartan and olmesartan. Int J Appl Pharm 2016;8:13-24.

Basalious EB, Shawky N, Badr-Eldin SM. SNEDDS containing bioenhancers for improvement of dissolution and oral absorption of lacidipine: I. Development and optimization. Int J Pharm 2010;391:203-11.

Kumanan R, Jitendra MR, Manasa R. Stability indicating RP-HPLC method development and validation of olmesartan medoxomil. Asian J Pharm Biol Res 2011;1:79-86.

Singh B, Khurana L, Bandyopadhay S, Kapil R, Katare OO. Development of optimized self-nanoemulsifying drug delivery systems (SNEDDS) of carvedilol with enhanced bioavailability potential. Drug Delivery 2011;18:599-612.

Date AA, Nagarsenker MS. Design and evaluation of self-nanoemulsifying drug delivery systems (SNEDDS) for cefpodoxime proxetil. Int J Pharm 2007;329:166-72.

Baek MK, Lee JH, Cho YO, Kim HH, Lee GW. Self-microemulsifying drug-delivery system for improved oral bioavailability of pranlukast hemihydrate: preparation and evaluation. Int J Nanomed 2013;8:167-76.

Palamakula A, Nutan MHT, Khan MA. Response surface methodology for optimization and characterization of Limonene-based coenzyme Q10 self nanoemulsified capsule dosage form. AAPS PharmSciTech 2004;5:114-21.

Bahloul B, Lassoued MA, Souad S. A novel approach for the development and optimization of self emulsifying drug delivery system using HLB and response surface methodology: application to fenofibrate encapsulation. Int J Pharm 2014; 466:341-8.

Pawar YB, Purohit H, Valicherla GR, Munjal B, Lale SV, Patel SB, et al. Novel lipid based oral formulation of curcumin: development and optimization by design of experiments approach. Int J Pharm 2012;436:617-23.

Jain AK, Thanki K, Jain S. Solidified self-nanoemulsifying formulation for oral delivery of combinatorial therapeutic regimen: part I. Formulation development, statistical optimization, and in vitro characterization. Pharm Res 2014;31:923-45.

Beg S, Swain S, Singh HP, Patra ChN, Rao ME. Development, optimization, and characterization of solid self-nanoemulsifying drug delivery systems of valsartan using porous carriers. AAPS PharmSciTech 2012;13:1416-27.

Singh S, Pathak K, Bali V. Product development studies on surface-adsorbed nanoemulsion of olmesartan medoxomil as a capsular dosage form. AAPS PharmSciTech 2012;13:1212-21.

Luykx DM, Peters RJ, van Ruth SM, Bouwmeester H. A review of analytical methods for the identification and characterization of nano delivery systems in food. J Agric Food Chem 2008;56:8231-47.

Taha EI. Development and characterization of new indomethacin self-nanoemulsifying formulations. Sci Pharm 2009;77:443-51.

Richard AS, James MH, Tod FJ, Myles S. Effects of sinker shapes on dissolution profiles. J Pharm Sci 2006;78:35-9.

Villar AMS, Naveros BC, Campmany ACC, Trenchs MA, Rocabert CB, Bellowa LH. Design and optimization of self-nanoemulsifying drug delivery systems (SNEDDS) for enhanced dissolution of gemfibrozil. Int J Pharm 2012; 431:161–75.

Patel J, Patel A, Raval M, Sheth N. Formulation and development of a self-nanoemulsifying drug delivery system of irbesartan. J Adv Pharm Technol Res 2011;2:9-16.

Huang YB, Tsai YH, Lee SH, Chang JS, Wu PC. Optimization of pH-dependent release of nicardipine hydrochloride extended-release matrix tablets using response surface methodology. Int J Pharm 2005;289:87-95.

Balakrishnan P, Lee BJ, Oh DH, Kim JO, Lee YI, Kim DD, et al. Enhanced oral bioavailability of coenzyme Q10 by self-emulsifying drug delivery systems. Int J Pharm 2009; 374:66-72.

Marasini N, Yan YD, Poudel BK, Choi HG, Yong CS, Kim JO. Development and optimization of self-nanoemulsifying drug delivery system with enhanced bioavailability by box–behnken design and desirability function. J Pharm Sci 2012;101:4584-96.

Wu XG, Li G, Gao YL. Optimization of the preparation of nalmefene-loaded sustained-release microspheres using central composite design. Chem Pharm Bull 2006;54:977-81.

Published

01-01-2017

How to Cite

Sisinthy, S. P., N. K. Rao, and C. Y. L. Sarah. “DESIGN, OPTIMIZATION AND IN VITRO CHARACTERIZATION OF SELF NANO EMULSIFYING DRUG DELIVERY SYSTEM OF OLMESARTAN MEDOXOMIL”. International Journal of Pharmacy and Pharmaceutical Sciences, vol. 9, no. 1, Jan. 2017, pp. 94-101, doi:10.22159/ijpps.2017v9i1.15166.

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