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Preparation and Bioavailability Assessment of SMEDDS Containing Valsartan

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Abstract

A self-microemulsifying drug delivery system (SMEDDS) has been developed to enhance diffusion rate and oral bioavailability of valsartan. The solubility of valsartan was checked in different oils, surfactants, and cosurfactants and ternary phase diagrams were constructed to evaluate the microemulsion domain. The valsartan SMEDDS was prepared using Capmul MCM (oil), Tween 80 (surfactant), and polyethylene glycol 400 (cosurfactant). The particle size distribution, zeta potential, and polydispersity index were determined and were found to be 12.3 nm, −0.746, and 0.138, respectively. Diffusion rate of valsartan was measured by in vitro dialysis bag method using phosphate buffer pH 6.8 as diffusion media. Developed high-performance liquid chromatography method was used to determine drug content in diffusion media. Oral bioavailability of valsartan SMEDDS was checked by using rabbit model. Results of diffusion rate and oral bioavailability of valsartan SMEDDS were compared with those of pure drug solution and of marketed formulation. Diffusion of valsartan SMEDDS showed maximum drug release when compared to pure drug solution and marketed formulation. The area under curve and time showed significant improvement as the values obtained were 607 ng h/mL and 1 h for SMEDDS in comparison to 445.36 and 1.36 h for market formulation suggesting significant increase (p < 0.01) in oral bioavailability of valsartan SMEDDS.

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Abbreviations

AUC:

area under curve

BA:

bioavailability

CD:

cyclodextrin

C max :

maximum concentration

GI:

gastrointestinal

HLB:

hydrophilic lipophilic balance

HPLC:

high-performance liquid chromatography

MRT:

mean residence time

o/w:

oil in water

PDI:

polydispersity index

S/CoS:

surfactant/cosurfactant

SMEDDS:

self-microemulsifying drug delivery system

T max :

maximum time

w/o:

water in oil

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Acknowledgment

We are thankful to Torrent Pharmaceuticals, Ahmedabad for providing Valsartan as a gift.

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Authors and Affiliations

  1. Pharmacy Department, The M.S. University of Baroda, Vadodara, Gujarat, India

    Adhvait R. Dixit, Sadhana J. Rajput & Samir G. Patel

  2. Dr. Reddy’s Laboratories Ltd., IPDO, Survey Nos. 42, 45 & 46, Bachupally, Qutubullpur, R.R. District, 500 072, Andhra Pradesh, India

    Adhvait R. Dixit

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  1. Adhvait R. Dixit
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  2. Sadhana J. Rajput
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  3. Samir G. Patel
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Correspondence to Adhvait R. Dixit.

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Dixit, A.R., Rajput, S.J. & Patel, S.G. Preparation and Bioavailability Assessment of SMEDDS Containing Valsartan. AAPS PharmSciTech 11, 314–321 (2010). https://doi.org/10.1208/s12249-010-9385-0

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