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Design and Evaluation of Self-Nanoemulsifying Pellets of Repaglinide

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Abstract

The aim of study was to develop self-nanoemulsifying pellets (SNEP) for oral delivery of poorly water soluble drug, repaglinide (RPG). Solubility of RPG in oily phases and surfactants was determined to identify components of self-nanoemulsifying drug delivery system (SNEDDS). The surfactants and cosurfactants were screened for their ability to emulsify oily phase. Ternary phase diagrams were constructed to identify nanoemulsification area for the selected systems. SNEDDS formulations with globule size less than 100 nm were evaluated for in vivo anti-hyperglycemic activity in neonatal streptozotocin rat model. A significant reduction in glucose levels was produced by optimized SNEDDS formulation in comparison to the control group. The optimized SNEDDS formulations were pelletized via extrusion/spheronization technique using microcrystalline cellulose and lactose. SNEP were characterized by X-ray powder diffraction and scanning electron microscopy. X-ray diffraction study indicated loss of crystallinity of RPG in SNEP. The SNEP exhibited good flow properties, mechanical strength and formed nanoemulsion with globule size less than 200 nm. SNEP showed in vitro release of more than 80% RPG in 10 min which was significantly higher than RPG containing reference pellets. In conclusion, our studies illustrated that RPG, a poorly water soluble drug can be successfully formulated into SNEP which can serve as a promising system for the delivery of poorly water soluble drugs.

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Acknowledgments

The authors are thankful to USV India Pvt. Limited, India for providing gift sample of repaglinide. We are thankful to Colorcon Asia Pvt. Ltd., India; Gattefosse India Pvt Ltd., India; BASF India Ltd., India; Karlshamns AB., Sweden; S. Zaveri & Co., India; for providing gift samples of oils and surfactants. The authors are also thankful to Associated Capsules, India, for gift sample of hard gelatin capsules. The authors wish to thank Mr. Nilesh Kulkarni, Tata Institute of Fundamental Research (TIFR), Mumbai, India for carrying out X-ray diffraction studies. The authors are thankful to the Department of Biotechnology (DBT), New Delhi, for providing fellowship.

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  1. Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz (E), Mumbai, 400098, India

    N. S. Desai & M. S. Nagarsenker

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  1. N. S. Desai
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  2. M. S. Nagarsenker
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Correspondence to M. S. Nagarsenker.

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Desai, N.S., Nagarsenker, M.S. Design and Evaluation of Self-Nanoemulsifying Pellets of Repaglinide. AAPS PharmSciTech 14, 994–1003 (2013). https://doi.org/10.1208/s12249-013-9990-9

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  • DOI: https://doi.org/10.1208/s12249-013-9990-9

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