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Spontaneous Emulsification of Nifedipine-Loaded Self-Nanoemulsifying Drug Delivery System

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ABSTRACT

Self-nanoemulsifying drug delivery system (SNEDDS) can be used to improve dissolution of poorly water-soluble drugs. The objective of this study was to prepare SNEDDS by using ternary phase diagram and investigate their spontaneous emulsifying property, dissolution of nifedipine (NDP), as well as the pharmacokinetic profile of selected SNEDDS formulation. The results showed that the composition of the SNEDDS was a great importance for the spontaneous emulsification. Based on ternary phase diagram, the region giving the SNEDDS with emulsion droplet size of less than 300 nm after diluting in aqueous medium was selected for further formulation. The small-angle X-ray scattering curves showed no sharp peak after dilution at different percentages of water, suggesting non-ordered structure. The system was found to be robust in different dilution volumes; the droplet size was in nanometer range. In vitro dissolution study showed remarkable increase in dissolution of NDP from SNEDDS formulations compared with NDP powders. The pharmacokinetic study of selected SNEDDS formulation in male Wistar rats revealed the improved maximum concentration and area under the curve. Our results proposed that the developed SNEDDS formations could be promising to improve the dissolution and oral bioavailability of NDP.

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ACKNOWLEDGMENTS

Financial support from The Thailand Research Fund (grant number BRG5480013) is greatly acknowledged. YW is financially supported by the Royal Golden Jubilee Ph.D. Program (grant number PHD/0346/2550). The authors wish to thank Synchrotron Light Research Institute (Public Organization) (Nakhon Ratchasima, Thailand) for the beamtime, and Dr. Jitrin Chaiprapa for his guidance on SAXS experiment and data interpretation. The authors are grateful to Associate Professor Dr. Chaweewan Jansakul (Prince of Songkla University, Thailand) for her guidance on animal studies. Thanks to BASF (Thai) Co., Ltd. (Thailand) and Gattefosse (France) who kindly donated samples.

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Authors and Affiliations

  1. Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom, 73000, Thailand

    Yotsanan Weerapol, Sontaya Limmatvapirat & Pornsak Sriamornsak

  2. Pharmaceutical Biopolymer Group (PBiG), Faculty of Pharmacy, Silpakorn University, Nakhon Pathom, 73000, Thailand

    Yotsanan Weerapol, Sontaya Limmatvapirat & Pornsak Sriamornsak

  3. Department of Chemical and Pharmaceutical Technology, Beuth Hochschule für Technik Berlin, Luxemburger Str.10, Berlin, 13353, Germany

    Mont Kumpugdee-Vollrath

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  1. Yotsanan Weerapol
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Correspondence to Pornsak Sriamornsak.

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Weerapol, Y., Limmatvapirat, S., Kumpugdee-Vollrath, M. et al. Spontaneous Emulsification of Nifedipine-Loaded Self-Nanoemulsifying Drug Delivery System. AAPS PharmSciTech 16, 435–443 (2015). https://doi.org/10.1208/s12249-014-0238-0

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