Design and Development of Oral Nanoparticulated Insulin in Multiple Emulsion

Author(s): T. Venkata Siddhartha, V. Senthil, Ilindra Sai Kishan, Rizwan Basha Khatwal, SubbaRao V. Madhunapantula

Journal Name: Current Drug Delivery

Volume 11 , Issue 4 , 2014

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Graphical Abstract:


The present research aimed at developing an injection-free nanoparticulated formulation in multiple emulsion form, for oral delivery of insulin, which otherwise undergoes degradation in the gastric environment if administered orally. Insulin-polymeric nanoparticles were prepared using layer by layer (LbL) adsorption method and incorporated into an emulsion to form a nanoparticulated multiple emulsion. Using 0.6 M sodium chloride, the insulin nanoaggregates of 300-400 nm size were obtained about a yield of 94%. The characteristics of a representative nanoparticle were as follows: particle size - 391.9±0.41 nm, polydispersity index -0.425, zeta potential- +20.6 mv, encapsulation efficiency- 86.7±1.42% and percentage entrapment efficiency of the insulin-polymeric nanoparticles in the inner aqueous phase of emulsion was 84.6%. The FT-IR analysis confirms that there were no drug interactions with the polymers. Stability analysis carried out for 3 months at 8-40 °C, showed only minor changes at the end period. The release kinetics of the nanoparticulated multiple emulsion at pH 7.4 followed first order kinetics and obeyed the Fickian law. However, at pH 2.0 the release kinetics from nanoparticulated multiple emulsion followed zero order kinetics without obeying to the Fickian law. In conclusion, our data demonstrate that the nanoparticulated multiple emulsion formulation has good release characteristics and imparted a tolerable protection for insulin at different pH conditions, which may be exploited for oral administration.

Keywords: Insulin, layer by layer (LbL), polymeric nanoparticles, multiple emulsion, methyl methacrylate and chitosan.

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Article Details

Year: 2014
Published on: 14 April, 2014
Page: [472 - 485]
Pages: 14
DOI: 10.2174/1567201811666140414115259
Price: $65

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