Enhanced insulin absorption from sublingual microemulsions: effect of permeation enhancers

Drug Delivery and Translational Research
Nilam H Patil, Padma V Devarajan

Abstract

Microemulsions of insulin (50 IU/mL) comprising permeation enhancers were formulated for sublingual delivery. Circular dichroism (CD) spectra indicated conformational stability, while chemical stability was confirmed by high-performance liquid chromatography (HPLC). CD spectra of insulin in combination with permeation enhancers revealed attenuation of molar ellipticity at 274 nm in the order TCTP > TC-AOT > TC > TC-NMT > Sol P > insulin solution. The molar ellipticity ratios at 208/222 nm confirmed dissociation of insulin in the microemulsions with the same rank order. Matrix-assisted laser diffraction ionization mass spectra (MALDI) revealed a significant shift in intensity signals towards monomer and dimers with a substantially high ratio of monomers, especially in the presence of the TCTP and TC-AOT. Permeation through porcine sublingual mucosa correlated with the dissociation data. A high correlation between the ratio of molar ellipticity at 208/222 nm and serum glucose levels (r (2) > 0.958) and serum insulin levels (r (2) > 0.952) strongly suggests the role of dissociation of insulin on enhanced absorption. While all microemulsions revealed a reduction in serum glucose levels and increase in serum insulin levels, signific...Continue Reading

References

Sep 1, 1992·Pharmaceutical Research·Z ShaoA K Mitra
Jul 6, 1988·Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences·E N BakerC D Reynolds
Dec 1, 1983·Journal of Pharmaceutical Sciences·R Quinn, J D Andrade
Nov 1, 1984·Proceedings of the National Academy of Sciences of the United States of America·G D SmithC D Reynolds
Jan 1, 1996·European Biophysics Journal : EBJ·M LovattP Camilleri
Apr 17, 2002·International Journal of Pharmaceutics·Lianli LiKwon H Kim
Oct 9, 2002·Current Protein & Peptide Science·S M Kelly, N C Price
Mar 20, 2003·Journal of Controlled Release : Official Journal of the Controlled Release Society·Ming-Thau SheuHsiu-O Ho
Feb 9, 2005·Colloids and Surfaces. B, Biointerfaces·Reeta R GuptaManoj Varshney
May 19, 2006·Journal of Controlled Release : Official Journal of the Controlled Release Society·Jian WangKazuhiro Morimoto
Jun 30, 2006·International Journal of Clinical Practice·S Bellary, A H Barnett
Dec 11, 2007·Nature Biotechnology·George S Mack
Feb 19, 2008·International Journal of Pharmaceutics·Jie LiuZhirong Zhang
Mar 11, 2008·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Anja GrafThomas Rades
Jul 12, 2008·Journal of Biomedical Materials Research. Part B, Applied Biomaterials·Xin WangChaoxing Li
Oct 31, 2008·Langmuir : the ACS Journal of Surfaces and Colloids·Mark M BaileyCory Berkland
Dec 17, 2008·Recent Patents on Drug Delivery & Formulation·Sushama TalegaonkarZeenat I Khan
Jul 8, 2009·Journal of Colloid and Interface Science·Zhang YongLi Zhengqiang
Aug 28, 2009·Journal of Controlled Release : Official Journal of the Controlled Release Society·Yong-Mei YinDae-Duk Kim
Jul 27, 2010·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·G SharmaM N V Ravi Kumar
Aug 17, 2010·Journal of Controlled Release : Official Journal of the Controlled Release Society·Amnon C SintovShafir Botner
Dec 25, 2010·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Abdallah MakhlofHirofumi Takeuchi
Jan 10, 2012·Colloids and Surfaces. B, Biointerfaces·S JoseE B Souto
Jan 18, 2012·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Xiaoyan ZhangJianxu Sun

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Citations

Oct 16, 2019·Current Pharmaceutical Biotechnology·Haofan LiuLiandong Hu
Aug 6, 2015·Drug Delivery and Translational Research·Steven RossDennis Douroumis
Dec 15, 2020·Journal of Pharmaceutical Sciences·Dao Ge ChenXiang Yuan Xiong
Jan 29, 2020·Nanomedicine : Nanotechnology, Biology, and Medicine·Darsheen J Kotak, Padma V Devarajan
May 30, 2020·International Journal of Pharmaceutics·You XuVictor C Yang

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