4.6 Article

Enhanced insulin absorption from sublingual microemulsions: effect of permeation enhancers

期刊

DRUG DELIVERY AND TRANSLATIONAL RESEARCH
卷 4, 期 5-6, 页码 429-438

出版社

SPRINGER HEIDELBERG
DOI: 10.1007/s13346-014-0205-z

关键词

Insulin; Permeation enhancer; Sublingual; Microemulsion; Circular dichroism; MALDI; Vitamin E TPGS

资金

  1. University Grants Commission, Government of India

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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, significant differences were observed with the TCTP and TC-AOT microemulsions. High pharmacological availability >60 % and bioavailability >55 % compared to subcutaneous insulin at a low dose of 2 IU/kg appears highly promising. The data clearly suggests the additional role of the permeation enhancers on dissociation of insulin on enhanced sublingual absorption from the microemulsions.

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