A skin permeability model of insulin in the presence of chemical penetration enhancer.

作者: K.M. Yerramsetty , B.J. Neely , S.V. Madihally , K.A.M. Gasem

DOI: 10.1016/J.IJPHARM.2009.12.028

关键词: Skin structureQuantitative structure–activity relationshipPenetration (firestop)InsulinStereochemistryChemistrySkin permeabilityPermeationTransdermalBiological systemPenetration enhancer

摘要: Enhancing transdermal delivery of insulin using chemical penetration enhancers (CPEs) has several advantages over other non-traditional methods; however, lack suitable predictive models, make experimentation the only alternative for discovering new CPEs. To address this limitation, a quantitative structure-property relationship (QSPR) model was developed, predicting permeation in presence A virtual design algorithm that incorporates QSPR models CPE properties used to identify 48 potential Permeation experiments Franz diffusion cells and resistance were performed quantify effect CPEs on permeability skin structure, respectively. Of CPEs, 35 training 13 validation. In addition, 12 reported literature also included validation set. Differential evolution (DE) coupled with artificial neural networks (ANNs) develop non-linear models. The six-descriptor had 16% absolute average deviation (%AAD) set 4 misclassifications Five six descriptors found be statistically significant after sensitivity analyses. results suggest, molecules low dipoles are capable forming intermolecular bonds lipid bi-layers show promise as effective insulin-specific

参考文章(49)
Omathanu Pillai, Ramesh Panchagnula, Transdermal iontophoresis of insulin. V. Effect of terpenes. Journal of Controlled Release. ,vol. 88, pp. 287- 296 ,(2003) , 10.1016/S0168-3659(03)00065-8
Panchagnula R, Borkute, Sivaprasad N, Dey Cs, Pillai O, Kumar N, Transdermal iontophoresis of insulin: III. Influence of electronic parameters. Methods and Findings in Experimental and Clinical Pharmacology. ,vol. 26, pp. 399- 408 ,(2004)
Zheng Jm, Yang Wz, Hao Js, [Transdermal iontophoresis of insulin: effect of penetration enhancers on blood glucose level in diabetic rats]. Acta pharmaceutica Sinica. ,vol. 30, pp. 776- 780 ,(1995)
Omathanu Pillai, S.D. Borkute, N. Sivaprasad, Ramesh Panchagnula, Transdermal iontophoresis of insulin II. Physicochemical considerations International Journal of Pharmaceutics. ,vol. 254, pp. 271- 280 ,(2003) , 10.1016/S0378-5173(03)00034-6
Russell O. Potts, Richard H. Guy, Predicting skin permeability. Pharmaceutical Research. ,vol. 9, pp. 663- 669 ,(1992) , 10.1023/A:1015810312465
Gerard Cesidio Mazzenga, Bret Berner, Transdermal administration of zwitterionic drugs ,(1991)
G. David Garson, Interpreting neural-network connection weights AI Expert archive. ,vol. 6, pp. 46- 51 ,(1991) , 10.5555/129449.129452
Kenneth Price, Rainer M. Storn, Jouni A. Lampinen, Differential Evolution: A Practical Approach to Global Optimization Springer. ,(2014)
Lemont B. Kier, Lowell H. Hall, Molecular Connectivity VII: Specific Treatment of Heteroatoms Journal of Pharmaceutical Sciences. ,vol. 65, pp. 1806- 1809 ,(1976) , 10.1002/JPS.2600651228
Jan Příborský, Kozo Takayama, Tsuneji Nagai, Danuše Waitzová, Jiří Elis, Yuji Makino, Yoshiki Suzuki, Comparison of penetration-enhancing ability of laurocapram, N-methyl-2-pyrrolidone and dodecyl-L-pyroglutamate. Pharmacy World & Science. ,vol. 10, pp. 189- 192 ,(1988) , 10.1007/BF01956869