Peptides polycarbophil delivery

LueBen, H.L., Verhoef, J.C., Borchard, G., Lehr, C.-M., De Boer, A.G., and Junginger, H.E., Mucoadhesive polymers in peroral peptide drug delivery. II. Carbomer and polycarbophil are potent inhibitors of the intestinal proteolytic enzyme trypsin, Pharm. Res., 12 1293-1298 (1995). 

Luessen, H.L., et al. 1997. Mucoadhesive polymers in peroral peptide drug delivery. IV. Polycarbophil and chitosan are potent enhancers of peptide transport across intestinal mucosae in vitro. 

Clausen, A. E. and Bernkop-Schnurch, A. Development an in vitro evaluation of a peptide drug delivery system based on thiolated polycarbophil. Pharm. Ind. 2001 63, 312-... 

Bernkop-Schniirch, A., and S. Thaler. 2000. Polycarbophil-cysteine conjugates as platforms for oral (poly)peptide delivery systems. J Pharm Sci 89 901. 

Bernkop-Schnurch A, Marschtitz MK (1997) Development and in vivo evaluation of systems to protect peptide drugs from aminopeptidase N. Pharm Res 14 181-185 Bernkop-Schnurch A, Paikl C, Valenta C (1997) Novel bioadhesive chitosan-EDTA conjugate protects leucine enkephalin from degradation by aminopeptidase N. Pharm Res 14 917-922 Bernkop-Schnurch A, Thaler S (2000) Polycarbophil-cysteine conjugates as platforms for oral (poly)peptide delivery systems. J Pharm Sci 89 901-909 Bernkop-Schnurch A, Walker G, Zarti H (2001) Thiolation of polycarbophil enhances its inhibition of intestinal brush border membrane bound aminopeptidase N. J Pharm Sci 90 1907-1914... 

Peptide delivery It has also been reported that a polycarbophil hydrogel formulation increased the vaginal membrane permeability of GnRH, in comparison to a solution, in rats. Co-administration of the GnRH loaded gel with various enzyme inhibitors (EDTA, sodium taurodihydrofusidate and sodium laurate) resulted in ovulation-inducing activity comparable with that of a sc injection. 

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