Novel Approaches for Oral Insulin Delivery - Pharmaceutical Technology

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Novel Approaches for Oral Insulin Delivery
The authors review various oral drug delivery systems that have been explored to increase patient compliance for insulin.

Pharmaceutical Technology
Volume 33, Issue 7

64. Leon-Bay, "N-acylated Alpha-Amino Acids as Novel Oral Delivery Agemts for Proteins," J Med Chem. 38, 4263–4269 (1995).

65. S. Milstein, "Partially Unfolded Proteins Efficiently Penetrate Cell Membranes- Implications for Oral Drug Delivery," J Controlled Release 53, 259–267 (1998).

66. J. Still and R. McAllister, "Effects of Orally Active Modified Insulin in TypeI Diabetic Patients," Clinical Pharmacol. Ther. 69 (2), (2001).

67. L.L. Chang, "Immunohistochemical Localization of Insulin Degrading Enzyme along the Rat Intestine, in the Human Colon Adenocarcinoma Cell Line (Caco-2) and in Human Ileum," J. Pharm Sci. 86, 116–119 (1997).

68. Y. Li, Z. Shao, and A.K. Mitra, "Dissociation of Insulin Oligomers by Bile Salt Micelles and Its Effect on Alpha-Chymotrypsin-Mediated Proteolytic Degradation," Pharm Res. 9 (7), 864–869. (1992).

69. R.J. Schilling and A.K. Mitra, "Intestinal Mucosal Transport of Insulin," Int. J. Pharm. 62, 53–64 (1990).

70. M. Bendayan et al., "Morpho-cytochemical and Biochemical Evidence for Insulin Absorption by the Rat Ileal Epithelium," Diabetologia. 33 (4), 197–204 (1990).

71. M. Bendayan et al., "Biochemical and Morpho-cytochemical Evidence for the Intestinal Absorption of Insulin in Control and Diabetic Rats. Comparison between the Effectiveness of Duodenal and Colon Mucosa," Diabetologia. 37 (2), 119–126 (1994).

72. J.J. Bergeron et al., "Polypeptide Hormone Receptors In Vivo: demonstration of Insulin Binding to Adrenal Gland and Gastrointestinal Epithelium by Quantitative Radioautography," J. Histochem. Cytochem. 28 (8), 824–835 (1980).

73. D.J. Pillion, V. Ganapathy, and F.H. Leibach, "Identification of Insulin Receptors on the Mucosal Surface of Colon Epithelial Cells," J. Biol Chem. 260 (9), 5244–5247. (1985).

74. R.L. Gingerich et al., "Identification and Characterization of Insulin Receptors in Basolateral Membranes of Dog Intestinal Mucosa," Diabetes 36 (10), 1124–1129 (1987).

75. R. Greenwood and A. Al-Achi, "Human Insulin Diffusion Profile through a Layer of Caco-2 Cells," Drug Dev. Ind. Pharm. 23, 221–224 (1997).

76. J. Brange and L. Langkjoer, "Insulin Structure and Stability," in Stability and Characterization of Protein and Peptide Drugs: Case Histories, Y.J. Wang and R. Pearlman, Eds. ( Plenum Press, New York, NY, 1993).

77 . O.L. Johnson, "Formulation of Proteins for Incorporation into Drug Delivery Sytems," in Protein Formulation and Delivery, E.J. McNally, Ed. (Marcel Dekker, New York, NY, 2000).

78. R. Pearlman and T.H. Nguyen, "Analysis of Protein Drugs," in Peptide and Protein Drug Delivery, V.H.L. Lee, Ed. (Marcel Dekker, New York, NY, 1991).

79. H. Hoffman, "Analytical Methods and Stability Testing of BioPharmaceuticals," in Protein Formulation and Delivery, E.J. McNally, Ed. (Marcel Dekker, New York, NY, 2000).

80. P.G. Shao and L.C. Bailey, "Porcine Insulin Biodegradable Polyester Microspheres: Stability and In Vitro Release Characteristics," Pharm Dev Technol. 5 (1), 1–9. (2000).

81. M.J. Pikal and D.R. Rigsbee, "The Stability of Insulin in Crystalline and Amorphous Solids: Observation of Greater Stability for the Amorphous Form," Pharm Res. 14 (10), 1379–1387. (1997).

82. R.T. Forbes et al., "Water Vapor Sorption Studies on the Physical Stability of a Series of Spray-Dried Protein/Sugar Powders for Inhalation," J. Pharm Sci. 87 (11), 1316–1321. (1998).


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