Insulin Formulation and Delivery

Brange, Jens; Langkjaer, L.

doi:10.1007/0-306-46803-4_13

Cited by 47 publications

(49 citation statements)

References 390 publications

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“…The optimal method of insulin delivery must be safe, should provide insulin to diabetic patients in a way that will correct the metabolic abnormalities of diabetes mellitus, and must be psychologically and socially acceptable (Brange and Langkjaer, 1997). Although oral administration of insulin is of greatest interest, its low bioavailability has not permitted to achieve an efficient formulation.…”

Section: Introductionmentioning

confidence: 99%

Alginate microspheres prepared by internal gelation: Development and effect on insulin stability

Silva

Ribeiro

Figueiredo

et al. 2006

International Journal of Pharmaceutics

183

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Recombinant human insulin was encapsulated within alginate microspheres by the emulsification/internal gelation technique with the objective of preserving protein stability during encapsulation procedure. The influence of process and formulation parameters was evaluated on the morphology and encapsulation efficiency of insulin. The in vitro release of insulin from microspheres was studied under simulated gastrointestinal conditions and the in vivo activity of protein after processing was assessed by subcutaneous administration of extracted insulin from microspheres to streptozotocin-induced diabetic rats. Microspheres mean diameter, ranging from 21 to 287 m, decreased with the internal phase ratio, emulsifier concentration, mixer rotational speed and increased with alginate concentration. Insulin encapsulation efficiency, near 75%, was not affected by emulsifier concentration, mixer rotational speed and zinc/insulin hexamer molar ratio but decreased either by increasing internal phase ratio and calcium/alginate mass ratio or by decreasing acid/calcium molar ratio and alginate concentration. A high insulin release, above 75%, was obtained at pH 1.2 and under simulated intestinal pH a complete dissolution of microspheres occurred. Extracted insulin from microspheres decreased hyperglycemia of diabetic rats proving to be bioactive and showing that encapsulation in alginate microspheres using the emulsification/internal gelation is an appropriate method for protein encapsulation.

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Section: Introductionmentioning

confidence: 99%

Alginate microspheres prepared by internal gelation: Development and effect on insulin stability

Silva

Ribeiro

Figueiredo

et al. 2006

International Journal of Pharmaceutics

183

View full text Add to dashboard Cite

show abstract

“…Intermediate-and longacting insulins have been complexed with protamine (NPH insulins) or the hexamerstabilizing agent zinc (lente and ultralente insulins) to delay absorption (3,4). These formulations fall short of maintaining optimal glycemic control because of a pronounced insulin peak after injection, variable absorption, or a duration of action that still falls short of the ideal basal insulin (5)(6)(7). Development of improved long-acting insulins constitutes an important step toward improving the quality of glycemic control and avoiding long-term complications of diabetes (8,9).…”

mentioning

confidence: 99%

Basal insulin glargine (HOE 901) versus NPH insulin in patients with type 1 diabetes on multiple daily insulin regimens. U.S. Insulin Glargine (HOE 901) Type 1 Diabetes Investigator Group.

2000

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OBJECTIVE: Insulin glargine (HOE 901, 21(A)-Gly-30(B)a-L-Arg-30(B)b-L-Arg human insulin) is a novel recombinant analog of human insulin with a shift in the isoelectric point producing a retarded absorption rate and an increased duration of action that closely mimics normal basal insulin secretion. It recently received approval from the Food and Drug Administration. The aim of this study was to evaluate 2 formulations of insulin glargine for safety and efficacy in the treatment of patients with type 1 diabetes. RESEARCH DESIGN AND METHODS: In a 4-week trial, 256 patients with type 1 diabetes received either NPH insulin or insulin glargine containing 30 microg/ml zinc (insulin glargine[30]) or 80 microg/ml zinc (insulin glargine[80]). Insulin glargine was given subcutaneously once daily at bedtime. NPH insulin was given either once daily (at bedtime) or twice daily (before breakfast and at bedtime), according to the patient's prestudy regimen. The initial doses of insulin glargine and NPH were based on the previous NPH total daily dose. RESULTS: At study end point, insulin glargine-pooled groups had significantly lower fasting plasma glucose (FPG) levels than the NPH insulin group, with adjusted mean FPG levels reduced by 2.2 mmol/l (P = 0.0001). Insulin glargine was superior to NPH insulin in reducing FPG levels in patients who had previously received NPH insulin twice daily but not in patients who had previously received NPH once daily. FPG levels were more stable in patients using insulin glargine than in patients using NPH insulin. A subset of patients (n = 71) underwent hourly overnight plasma glucose measurements. Insulin glargine patients exhibited lower FPG levels after 5:00 A.M.; the difference was significant by 8:00 A.M. The adjusted mean FPG for insulin glargine[30] was 7.8 mmol/l; for insulin glargine[80], 7.3 mmol/l; and for NPH, 10.7 mmol/l. Both formulations of insulin glargine were well tolerated, similar to NPH insulin. CONCLUSIONS: Basal insulin glargine administered once daily for 4 weeks as part of a basal-bolus multiple daily insulin regimen was safe and more effective in lowering fasting plasma glucose levels than NPH in patients with type 1 diabetes.

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“…Therefore, there is a continuous search for improved insulin formulations in order to reproduce the physiological pattern of insulin secretion as close as possible and, thereby, to minimize the complications of diabetes mellitus. Numerous attempts to deliver insulin by routes avoiding injections have been reported in the literature: buccal, nasal, oral, rectal, pulmonary, ocular, transdermal, vaginal, and intrauterine (Brange & Langkjaer, 1997;Owens et al, 2003;Peppas & Kavimandan, 2006). Of all these routes, oral administration would be the most desirable on the long-term basis.…”

Section: Introductionmentioning

confidence: 99%

Influence of polymers ratio on insulin-loaded nanoparticles based on poly-ε-caprolactone and Eudragit^®RS for oral administration

Socha¹,

Sapin²,

Damgé³

et al. 2009

Drug Delivery

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Insulin Formulation and Delivery

Cited by 47 publications

References 390 publications

Alginate microspheres prepared by internal gelation: Development and effect on insulin stability

Alginate microspheres prepared by internal gelation: Development and effect on insulin stability

Basal insulin glargine (HOE 901) versus NPH insulin in patients with type 1 diabetes on multiple daily insulin regimens. U.S. Insulin Glargine (HOE 901) Type 1 Diabetes Investigator Group.

Influence of polymers ratio on insulin-loaded nanoparticles based on poly-ε-caprolactone and Eudragit^®RS for oral administration

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Insulin Formulation and Delivery

Cited by 47 publications

References 390 publications

Alginate microspheres prepared by internal gelation: Development and effect on insulin stability

Alginate microspheres prepared by internal gelation: Development and effect on insulin stability

Basal insulin glargine (HOE 901) versus NPH insulin in patients with type 1 diabetes on multiple daily insulin regimens. U.S. Insulin Glargine (HOE 901) Type 1 Diabetes Investigator Group.

Influence of polymers ratio on insulin-loaded nanoparticles based on poly-ε-caprolactone and Eudragit®RS for oral administration

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Influence of polymers ratio on insulin-loaded nanoparticles based on poly-ε-caprolactone and Eudragit^®RS for oral administration