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[Studies on the insulin-liposomes double-coated by chitosan and chitosan-EDTA conjugates].
Yao Xue Xue Bao. 2004 Nov; 39(11):933-8.YX

Abstract

AIM

To evaluate the characteristics, the hypoglycemic efficacy and the pharmacokinetics of the insulin-liposomes double-coated by chitosan (CH) and chitosan-EDTA conjugates (CEC).

METHODS

Insulin-liposomes were prepared by reversed-phase evaporation. The protection of insulin against peptic and tryptic digestion was studied with HPLC. The hypoglycemic effects of insulin-liposomes were investigated using the glucose oxidase method after oral administration to rats. Serum insulin concentration in rats were determined by radio-immunoassay, and were assessed by Pkanalyst computer program.

RESULTS

The insulin-liposomes double-coated by CH and CEC was shown to protect insulin against digestion of pepsin, trypsin and gastrointestinal contents. In glucose tolerance test in normal rats, as compared with phosphate buffer solution control group, the insulin-liposomes coated by CH and CEC could reduce the glucose-induced peak of hyperglycemia. The reduction of the insulin-liposomes double-coated by CH and CEC was superior to that of other insulin-liposomes. When administered intragastrically to normal rats, the insulin-liposomes coated by CH and CEC could reduce glycemia measured after an overnight fast. The hypoglycemic effect the insulin-liposomes double-coated by CH and CEC was superior to that of other insulin-liposomes, and the dosage of 50 mu x kg(-1) decreased by 45.98% of initial blood glucose level at 1 h. As compared with subcutaneous injection, the relative pharmacological bioavailability was 17.02% calculated by area under the curve of glucose level versus time profile after oral administration of the insulin-liposomes double-coated by CH and CEC to rats. The serum insulin concentration-time curves were found to best fit the one-compartment open model. As compared with subcutaneous injection, the relative bioavailability was 8.91% calculated by the area under the curve of serum insulin concentration versus time profile after oral administration of the insulin-liposomes double-coated by CH and CEC to rats.

CONCLUSION

The stability and absorption of insulin-liposomes double-coated by CH and CEC was superior to that of the insulin-liposomes coated either by CH, or by CEC respectively.

Authors+Show Affiliations

Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

English Abstract
Journal Article

Language

chi

PubMed ID

15696937

Citation

Wu, Zheng-Hong, et al. "[Studies On the Insulin-liposomes Double-coated By Chitosan and chitosan-EDTA Conjugates]." Yao Xue Xue Bao = Acta Pharmaceutica Sinica, vol. 39, no. 11, 2004, pp. 933-8.
Wu ZH, Ping QN, Song YM, et al. [Studies on the insulin-liposomes double-coated by chitosan and chitosan-EDTA conjugates]. Yao Xue Xue Bao. 2004;39(11):933-8.
Wu, Z. H., Ping, Q. N., Song, Y. M., Lei, X. M., Li, J. Y., & Cai, P. (2004). [Studies on the insulin-liposomes double-coated by chitosan and chitosan-EDTA conjugates]. Yao Xue Xue Bao = Acta Pharmaceutica Sinica, 39(11), 933-8.
Wu ZH, et al. [Studies On the Insulin-liposomes Double-coated By Chitosan and chitosan-EDTA Conjugates]. Yao Xue Xue Bao. 2004;39(11):933-8. PubMed PMID: 15696937.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - [Studies on the insulin-liposomes double-coated by chitosan and chitosan-EDTA conjugates]. AU - Wu,Zheng-Hong, AU - Ping,Qi-Neng, AU - Song,Yun-Mei, AU - Lei,Xiao-Min, AU - Li,Jian-Ying, AU - Cai,Peng, PY - 2005/2/9/pubmed PY - 2005/7/27/medline PY - 2005/2/9/entrez SP - 933 EP - 8 JF - Yao xue xue bao = Acta pharmaceutica Sinica JO - Yao Xue Xue Bao VL - 39 IS - 11 N2 - AIM: To evaluate the characteristics, the hypoglycemic efficacy and the pharmacokinetics of the insulin-liposomes double-coated by chitosan (CH) and chitosan-EDTA conjugates (CEC). METHODS: Insulin-liposomes were prepared by reversed-phase evaporation. The protection of insulin against peptic and tryptic digestion was studied with HPLC. The hypoglycemic effects of insulin-liposomes were investigated using the glucose oxidase method after oral administration to rats. Serum insulin concentration in rats were determined by radio-immunoassay, and were assessed by Pkanalyst computer program. RESULTS: The insulin-liposomes double-coated by CH and CEC was shown to protect insulin against digestion of pepsin, trypsin and gastrointestinal contents. In glucose tolerance test in normal rats, as compared with phosphate buffer solution control group, the insulin-liposomes coated by CH and CEC could reduce the glucose-induced peak of hyperglycemia. The reduction of the insulin-liposomes double-coated by CH and CEC was superior to that of other insulin-liposomes. When administered intragastrically to normal rats, the insulin-liposomes coated by CH and CEC could reduce glycemia measured after an overnight fast. The hypoglycemic effect the insulin-liposomes double-coated by CH and CEC was superior to that of other insulin-liposomes, and the dosage of 50 mu x kg(-1) decreased by 45.98% of initial blood glucose level at 1 h. As compared with subcutaneous injection, the relative pharmacological bioavailability was 17.02% calculated by area under the curve of glucose level versus time profile after oral administration of the insulin-liposomes double-coated by CH and CEC to rats. The serum insulin concentration-time curves were found to best fit the one-compartment open model. As compared with subcutaneous injection, the relative bioavailability was 8.91% calculated by the area under the curve of serum insulin concentration versus time profile after oral administration of the insulin-liposomes double-coated by CH and CEC to rats. CONCLUSION: The stability and absorption of insulin-liposomes double-coated by CH and CEC was superior to that of the insulin-liposomes coated either by CH, or by CEC respectively. SN - 0513-4870 UR - https://www.unboundmedicine.com/medline/citation/15696937/[Studies_on_the_insulin_liposomes_double_coated_by_chitosan_and_chitosan_EDTA_conjugates]_ L2 - https://antibodies.cancer.gov/detail/CPTC-GST+Mu1-6 DB - PRIME DP - Unbound Medicine ER -