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Relationship between drug effects and particle size of insulin-loaded bioadhesive microspheres.
Acta Pharmacol Sin. 2002 Nov; 23(11):1051-6.AP

Abstract

AIM

To formulate and characterize insulin-loaded adhesive microspheres (MP) and evaluate drug effects of MP with various sizes, 120, 350, and 1000 nm in diameter, in the alloxan-induced diabetic rats.

METHODS

Insulin-loaded MP were formulated by an ionotropic gelation procedure. Particle size distributions were determined by photon correlation spectroscopy and optical microscopy. The factors that influenced the particle sizes and loading capacity were investigated, and the release properties were assessed in vitro. The hypoglycemic effect was investigated by monitoring the plasma glucose level of the alloxan-induced diabetic rats after oral administration.

RESULTS

All the MPs with three sizes formulated were in the desired size range, and the loading capacity was 15.3 %+/-1.7 % (120 nm), 32.4 %+/-2.4 % (350 nm), and 53.3 %+/-2.7 % (1000 nm) respectively. The particle size also had an influence on the release property of the MPs. Half an hour later, 25 %+/-4 % (120 nm), 18.3 %+/-2.4 % (350 nm), and 8.6 %+/-1.3 % (1000 nm) of insulin were released. MP with different sizes had various degree of hypoglycemic effects after 10 h (P<0.05 vs control insulin solution). The plasma glucose level of 350 nm size particles remarkably decreased 15 h later (P<0.05 vs 120 nm) or 35 h later (P<0.01 vs others). The relative pharmacological availability was 10.2 %+/-0.5 % (120 nm), 14.9 %+/-1.3 % (350 nm), and 7.3 %+/-0.8 % (1000 nm) respectively. Particles of 350 nm showed a comparatively higher availability (P<0.05).

CONCLUSION

Adhesive CS-MP were helpful in increasing the relative pharmacological bioavailability of insulin, and a distinct advantage of proper particle size helped to increase the drug effects.

Authors+Show Affiliations

Department of Pharmacy, Shenyang Pharmaceutical University, Shenyang, 110016, China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

12421485

Citation

Pan, Yan, et al. "Relationship Between Drug Effects and Particle Size of Insulin-loaded Bioadhesive Microspheres." Acta Pharmacologica Sinica, vol. 23, no. 11, 2002, pp. 1051-6.
Pan Y, Zheng JM, Zhao HY, et al. Relationship between drug effects and particle size of insulin-loaded bioadhesive microspheres. Acta Pharmacol Sin. 2002;23(11):1051-6.
Pan, Y., Zheng, J. M., Zhao, H. Y., Li, Y. J., Xu, H., & Wei, G. (2002). Relationship between drug effects and particle size of insulin-loaded bioadhesive microspheres. Acta Pharmacologica Sinica, 23(11), 1051-6.
Pan Y, et al. Relationship Between Drug Effects and Particle Size of Insulin-loaded Bioadhesive Microspheres. Acta Pharmacol Sin. 2002;23(11):1051-6. PubMed PMID: 12421485.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Relationship between drug effects and particle size of insulin-loaded bioadhesive microspheres. AU - Pan,Yan, AU - Zheng,Jun-Min, AU - Zhao,Hui-Ying, AU - Li,Ying-Jian, AU - Xu,Hui, AU - Wei,Gang, PY - 2002/11/8/pubmed PY - 2004/8/3/medline PY - 2002/11/8/entrez SP - 1051 EP - 6 JF - Acta pharmacologica Sinica JO - Acta Pharmacol Sin VL - 23 IS - 11 N2 - AIM: To formulate and characterize insulin-loaded adhesive microspheres (MP) and evaluate drug effects of MP with various sizes, 120, 350, and 1000 nm in diameter, in the alloxan-induced diabetic rats. METHODS: Insulin-loaded MP were formulated by an ionotropic gelation procedure. Particle size distributions were determined by photon correlation spectroscopy and optical microscopy. The factors that influenced the particle sizes and loading capacity were investigated, and the release properties were assessed in vitro. The hypoglycemic effect was investigated by monitoring the plasma glucose level of the alloxan-induced diabetic rats after oral administration. RESULTS: All the MPs with three sizes formulated were in the desired size range, and the loading capacity was 15.3 %+/-1.7 % (120 nm), 32.4 %+/-2.4 % (350 nm), and 53.3 %+/-2.7 % (1000 nm) respectively. The particle size also had an influence on the release property of the MPs. Half an hour later, 25 %+/-4 % (120 nm), 18.3 %+/-2.4 % (350 nm), and 8.6 %+/-1.3 % (1000 nm) of insulin were released. MP with different sizes had various degree of hypoglycemic effects after 10 h (P<0.05 vs control insulin solution). The plasma glucose level of 350 nm size particles remarkably decreased 15 h later (P<0.05 vs 120 nm) or 35 h later (P<0.01 vs others). The relative pharmacological availability was 10.2 %+/-0.5 % (120 nm), 14.9 %+/-1.3 % (350 nm), and 7.3 %+/-0.8 % (1000 nm) respectively. Particles of 350 nm showed a comparatively higher availability (P<0.05). CONCLUSION: Adhesive CS-MP were helpful in increasing the relative pharmacological bioavailability of insulin, and a distinct advantage of proper particle size helped to increase the drug effects. SN - 1671-4083 UR - https://www.unboundmedicine.com/medline/citation/12421485/Relationship_between_drug_effects_and_particle_size_of_insulin_loaded_bioadhesive_microspheres_ L2 - http://www.chinaphar.com/1671-4083/23/1051.pdf DB - PRIME DP - Unbound Medicine ER -