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Progesterone-loaded chitosan microspheres: a long acting biodegradable controlled delivery system.
J Control Release 1998; 52(1-2):17-24JC

Abstract

Smooth, highly spherical, crosslinked chitosan microspheres in the size range of 45-300 microns loaded with progesterone were prepared by glutaraldehyde crosslinking of an aqueous acetic acid dispersion of chitosan containing progesterone in a non-aqueous dispersion medium consisting of liquid paraffin and petroleum ether stabilized using sorbitan sesquioleate. In vitro release of the drug into phosphate buffer at 37 degrees C was determined as a function of crosslinking density of the microspheres and particle size. The extent of drug release had a remarkable dependence on the crosslinking density of the microspheres, the highly crosslinked spheres releasing only around 35% of the incorporated steroid in 40 days compared to 70% from spheres lightly crosslinked. Determination of the in vivo bioavailability of the steroid from microsphere formulation by intramuscular injection in rabbits showed that a plasma concentration of 1 to 2 ng/ml was maintained up to 5 months without a high 'burst effect'. Data obtained suggest that the crosslinked chitosan microspheres would be an interesting system for long term delivery of steroids.

Authors+Show Affiliations

Division of Polymer Chemistry, Sree Chitra Tirunal Institute for Medical Sciences and Technology, Trivandrum, India.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

9685932

Citation

Jameela, S R., et al. "Progesterone-loaded Chitosan Microspheres: a Long Acting Biodegradable Controlled Delivery System." Journal of Controlled Release : Official Journal of the Controlled Release Society, vol. 52, no. 1-2, 1998, pp. 17-24.
Jameela SR, Kumary TV, Lal AV, et al. Progesterone-loaded chitosan microspheres: a long acting biodegradable controlled delivery system. J Control Release. 1998;52(1-2):17-24.
Jameela, S. R., Kumary, T. V., Lal, A. V., & Jayakrishnan, A. (1998). Progesterone-loaded chitosan microspheres: a long acting biodegradable controlled delivery system. Journal of Controlled Release : Official Journal of the Controlled Release Society, 52(1-2), pp. 17-24.
Jameela SR, et al. Progesterone-loaded Chitosan Microspheres: a Long Acting Biodegradable Controlled Delivery System. J Control Release. 1998 Mar 2;52(1-2):17-24. PubMed PMID: 9685932.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Progesterone-loaded chitosan microspheres: a long acting biodegradable controlled delivery system. AU - Jameela,S R, AU - Kumary,T V, AU - Lal,A V, AU - Jayakrishnan,A, PY - 1998/8/1/pubmed PY - 1998/8/1/medline PY - 1998/8/1/entrez SP - 17 EP - 24 JF - Journal of controlled release : official journal of the Controlled Release Society JO - J Control Release VL - 52 IS - 1-2 N2 - Smooth, highly spherical, crosslinked chitosan microspheres in the size range of 45-300 microns loaded with progesterone were prepared by glutaraldehyde crosslinking of an aqueous acetic acid dispersion of chitosan containing progesterone in a non-aqueous dispersion medium consisting of liquid paraffin and petroleum ether stabilized using sorbitan sesquioleate. In vitro release of the drug into phosphate buffer at 37 degrees C was determined as a function of crosslinking density of the microspheres and particle size. The extent of drug release had a remarkable dependence on the crosslinking density of the microspheres, the highly crosslinked spheres releasing only around 35% of the incorporated steroid in 40 days compared to 70% from spheres lightly crosslinked. Determination of the in vivo bioavailability of the steroid from microsphere formulation by intramuscular injection in rabbits showed that a plasma concentration of 1 to 2 ng/ml was maintained up to 5 months without a high 'burst effect'. Data obtained suggest that the crosslinked chitosan microspheres would be an interesting system for long term delivery of steroids. SN - 0168-3659 UR - https://www.unboundmedicine.com/medline/citation/9685932/Progesterone_loaded_chitosan_microspheres:_a_long_acting_biodegradable_controlled_delivery_system_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0168-3659(97)00187-9 DB - PRIME DP - Unbound Medicine ER -