Tags

Type your tag names separated by a space and hit enter

Chemical cross-linking: A feasible approach to prolong doxylamine/pyridoxine release from spray-dried chitosan microspheres.
Eur J Pharm Sci. 2018 Oct 15; 123:387-394.EJ

Abstract

Spray-dried chitosan microparticles have been widely exploited as vehicles for mucosal drug delivery. Despite their advantages as pharmaceutical formulations, one of the major challenges is achieving sustained drug release, which would diminish toxicity and dosage frequency. The aim of this study was to formulate mucoadhesive glutaraldehyde cross-linked chitosan microparticles loaded with doxylamine succinate and pyridoxine hydrochloride as potential nasal drug delivery systems with sustained release. Microparticle models were formulated via spray-drying technique, using glutaraldehyde in different concentrations (0.1-1.0 mg/mL) as a cross-linking agent for chitosan. The obtained particles were with spherical shape, smooth surface and median diameter of 4 μm. The drug entrapment efficiency was high (80.47%-94.25%), indicating a tendency to decrease at higher glutaraldehyde concentrations. FTIR data demonstrated that there were no chemical interactions between glutaraldehyde and the drugs. The in vitro studies showed that the cross-linking process substantially limited particles swelling. The cross-linked particles exhibited sustained drug release characteristics at pH 6.8 over a period of 5 h with an initial burst-effect in the first 30 min. Drug release followed Korsmeyer-Peppas kinetics. Although a decrease of the particles mucoadhesive properties was observed after modification, all cross-linked formulations demonstrated high in vitro adsorption of mucin. The proposed models of mucoadhesive microsphere with sustained drug release are a perspective ground for further development of a novel delivery system for nasal administration of doxylamine and pyridoxine.

Authors+Show Affiliations

Department of Pharmaceutical Sciences, Faculty of Pharmacy, Medical University - Plovdiv, Bulgaria; High-technological Center for Emergency Medicine, Plovdiv, Bulgaria. Electronic address: plamen.katsarov@yahoo.com.Department of Pharmaceutical Sciences, Faculty of Pharmacy, Medical University - Plovdiv, Bulgaria; High-technological Center for Emergency Medicine, Plovdiv, Bulgaria. Electronic address: bisserapi@gbg.bg.Department of Chemistry and Biochemistry, Faculty of Pharmacy, Medical University - Plovdiv, Bulgaria.Department of Chemistry, Faculty of Pharmacy, Medical University - Sofia, Bulgaria.Department of Pharmaceutical Sciences, Faculty of Pharmacy, Medical University - Plovdiv, Bulgaria; High-technological Center for Emergency Medicine, Plovdiv, Bulgaria.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

30077710

Citation

Katsarov, Plamen, et al. "Chemical Cross-linking: a Feasible Approach to Prolong Doxylamine/pyridoxine Release From Spray-dried Chitosan Microspheres." European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, vol. 123, 2018, pp. 387-394.
Katsarov P, Pilicheva B, Uzunova Y, et al. Chemical cross-linking: A feasible approach to prolong doxylamine/pyridoxine release from spray-dried chitosan microspheres. Eur J Pharm Sci. 2018;123:387-394.
Katsarov, P., Pilicheva, B., Uzunova, Y., Gergov, G., & Kassarova, M. (2018). Chemical cross-linking: A feasible approach to prolong doxylamine/pyridoxine release from spray-dried chitosan microspheres. European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, 123, 387-394. https://doi.org/10.1016/j.ejps.2018.07.059
Katsarov P, et al. Chemical Cross-linking: a Feasible Approach to Prolong Doxylamine/pyridoxine Release From Spray-dried Chitosan Microspheres. Eur J Pharm Sci. 2018 Oct 15;123:387-394. PubMed PMID: 30077710.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Chemical cross-linking: A feasible approach to prolong doxylamine/pyridoxine release from spray-dried chitosan microspheres. AU - Katsarov,Plamen, AU - Pilicheva,Bissera, AU - Uzunova,Yordanka, AU - Gergov,Georgi, AU - Kassarova,Margarita, Y1 - 2018/08/02/ PY - 2018/03/20/received PY - 2018/07/25/revised PY - 2018/07/31/accepted PY - 2018/8/6/pubmed PY - 2019/1/15/medline PY - 2018/8/6/entrez KW - Chitosan microspheres KW - Doxylamine succinate KW - Glutaraldehyde cross-linking KW - Pyridoxine hydrochloride KW - Sustained release SP - 387 EP - 394 JF - European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences JO - Eur J Pharm Sci VL - 123 N2 - Spray-dried chitosan microparticles have been widely exploited as vehicles for mucosal drug delivery. Despite their advantages as pharmaceutical formulations, one of the major challenges is achieving sustained drug release, which would diminish toxicity and dosage frequency. The aim of this study was to formulate mucoadhesive glutaraldehyde cross-linked chitosan microparticles loaded with doxylamine succinate and pyridoxine hydrochloride as potential nasal drug delivery systems with sustained release. Microparticle models were formulated via spray-drying technique, using glutaraldehyde in different concentrations (0.1-1.0 mg/mL) as a cross-linking agent for chitosan. The obtained particles were with spherical shape, smooth surface and median diameter of 4 μm. The drug entrapment efficiency was high (80.47%-94.25%), indicating a tendency to decrease at higher glutaraldehyde concentrations. FTIR data demonstrated that there were no chemical interactions between glutaraldehyde and the drugs. The in vitro studies showed that the cross-linking process substantially limited particles swelling. The cross-linked particles exhibited sustained drug release characteristics at pH 6.8 over a period of 5 h with an initial burst-effect in the first 30 min. Drug release followed Korsmeyer-Peppas kinetics. Although a decrease of the particles mucoadhesive properties was observed after modification, all cross-linked formulations demonstrated high in vitro adsorption of mucin. The proposed models of mucoadhesive microsphere with sustained drug release are a perspective ground for further development of a novel delivery system for nasal administration of doxylamine and pyridoxine. SN - 1879-0720 UR - https://www.unboundmedicine.com/medline/citation/30077710/Chemical_cross_linking:_A_feasible_approach_to_prolong_doxylamine/pyridoxine_release_from_spray_dried_chitosan_microspheres_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0928-0987(18)30363-4 DB - PRIME DP - Unbound Medicine ER -