Nzekwe, ITAzodo, VIAgubata, CONaicker, BOkore, VEsimone, CO2015-09-092015-09-092015-02Nzekwe, I.T, Azodo, V.I, Agubata, C.O, Naicker, B, Okore, V and Esimone, C.O. 2015. Preliminary formulation and characterization of solid lipid nanoparticles containing chloroquine and a P-glycoprotein inhibitor: Influences of lipid-surfactant ratios. Journal of Chemical and Pharmaceutical Research, vol. 7(2), pp 932-9390975-7384http://jocpr.com/vol7-iss2-2015/JCPR-2015-7-2-932-939.pdfhttp://hdl.handle.net/10204/8129Copyright: 2015 Journal of Chemical and Pharmaceutical Research. Due to copyright restrictions, the attached PDF file only contains the abstract of the full text item. For access to the full text item, please consult the publisher's website. The definitive version of the work is published in the Journal of Chemical and Pharmaceutical Research, vol. 7(2), pp 932-939Chloroquine, a once useful therapy, currently faces problems of plasmodial resistance mediated through a number of mechanisms, such as P-glycoprotein (P-gp) mediated drug efflux, which makes attainment of adequate drug levels impossible. In this work, the inclusion of a P-gp inhibitor, chlorpheniramine, and chloroquine in a lipid-based nanoparticle carrier is proposed, with the aim of ensuring that adequate drug levels are attained, so as to overcome drug resistance. Methods: The nanoparticles were prepared by a simple method based on hot pre-emulsion. Physicochemical characterization involved determination of particle size and zeta potential, drug loading, entrapment efficiency and in vitro drug release. Results: The particle sizes varied with ratio of surfactant to lipid and also total excipients concentration. Drug encapsulation was higher than 50 % in all cases. Equal lipid-surfactant systems achieved higher loading than unequal ratios. The nanoparticle dispersion exhibited biphasic drug release in buffer. Conclusions: We conclude that, pending the outcome of in vivo trials and toxicological tests, co-formulation of choroquine and chlorpheniramine in lipid-based nanoparticles is feasible using a simple hot emulsion-dilution method.enChloroquineResistanceP-gpCo-formulationNanoparticleArticleNzekwe, I., Azodo, V., Agubata, C., Naicker, B., Okore, V., & Esimone, C. (2015). Preliminary formulation and characterization of solid lipid nanoparticles containing chloroquine and a P-glycoprotein inhibitor: Influences of lipid-surfactant ratios. http://hdl.handle.net/10204/8129Nzekwe, IT, VI Azodo, CO Agubata, B Naicker, V Okore, and CO Esimone "Preliminary formulation and characterization of solid lipid nanoparticles containing chloroquine and a P-glycoprotein inhibitor: Influences of lipid-surfactant ratios." (2015) http://hdl.handle.net/10204/8129Nzekwe I, Azodo V, Agubata C, Naicker B, Okore V, Esimone C. Preliminary formulation and characterization of solid lipid nanoparticles containing chloroquine and a P-glycoprotein inhibitor: Influences of lipid-surfactant ratios. 2015; http://hdl.handle.net/10204/8129.TY - Article AU - Nzekwe, IT AU - Azodo, VI AU - Agubata, CO AU - Naicker, B AU - Okore, V AU - Esimone, CO AB - Chloroquine, a once useful therapy, currently faces problems of plasmodial resistance mediated through a number of mechanisms, such as P-glycoprotein (P-gp) mediated drug efflux, which makes attainment of adequate drug levels impossible. In this work, the inclusion of a P-gp inhibitor, chlorpheniramine, and chloroquine in a lipid-based nanoparticle carrier is proposed, with the aim of ensuring that adequate drug levels are attained, so as to overcome drug resistance. Methods: The nanoparticles were prepared by a simple method based on hot pre-emulsion. Physicochemical characterization involved determination of particle size and zeta potential, drug loading, entrapment efficiency and in vitro drug release. Results: The particle sizes varied with ratio of surfactant to lipid and also total excipients concentration. Drug encapsulation was higher than 50 % in all cases. Equal lipid-surfactant systems achieved higher loading than unequal ratios. The nanoparticle dispersion exhibited biphasic drug release in buffer. Conclusions: We conclude that, pending the outcome of in vivo trials and toxicological tests, co-formulation of choroquine and chlorpheniramine in lipid-based nanoparticles is feasible using a simple hot emulsion-dilution method. DA - 2015-02 DB - ResearchSpace DP - CSIR KW - Chloroquine KW - Resistance KW - P-gp KW - Co-formulation KW - Nanoparticle LK - https://researchspace.csir.co.za PY - 2015 SM - 0975-7384 T1 - Preliminary formulation and characterization of solid lipid nanoparticles containing chloroquine and a P-glycoprotein inhibitor: Influences of lipid-surfactant ratios TI - Preliminary formulation and characterization of solid lipid nanoparticles containing chloroquine and a P-glycoprotein inhibitor: Influences of lipid-surfactant ratios UR - http://hdl.handle.net/10204/8129 ER -