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Development of a new delivery system consisting in "drug--in cyclodextrin--in nanostructured lipid carriers" for ketoprofen topical delivery.
Eur J Pharm Biopharm. 2012 Jan; 80(1):46-53.EJ

Abstract

A new delivery system based on drug cyclodextrin (Cd) complexation and loading into nanostructured lipid carriers (NLC) has been developed to improve ketoprofen therapeutic efficacy. The proposed strategy exploits both the solubilizing and stabilizing properties of Cds and the prolonged release, high tolerability and percutaneous absorption enhancer properties of NLC. Two different polymeric Cds, i.e. β-Cd-epichlorohydrin polymer (EPI-βCd) and carboxymethylathed-β-Cd-epichlorohydrin polymer (EPI-CMβCd) were tested and two different techniques to obtain solid ketoprofen-polymeric Cd complexes (i.e. co-grinding and co-lyophilization) were compared, to investigate the influence of the preparation method on the physicochemical properties of the end product. EPI-βCd was more effective than EPI-CMβCd in enhancing the solubility and dissolution properties of ketoprofen. Co-grinding in dry conditions was the best preparation technique of solid drug-Cd systems, allowing obtainment of homogeneous amorphous particles of nanometric range. NLC consisting in a mixture of Compritol® 888 ATO (glyceryl behenate) and Labrafac Lipophile were obtained by ultrasonication. Both empty and loaded NLC were suitably characterized for particle size, pH, entrapment efficiency and drug release behavior. The best (drug-Cd)-loaded NLC system, formulated into a xanthan hydrogel, exhibited drug permeation properties clearly better than those of the plain drug suspension or the plain drug-loaded NLC, in virtue of the simultaneous exploitation of the solubilizing effect of cyclodextrin and the penetration enhancer properties of NLC.

Authors+Show Affiliations

Department of Pharmaceutical Sciences, University of Florence, Florence, Italy. marzia.cirri@unifi.itNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

21839833

Citation

Cirri, M, et al. "Development of a New Delivery System Consisting in "drug--in Cyclodextrin--in Nanostructured Lipid Carriers" for Ketoprofen Topical Delivery." European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, vol. 80, no. 1, 2012, pp. 46-53.
Cirri M, Bragagni M, Mennini N, et al. Development of a new delivery system consisting in "drug--in cyclodextrin--in nanostructured lipid carriers" for ketoprofen topical delivery. Eur J Pharm Biopharm. 2012;80(1):46-53.
Cirri, M., Bragagni, M., Mennini, N., & Mura, P. (2012). Development of a new delivery system consisting in "drug--in cyclodextrin--in nanostructured lipid carriers" for ketoprofen topical delivery. European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, 80(1), 46-53. https://doi.org/10.1016/j.ejpb.2011.07.015
Cirri M, et al. Development of a New Delivery System Consisting in "drug--in Cyclodextrin--in Nanostructured Lipid Carriers" for Ketoprofen Topical Delivery. Eur J Pharm Biopharm. 2012;80(1):46-53. PubMed PMID: 21839833.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Development of a new delivery system consisting in "drug--in cyclodextrin--in nanostructured lipid carriers" for ketoprofen topical delivery. AU - Cirri,M, AU - Bragagni,M, AU - Mennini,N, AU - Mura,P, Y1 - 2011/08/04/ PY - 2011/04/29/received PY - 2011/07/22/revised PY - 2011/07/27/accepted PY - 2011/8/16/entrez PY - 2011/8/16/pubmed PY - 2012/7/3/medline SP - 46 EP - 53 JF - European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V JO - Eur J Pharm Biopharm VL - 80 IS - 1 N2 - A new delivery system based on drug cyclodextrin (Cd) complexation and loading into nanostructured lipid carriers (NLC) has been developed to improve ketoprofen therapeutic efficacy. The proposed strategy exploits both the solubilizing and stabilizing properties of Cds and the prolonged release, high tolerability and percutaneous absorption enhancer properties of NLC. Two different polymeric Cds, i.e. β-Cd-epichlorohydrin polymer (EPI-βCd) and carboxymethylathed-β-Cd-epichlorohydrin polymer (EPI-CMβCd) were tested and two different techniques to obtain solid ketoprofen-polymeric Cd complexes (i.e. co-grinding and co-lyophilization) were compared, to investigate the influence of the preparation method on the physicochemical properties of the end product. EPI-βCd was more effective than EPI-CMβCd in enhancing the solubility and dissolution properties of ketoprofen. Co-grinding in dry conditions was the best preparation technique of solid drug-Cd systems, allowing obtainment of homogeneous amorphous particles of nanometric range. NLC consisting in a mixture of Compritol® 888 ATO (glyceryl behenate) and Labrafac Lipophile were obtained by ultrasonication. Both empty and loaded NLC were suitably characterized for particle size, pH, entrapment efficiency and drug release behavior. The best (drug-Cd)-loaded NLC system, formulated into a xanthan hydrogel, exhibited drug permeation properties clearly better than those of the plain drug suspension or the plain drug-loaded NLC, in virtue of the simultaneous exploitation of the solubilizing effect of cyclodextrin and the penetration enhancer properties of NLC. SN - 1873-3441 UR - https://www.unboundmedicine.com/medline/citation/21839833/Development_of_a_new_delivery_system_consisting_in_"drug__in_cyclodextrin__in_nanostructured_lipid_carriers"_for_ketoprofen_topical_delivery_ DB - PRIME DP - Unbound Medicine ER -