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Cited by 155Advancements in Transdermal Drug DeliveryDrug Solubulity and Delivery SystemsAdvanced Drug Delivery Systems

Development of a new delivery system consisting in “drug–in cyclodextrin–in nanostructured lipid carriers” for ketoprofen topical delivery

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Cirri, M., Bragagni, M., Mennini, N., Mura, P.·2012·European Journal of Pharmaceutics and Biopharmaceutics
DOI 10.1016/j.ejpb.2011.07.015
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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.

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Authors
Cirri, M., Bragagni, M., Mennini, N., & Mura, P.
Affiliations
University of Florence (IT)
Corresponding author
Cirri, M.
ORCID
Venue
European Journal of Pharmaceutics and Biopharmaceutics
Publisher
Elsevier BV
Published
2012-01
Volume
80
Issue
1
Pages
46-53
ISSN
0939-6411 (ISSN-L)
DOI
10.1016/j.ejpb.2011.07.015
OpenAlex
W2002418262
Cited by
155
References
41
Citations by year
2026: 1 · 2025: 9 · 2024: 8 · 2023: 10 · 2022: 18 · 2021: 13 · 2020: 9 · 2019: 6 · 2018: 18 · 2017: 15 · 2016: 7 · 2015: 13 · 2014: 9 · 2013: 9 · 2012: 10
FWCI
5.49
Type
journal article
Language
en
Open access
Licence
Locations
  • European Journal of Pharmaceutics and Biopharmaceutics (publishedVersion)
  • PubMed (publishedVersion)
  • Florence Research (University of Florence) (submittedVersion, other-oa)
Funders
Ministero dell’Istruzione, dell’Università e della Ricerca
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
Keywords
ketoprofen, topical drug delivery, cyclodextrins, nanostructured lipid carriers, drug solubilization, co-grinding, Compritol 888 ATO, amorphous nanoparticles, drug release
MeSH terms
Administration, Topical, Chemistry, Pharmaceutical, Cyclodextrins, Delayed-Action Preparations, Drug Carriers, Drug Stability, Epichlorohydrin, Freeze Drying, Ketoprofen, Lipids, Particle Size, Permeability, Polymers, Polysaccharides, Bacterial, Solubility, Hydrogel, Polyethylene Glycol Dimethacrylate, beta-Cyclodextrins, Nanostructures

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