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AuthorKoummich, Sarra Aicha
AuthorZoukh, Ikram Mustapha
AuthorGorachinov, Filip
AuthorGeskovski, Nikola
AuthorMakreski, Petre
AuthorDodov, Marija Glavas
AuthorGoracinova, Katerina
Available date2023-03-29T08:11:15Z
Publication Date2022-06-01
Publication NameDrug Delivery and Translational Research
Identifierhttp://dx.doi.org/10.1007/s13346-021-01030-4
CitationKoummich, S.A., Zoukh, I.M., Gorachinov, F. et al. Design of ophthalmic micelles loaded with diclofenac sodium: effect of chitosan and temperature on the block-copolymer micellization behaviour. Drug Deliv. and Transl. Res. 12, 1488–1507 (2022). https://doi.org/10.1007/s13346-021-01030-4
ISSN2190393X
URIhttps://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85110780455&origin=inward
URIhttp://hdl.handle.net/10576/41413
AbstractDiclofenac sodium 0.1% is a commonly used NSAID with well-documented clinical efficacy in reducing postoperative inflammation; however, its corneal tolerability and ophthalmic tissue bioavailability require further improvement. Advanced micellar delivery systems composed of block-copolymers and chitosan showing fine balance between the mucoadhesion and mucus permeation, capable to slip through the mucus barrier and adhere to the epithelial ocular surface, may be used to tackle both challenges. The aggregation behaviour of the block-copolymers in the presence of different additives will dramatically influence the quality attributes like particle size, particle size distribution, drug-polymer interaction, zeta potential, drug incorporation, important for the delicate balance among mucoadhesion and permeation, as well as safety and efficacy of the ophthalmic micelles. Therefore, quality by design approach and D-optimal experimental design model were used to create a pool of useful data for the influence of chitosan and the formulation factors on the block copolymer’s aggregation behaviour during the development and optimization of Diclofenac loaded Chitosan/Lutrol F127 or F68 micelles. Particle size, polydispersity index, dissolution rate, FTIR and DSC studies, NMR spectroscopy, cytotoxicity, mucoadhesivity, mucus permeation studies, and bioadhesivity were assessed as critical quality attributes. FTIR and DSC studies pointed to the chaotropic effect of chitosan during the micelle aggregation. Mainly, Pluronic F68 micellization behaviour was more dramatically affected by the presence of chitosan, and self-aggregation into larger micelles with high polydispersity index was favoured at higher chitosan concentration. The optimized formulation with highest potential for ophthalmic delivery of diclofenac sodium, good cytotoxicity profile, delicate balance of the mucoadhesivity, and mucus permeation was in the design space of Chitosan/Lutrol F127 micelles. Graphical abstract: [Figure not available: see fulltext.]
SponsorThe authors received financial support from the project Drug delivery systems for improved ophthalmic delivery, QUST-1-CPH2020-8, Qatar University.
Languageen
PublisherSpringer
SubjectD-optimal design model
Diclofenac sodium
DSC
FTIR
Mucus adhesion and permeation
NMR
Ophthalmic micelles
PEO-PPO-PEO
TitleDesign of ophthalmic micelles loaded with diclofenac sodium: effect of chitosan and temperature on the block-copolymer micellization behaviour
TypeArticle
Pagination1488-1507
Issue Number6
Volume Number12


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