Critical quality attributes, in vitro release and correlated in vitro skin permeation-in vivo tape stripping collective data for demonstrating therapeutic (non) equivalence of topical semisolids: A case study of "ready-to-use" vehicles
Authorized Users Only
Article (Published version)
MetadataShow full item record
This work aimed to prove the ability of "ready-to-use" topical vehicles based on alkyl polyglucoside-mixed emulsifier (with/without co-solvent modifications) to replace the conventionally used pharmacopoeial bases (e.g., non-ionic hydrophilic cream) in compounding practice. For this purpose, considering the regulatory efforts to establish alternative, scientifically valid methods for evaluating therapeutic equivalence of topical semisolids, we performed a comparative assessment of microstructure, selected critical quality attributes (CQAs) and in vitro/in vivo product performances, by utilizing aceclofenac as a model drug. The differences in composition between investigated samples have imposed remarkable variances in monitored CQAs (particularly in the amount of aceclofenac dissolved, rheological properties and water distribution mode), reflecting the distinct differences in microstructure formed, as partially observed by polarization microscopy and confocal Raman spectral imaging. Al...though not fully indicative of the in vivo performances, in vitro release data (vertical diffusion vs. immersion cells) proved the microstructure peculiarities, asserting the rheological properties as decisive factor for obtained liberation profiles. Contrary, in vitro permeation results obtained using pig ear epidermis correlated well with in vivo dermatopharmacokinetic data and distinguished unequivocally between tested formulations, emphasizing the importance of skin/vehicle interactions. In summary, suggested multi-faceted approach can provide adequate proof on topical semisolids therapeutic equivalence or lack thereof.
Keywords:Microstructure / Critical quality attributes / In vitro release / In vitro skin permeation / In vivo tape stripping / In vitro-in vivo correlation
Source:International Journal of Pharmaceutics, 2017, 528, 1-2, 253-267
- Elsevier Science BV, Amsterdam
- Development of micro- and nanosystems as carriers for drugs with anti-inflammatory effect and methods for their characterization (RS-34031)
- Federal Republic of Germany
Showing items related by title, author, creator and subject.
Role of metabolism in drug development: In vitro studies / Značaj izučavanja metabolizma u razvoju novih lekova - in vitro pristup Rakić-Ignjatović, Anita; Miljković, Branislava; Ilić, Marija; Pokrajac, Milena; Prostran, Milica (Savez farmaceutskih udruženja Srbije, Beograd, 2010)
Human skin equivalents produced by in vitro cells culture: Characteristics, quality requirements and application possibilities / Ekvivalenti humane kože dobijeni in vitro kulturom ćelija - karakteristike, zahtevi u pogledu kvaliteta i mogućnosti primene Savić, Snežana; Milić, Jela; Vuleta, Gordana (Savez farmaceutskih udruženja Srbije, Beograd, 2006)
Pharmacological in vitro screening of the central monoaminergic effects of Valeriana officinalis extracts / Farmakološki in vitro skrining centralnih monoaminoergičnih efekata ekstrakata Valeriana officinalis Tomić, Mirko D.; Kundaković, Marija J.; Petrović, Silvana (Unija bioloških naučnih društava Jugoslavije, Beograd, 2005)