RT Journal Article
T1 Supercritical fluid (SCF)-assisted preparation of cyclodextrin-based poly(pseudo)rotaxanes for transdermal purposes
A1 Cardoso, Gleidson
A1 García González, Carlos A.
A1 Santos Rosales, Víctor
A1 Taveira, Stephania Fleury
A1 Cunha-Filho, Marcilio
A1 Concheiro Nine, Ángel Joaquín
A1 Álvarez Lorenzo, Carmen
A1 Marreto, Ricardo Neves
K1 Cyclodextrin 
K1 Permeation enhancer 
K1 Solid dispersion 
K1 Microstructure
AB This study aims to investigate the effect of the preparation of solid dispersions using supercritical CO2 (scCO2) on the physicochemical properties and the performance of supramolecular gels based on polymer-cyclodextrin (CD) interactions (named poly(pseudo)rotaxanes, PPR) envisaging a transdermal administration. Solid dispersions containing Soluplus®, the antihypertensive drug carvedilol (CAR), and CD (αCD or HPβCD) were prepared and characterized by HPLC, XRPD, FTIR, and DSC. PPRs prepared from solid dispersions (SCF gels) and the corresponding physical mixtures (PM gels) were analyzed regarding rheology, morphology, in vitro drug diffusion, and ex vivo drug skin permeation. The application of scCO2 led to the loss of the crystalline lattice of CAR while preserving its chemical identity. On the contrary, αCD crystals were still present in the SCF solid dispersions. SCF gels were more uniform than their corresponding PM, and the supercritical treatment resulted in changes in the rheological behavior, reducing the viscosity. CAR in vitro diffusion was significantly higher (p < 0.05) for the αCD-based SCF gel than its corresponding PM gel. Drug skin permeation showed a significant increase in drug flux from CD-based SCF gels (containing αCD or HPβCD) compared to corresponding PM gels. Additionally, the pretreatment of the skin with αCD exhibited increased CAR permeation, suggesting an interaction between αCD and the skin membrane. Results evidenced that SCF processing decisively modified the properties of the supramolecular gels, particularly those prepared with αCD
PB Springer
SN 2190-393X
YR 2023
FD 2023-08-09
LK http://hdl.handle.net/10347/31202
UL http://hdl.handle.net/10347/31202
LA eng
NO Drug Deliv. and Transl. Res. (2023)
NO Open Access funding provided thanks to the CRUE-CSIC agreement with Springer Nature. This research was partially supported by the Brazilian agency Fundação de Apoio à Pesquisa do Estado de Goiás (FAPEG). The work was supported by MCIN/AEI/10.13039/501100011033 (PID 2020-113881RB-I00), Spain, Xunta de Galicia (ED431C 2020/17), and FEDER
DS Minerva
RD 24 abr 2026