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1.
Int J Biol Macromol ; 224: 223-232, 2023 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-36265543

RESUMO

Scaffold development is a nascent field in drug development. The scaffolds mimic the innate microenvironment of the body. The goal of this study was to formulate a biocompatible and biodegradable scaffold, loaded with an analgesic drug, aceclofenac (Ace). The bioscaffold is aimed to have optimum mechanical strength and rheology, with drug released in a sustained manner. It was prepared via chemical cross-linking method: a chitosan (CS) solution was prepared and loaded with Ace; gelatin (GEL) was added and the mixture was cross-linked to get a hydrogel. 20 formulations were prepared to optimize different parameters including the stirring speed, drug injection rate and crosslinker volume. The optimal formulation was selected based on the viscosity, drug solubility, homogeneity, porosity and swelling index. A very high porosity and swelling index were attained. In vitro release data showed sustained drug delivery, with effective release at physiological and slightly acidic pH. SEM analysis revealed a homogeneous microstructure with highly interconnected pores within an extended polymer matrix. FT-IR spectra confirmed the absence of polymer-drug interactions, XRD provided evidences for efficient drug entrapment within the scaffold. Rheological analysis corroborated the scaffold injectability. Mathematical models were applied to in-vitro data, and the best fit was attained with Korsmeyer-Peppas.


Assuntos
Quitosana , Quitosana/química , Gelatina/química , Espectroscopia de Infravermelho com Transformada de Fourier , Alicerces Teciduais/química , Porosidade , Polímeros , Engenharia Tecidual , Materiais Biocompatíveis/química
2.
Gels ; 8(11)2022 Nov 17.
Artigo em Inglês | MEDLINE | ID: mdl-36421568

RESUMO

Psoriasis is chronic autoimmune disease that affects 2-5% of the global population. Fluocinolone acetonide (FLU) and acitretin (ACT) are widely used antipsoriatic drugs that belong to BCS classes II and IV, respectively. FLU exhibits side effects, such as skin irritation and a burning sensation. ACT also shows adverse effects, such as gingivitis, teratogenic effects and xerophthalmia. In the present study, topical nanostructured lipid carriers (NLCs) were fabricated to reduce the side effects and enhance the therapeutic efficacy. FLU-ACT-coloaded NLCs were prepared by the modified microemulsion method and optimized by the Box-Behnken model of Design Expert® version 12. The optimization was based on the particle size (PS), zeta potential (ZP) and percentage of encapsulation efficiency (%EE). The physicochemical analyses were performed by TEM, FTIR, XRD and DSC to assess the morphology, chemical interactions between excipients, crystallinity and thermal behavior of the optimized FLU-ACT-coloaded NLCs. The FLU-ACT-coloaded NLCs were successfully loaded into gel and characterized appropriately. The dialysis bag method and Franz diffusion cells were used for the in vitro release and ex vivo permeation studies, respectively. The optimized FLU-ACT-coloaded NLCs had the desired particle size of 288.2 ± 2.3 nm, ZP of -34.2 ± 1.0 mV and %EE values of 81.6 ± 1.1% for ACT and 75 ± 1.3% for FLU. The TEM results confirmed the spherical morphology, while the FTIR results showed the absence of chemical interactions of any type among the ingredients of the FLU-ACT-coloaded NLCs. The XRD and DSC analyses confirmed the amorphous nature and thermal behavior. The in vitro study showed the sustained release of the FLU and ACT from the optimized FLU-ACT-coloaded NLCs and FLU-ACT-coloaded NLC gel compared with the FLU-ACT suspension and conventional gel. The ex vivo study confirmed the minimal permeation of both drugs from the FLU-ACT-coloaded NLC gel.

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