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1.
Int J Pharm ; 608: 121114, 2021 Oct 25.
Artigo em Inglês | MEDLINE | ID: mdl-34543618

RESUMO

Lecithin-chitosan hybrid nanoparticles are emerging as a promising nanocarrier for topical drug delivery. They could achieve a maximized encapsulation of hydrophobic drugs due to the lipophilic nature of lecithin that comprises the core while enhancing retention in the upper skin layers using the positively charged polymeric coat of chitosan. The aim of this study is to incorporate tacrolimus; a hydrophobic anti-proliferative agent into lecithin chitosan hybrid nanoparticles by ethanolic injection technique using a suitable co-solvent to enhance encapsulation of the drug and allow a satisfactory release profile in the upper skin layers. Tacrolimus was successfully incorporated into the synthesized particles using olive oil and Tween 80 as co-solvents, with particle size (160.9 nm ± 15.9 and 118.7 nm ± 13.3, respectively) and EE (88.27% ± 4.3 and 66.72% ± 1.8, respectively). The in vitro drug release profile showed a faster release pattern for the Tween 80-containing particles over a 48-hour period (79.98% vs. 35.57%), hence, were selected for further investigation. The hybrid nanoparticles achieved significantly higher skin deposition than the marketed product (63.51% vs. 34.07%) through a 24-hour time interval, particularly, to the stratum corneum and epidermis skin layers. The in vivo results on IMQ-mouse models revealed superior anti-psoriatic efficacy of the synthesized nanoparticles in comparison to the marketed product in terms of visual observation of the skin condition, PASI score and histopathological examination of autopsy skin samples. Additionally, the in vivo drug deposition showed superior skin deposition of the nanoparticles compared to the marketed product (74.9% vs. 13.4%).


Assuntos
Quitosana , Nanopartículas , Psoríase , Animais , Quitosana/uso terapêutico , Portadores de Fármacos/uso terapêutico , Lecitinas , Camundongos , Tamanho da Partícula , Psoríase/tratamento farmacológico , Tacrolimo/uso terapêutico
2.
Carbohydr Polym ; 268: 118238, 2021 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-34127220

RESUMO

Tacrolimus is a natural macrolide that exhibits an anti-proliferative action by T-lymphocytic cells inhibition. Hence, it was tested as a potential topical treatment to improve and control psoriatic plaques. In this study, for the first time the lipophilic tacrolimus in chitosan nanoparticles was used to achieve the desired response and dermal retention of the drug using a modified ionic gelation technique. The hydrophobic drug, tacrolimus, was successfully encapsulated into the synthesized positively-charged particles (140.8 nm ± 50.0) and EE of (65.5% ± 1.3). Local skin deposition of the drug was significantly enhanced with 82.0% ± 0.6 of the drug retained in the skin compared to 34.0% ± 0.9 from tarolimus® ointment. An outstanding response to the prepared formula was the enhanced hair growth rate in the treated animals, which can be considered an excellent sign of the skin recovery from the induced psoriatic plaques after only three days of treatment.


Assuntos
Quitosana/química , Portadores de Fármacos/química , Imunossupressores/uso terapêutico , Nanopartículas/química , Psoríase/tratamento farmacológico , Tacrolimo/uso terapêutico , Administração Cutânea , Animais , Quitosana/administração & dosagem , Portadores de Fármacos/administração & dosagem , Liberação Controlada de Fármacos , Orelha/patologia , Imiquimode , Imunossupressores/administração & dosagem , Imunossupressores/química , Camundongos Endogâmicos C57BL , Nanopartículas/administração & dosagem , Tamanho da Partícula , Psoríase/induzido quimicamente , Psoríase/patologia , Ratos Sprague-Dawley , Pele/efeitos dos fármacos , Pele/patologia , Tacrolimo/administração & dosagem , Tacrolimo/química
3.
Drug Deliv ; 27(1): 662-680, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-32393082

RESUMO

Psoriasis is a dermatological chronic skin condition with underlying autoimmune etiology. It deeply affects patients' quality of life. Therefore, it was an interesting target for researchers throughout the past years. Conventionally, the treatment options include anti-inflammatory agents, immune suppressants, biologic treatment, and phototherapy. Nanotechnology offers promising characteristics that allow for tailoring a drug carrier to achieve dermal targeting, improved efficacy and minimize undesirable effects. Being the safest route, the first line of treatment and a targeted approach, we solely discussed the use of the topical route, combined with advanced drug delivery systems for the management of psoriasis in this article. Advanced systems include polymeric, metallic, lipidic and hybrid nanocarriers incorporating different active agents. All formerly mentioned types of drug delivery systems were investigated through the past decades for the purpose of topical application on psoriatic plaques. Scientists' efforts are promising to reach an optimized formula with a convenient dosage form to improve efficacy, safety, and compliance for the treatment of psoriasis. Accordingly, it will offer a better quality of life for patients.


Assuntos
Anti-Inflamatórios/administração & dosagem , Portadores de Fármacos/química , Nanopartículas/química , Psoríase/tratamento farmacológico , Pele/efeitos dos fármacos , Anti-Inflamatórios/farmacocinética , Anti-Inflamatórios/uso terapêutico , Humanos , Psoríase/imunologia , Pele/imunologia , Absorção Cutânea/efeitos dos fármacos
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