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1.
Pharm Dev Technol ; 26(8): 852-866, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34193003

RESUMO

The goal of this study was to develop and examine the nanogel-based topical delivery system of mupirocin. Nanogels were prepared with chitosan and bovine serum albumin by ionic gelation and Carbopol 940 was added to improve the gelling/adhesive properties. Detailed characterization studies were performed and the cellular binding capacity of radiolabeled nanogels was investigated on CCD-1070Sk cell lines. Results indicate the successful formation of nanogels with particle size and zeta potential ranged between 341.920-603.320 nm and 13.120-24.300 mV, respectively. The mechanical and rheological studies proved pseudoplastic and strong elastic gel behavior (G' > G''). Mupirocin was successfully entrapped into nanogels with a ratio of more than 95% and the loaded drug was slowly released up to 93.89 ± 3.07% within 24 h. The ex vivo penetration and permeation percentages of mupirocin were very low (1.172 ± 0.202% and 0.161 ± 0.136%) indicating the suitability of nanogels for dermal use against superficial skin infections. The microbiological studies pointed out the effectiveness of nanogels against Staphylococcus aureus strains. Nanogels did not show toxicity signs and the cell binding capacity of radiolabeled formulations was found to be higher than [99mTc]NaTcO4 to CCD-1070Sk cell line. Overall, mupirocin nanogels might be considered as a potential and safe topical treatment option for bacterial skin infections.


Assuntos
Antibacterianos/administração & dosagem , Mupirocina/administração & dosagem , Nanogéis , Resinas Acrílicas/administração & dosagem , Resinas Acrílicas/química , Administração Cutânea , Antibacterianos/farmacocinética , Quitosana/administração & dosagem , Quitosana/química , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Humanos , Mupirocina/farmacocinética , Nanogéis/administração & dosagem , Nanogéis/química , Permeabilidade , Compostos Radiofarmacêuticos , Soroalbumina Bovina/administração & dosagem , Soroalbumina Bovina/química , Espectroscopia de Infravermelho com Transformada de Fourier , Staphylococcus aureus/efeitos dos fármacos
2.
Pharm Dev Technol ; 26(4): 431-443, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-33567946

RESUMO

This study aimed to present an effective formulation targeting oral ulcers that will remain in the application site for a longer period, reducing the frequency of administration. As a candidate formulation, usnic acid (UA) was loaded into the optimum nanogels. The characterization studies included physical, rheological, and bioadhesive properties as well as in vitro release and ex vivo studies. The rheological results revealed that the nanogels present pseudoplastic flow behavior. In vitro drug release showed a prolonged pattern. In further, the chosen UA nanogels showed very low percentages of penetration and permeation. F13, which showed the highest release, suitable bioadhesive properties (0.475 ± 0.033 N/cm2) and eligible particle size (250.22 ± 4.11 nm), PDI (0.089 ± 0.052), and zeta potential (20.56 ± 0.330 mV) values were chosen for in vivo experiments. The selected UA nanogels showed effective antimicrobial activity against Bacillus Cereus and great in vivo wound healing properties. The results indicated that suitable UA nanogels with desired properties could be prepared. The therapeutic potential of the nanogels for oral ulcers was assessed using an animal model and the histopathological findings suggested that the optimized formulation is a good choice for oral ulcer treatment. Nonetheless, further research is recommended to support its efficacy by applying pharmacodynamic and pharmacokinetic studies in human individuals.


Assuntos
Benzofuranos/administração & dosagem , Nanogéis , Úlceras Orais/tratamento farmacológico , Cicatrização/efeitos dos fármacos , Adesividade , Animais , Anti-Infecciosos/administração & dosagem , Anti-Infecciosos/farmacologia , Bacillus cereus/efeitos dos fármacos , Benzofuranos/farmacologia , Preparações de Ação Retardada , Modelos Animais de Doenças , Liberação Controlada de Fármacos , Masculino , Úlceras Orais/patologia , Tamanho da Partícula , Coelhos , Reologia
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