Please use this identifier to cite or link to this item: https://www.arca.fiocruz.br/handle/icict/61707

Type
Article
Copyright
Open access
Collections
Share

Statistics
Metadata
Show full item record

DEVELOPMENT, PHYSICOCHEMICAL EVALUATION, AND IN VIVO PERMEATION STUDIES OF TOPICAL FORMULATIONS CONTAINING 0.1% TACROLIMUS
Oliveira, Mariana Villas Bôas Vidal de et al. | Date Issued: 2023
Author
Oliveira, Mariana Villas Bôas Vidal de
Alves, Priscila Elias
Teixeira, Jessica
Monteiro, Mariana Sato de Souza de Bustamante
Moreira, Tailane Sant’Anna
Ricci Junior, Eduardo
Santos, Elisabete Pereira dos
Santos-Oliveira, Ralph
Marins, Rita de Cássia Elias Estrela
Freitas, Zaida Maria Faria de
Affilliation
Federal University of Rio de Janeiro. Health Sciences Center. Medicine Department. Pharmacy School. Rio de Janeiro, RJ, Brasil.
Federal University of Rio de Janeiro. Health Sciences Center. Medicine Department. Pharmacy School. Rio de Janeiro, RJ, Brasil.
Federal University of Rio de Janeiro. Health Sciences Center. Medicine Department. Pharmacy School. Rio de Janeiro, RJ, Brasil.
Federal University of Rio de Janeiro. Health Sciences Center. Medicine Department. Pharmacy School. Rio de Janeiro, RJ, Brasil.
Federal University of Rio de Janeiro. Health Sciences Center. Medicine Department. Pharmacy School. Rio de Janeiro, RJ, Brasil.
Federal University of Rio de Janeiro. Health Sciences Center. Medicine Department. Pharmacy School. Rio de Janeiro, RJ, Brasil.
Federal University of Rio de Janeiro. Health Sciences Center. Medicine Department. Pharmacy School. Rio de Janeiro, RJ, Brasil.
Nuclear Engineering Institute. Laboratory of Nanoradiopharmaceuticals and Synthesis of Novel Radiopharmaceuticals. Rio de Janeiro, RJ, Brazil / Rio de Janeiro State University. Laboratory of Nanoradiopharmacy and Radiopharmacy. Rio de Janeiro, RJ, Brazil.
Federal University of Rio de Janeiro. Health Sciences Center. Medicine Department. Pharmacy School. Rio de Janeiro, RJ, Brasil / Fundação Oswaldo Cruz. Instituto Nacional de Infectologia Evandro Chagas. Rio de Janeiro, RJ, Brasil.
Federal University of Rio de Janeiro. Health Sciences Center. Medicine Department. Pharmacy School. Rio de Janeiro, RJ, Brasil.
Abstract
The objective of this paper was to develop and evaluate two semi-solid pharmaceutical forms containing 0.1% tacrolimus: cream (CRT01) and gel (GLT01). For the evaluation of physicochemical stability, at times 0, 30, 60 and 90 days, at 23°C and at 40°C, High Performance Liquid Chromatography coupled with a Diode Array Detector (HPLC-DAD) was employed. This method was developed and validated for tacrolimus quantification. The occlusivity test and skin permeation assay were also performed, using an animal model (Wistar rats), and the CRT01 and GLT01 were compared to the 0.1% tacrolimus ointment (PFU01) obtained from the University Pharmacy, Federal University of Rio de Janeiro, Brazil. CRT01 and GLT01 presented a homogeneous aspect and consistency adequate for topical products, along with sensory characteristics above PFU01. They also presented adequate physicochemical stability for 90 days and a lower occlusive effect than PFU01 (p<0.05). CRT01 showed greater affinity for the skin when compared to PFU01 and GLT01, with low systemic absorption. The CRT01 semi solid formulation was considered the most adequate one to treat patients with atopic dermatitis or other dermatologic inflammatory diseases, promoting rational use of tacrolimus.
Keywords
Semi-solid pharmaceutical forms
Analytical methodology
Occlusivity test
In vivo permeation
Tacrolimus
 
Publisher
Universidade de São Paulo. Faculdade de Ciências Farmacêuticas
Citation
OLIVEIRA, Mariana Villas Bôas Vidal de et al. Development, physicochemical evaluation, and in vivo permeation studies of topical formulations containing 0.1% tacrolimus. Brazilian Journal of Pharmaceutical Sciences, n. 59, p. 1-14, 2023.
DOI
10.1590/s2175-97902023e201150
ISSN
2175-9790