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Formulation and evaluation of letrozole-loaded spray dried liposomes with PEs for topical application.
Maniyar, Mithun; Chakraborty, Avik; Kokare, Chandrakant.
Afiliação
  • Maniyar M; STES's Smt Kashibai Navale College of Pharmacy, Kondhwa (Bk), (Affiliated to Savitribai Phule Pune University), Pune, India.
  • Chakraborty A; SVERI's College of Pharmacy, Pandharpur, India.
  • Kokare C; Radiation Medicine Centre (RMC), Bhabha Atomic Research Centre (BARC), Mumbai, India.
J Liposome Res ; 30(3): 274-284, 2020 Sep.
Article em En | MEDLINE | ID: mdl-31223043
Letrozole (LET), an aromatase inhibitor widely used as a first-line drug for the estrogen-dependent breast cancer treatment in postmenopausal women. In this study, an attempt has been made to develop LET topical drug delivery which would be a more efficient system to treat elevated blood levels of estrogen found in breast cancer patients. The technique involves, encapsulation of the LET in phospholipids using spray dryer. The LET spray-dried powder (LT-SDP) powder was tested by Fourier transform infrared, X-RD, and differential scanning calorimetry. These studies confirm the entrapment efficiency (EE) of the system. The LT-SDP in the form dispersion was further evaluated. The confocal laser scanning microscopy (CLSM) showed spherical vesicles, the particle size, polydispersity index, and the EE was found to be 284.0 nm, 0.247, and 59.08%, respectively. LT-SDP dispersion was added into a cream base with peppermint and olive oil as natural penetration enhancers. Optimized formulation showed superior skin targeting in in vitro and in vivo studies. Cell proliferation assay and flow cytometry was carried out using human cancer cell line of breast MDA-MB-231 which showed superior anti-proliferative action and enhanced apoptosis activity of LT-SDP cream (43.9%) in comparison. The CLSM micrograph, skin irritation, and histopathology studies showed the penetration ability and inertness of the LT-SDP cream, respectively. In vivo bioavailability studies showed an almost four-fold increase in the plasma concentration (11.3 versus 4.2) while the mean residence time (81.11 versus 64.42 h) and half-life (51.01 versus 39.36 h) were reasonably higher than plain LET cream.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Letrozol Limite: Animals / Humans Idioma: En Revista: J Liposome Res Assunto da revista: BIOQUIMICA Ano de publicação: 2020 Tipo de documento: Article País de afiliação: Índia País de publicação: Reino Unido

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Letrozol Limite: Animals / Humans Idioma: En Revista: J Liposome Res Assunto da revista: BIOQUIMICA Ano de publicação: 2020 Tipo de documento: Article País de afiliação: Índia País de publicação: Reino Unido