Formulation and evaluation of letrozole-loaded spray dried liposomes with PEs for topical application. (2nd July 2020)

• Record Type: Journal Article
• Authors: Maniyar, Mithun; Chakraborty, Avik; Kokare, Chandrakant
• Is Part Of: Journal of liposome research. Volume 30:Number 3(2020)
• Page Start: 274
• Page End: 284
• Publication Date: 2020-07-02
• Subjects: Liposomes -- zeta potential -- cell proliferation assay -- flow cytometry -- CLSM -- in vivo bioavailability studies; Liposomes -- Periodicals; Liposomes -- Periodicals; 575.57
• DOI: 10.1080/08982104.2019.1634723
• Languages: English
• ISSNs: 0898-2104

Abstract

Abstract: 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.