Objectives: This project aimed at the formulation of dual drug entrapped liposomes held as freeze-dried intravaginal rod insert (IVR), to be administered by vaginal route for uterine targeting.
Methods: Liposomes were formulated by dehydration-rehydration method using 3 : 1 molar ratio of1,2-distearoyl-sn-glycero-3-phosphocholine : Cholesterol. Characterization was done for vesicle size, zeta potential, entrapment efficiency, surface morphology and % loading.
Key Findings: Spherical and discrete vesicles of size 354 nm were observed in transmission electron microscopy (TEM) image. The entrapment efficiency of 90.91% and 74.3% w/w was obtained for Raloxifene Hydrochloride (RLX) and Leuprolide acetate (LA) respectively. Drug release was sustained for 6 days. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay results showed that dual drug entrapped liposomal formulation show significant cytotoxicity, as also confirmed by higher apoptosis in cell cycle analysis and apoptosis studies (FACS) analysis. Pharmacodynamic studies in New Zealand white female rabbits revealed that intravaginal administration of RLX-LA entrapped liposomal formulation shows considerable fibroid regression.
Conclusions: Uterine targeting of liposomal RLX-LA suggests its potential to solve the limitations of the presently available therapeutic options.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1093/jpp/rgab003 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Chitosan-based sponges containing clotrimazole for the topical management of vulvovaginal candidiasis.
Int J Pharm
November 2023
i3S - Instituto de Investigação e Inovação em Saúde, Universidade do Porto, Rua Alfredo Allen 208, 4200-135 Porto, Portugal; INEB - Instituto de Engenharia Biomédica, Universidade do Porto, Rua Alfredo Allen 208, 4200-135 Porto, Portugal; IUCS - Instituto Universitário de Ciências da Saúde, CESPU, Rua Central de Gandra 1317, 4585-116 Gandra, Portugal. Electronic address:
Vulvovaginal candidiasis (VVC) persists as a worrying women's healthcare issue, often relying on suboptimal therapeutics. Novel intravaginal dosage forms focusing on improving patient acceptability and featuring improved biopharmaceutical properties could be interesting alternatives to available antifungal products. Different formulations of sponges based on chitosan (Ch), with or without crosslinking and co-formulated with poly(N-vinylcaprolactam) (PNVCL), were produced for the topical administration of clotrimazole (CTZ) and further tested for physicochemical properties, drug release, cytotoxicity and antifungal activity.
View Article and Find Full Text PDFIntravaginal electrical stimulation associated with pelvic floor muscle training for women with stress urinary incontinence: study protocol for a randomized controlled trial with economic evaluation.
Trials
November 2021
Women's Health Research Laboratory, Physical Therapy Post-Graduate Program, Federal University of São Carlos, Rod. Washington Luis, km 235, CEP, São Carlos, SP, 13565-905, Brazil.
Introduction: Pelvic floor muscle training (PFMT) exercises and neuromuscular electrical stimulation (NMES) are described as conservative interventions to prevent or treat female stress urinary incontinence (SUI). However, it has not been described yet the effect of PFMT associated to intravaginal NMES which evaluated the cost-effectiveness and cost-utility of treating.
Aims: To evaluate the effects of intravaginal NMES associated with the PFMT protocol on urinary loss and quality of life in women with SUI and to evaluate the cost-effectiveness and cost-utility and pelvic floor muscle in women with SUI.
Antral follicle count, oocyte production and embryonic developmental competence of senescent Nellore (Bos indicus) cows.
Theriogenology
October 2021
Division of Reproduction, Department of Clinical Sciences, SLU, Uppsala, Sweden.
Information on the follicular population and oocyte quality of cows in the final period of reproductive life is scarce. The present study aimed to compare the antral follicle count (AFC), oocyte production and embryonic developmental competence of young versus long-lived and senescent Bos indicus beef cows. Nellore cows (Bos indicus) were classified into three groups according to age: young (4-9 years, n = 10), long-lived (14-17 years, n = 10) and senescent (17-23 years, n = 10).
View Article and Find Full Text PDFDevelopment of intravaginal rod insert bearing liposomal raloxifene hydrochloride and Leuprolide acetate as a potential carrier for uterine targeting.
J Pharm Pharmacol
March 2021
Shri G.H. Patel Pharmacy Building, Centre for Postgraduate Studies in Pharmacy, TIFAC Core in NDDS, Donor's Plaza, Fatehgunj, Vadodara, India.
Objectives: This project aimed at the formulation of dual drug entrapped liposomes held as freeze-dried intravaginal rod insert (IVR), to be administered by vaginal route for uterine targeting.
Methods: Liposomes were formulated by dehydration-rehydration method using 3 : 1 molar ratio of1,2-distearoyl-sn-glycero-3-phosphocholine : Cholesterol. Characterization was done for vesicle size, zeta potential, entrapment efficiency, surface morphology and % loading.
In vitro characteristics of intravaginal Lactobacilli; why is L. iners detected in abnormal vaginal microbial flora?
Arch Gynecol Obstet
September 2020
Department of Microbiology, University of Occupational and Environmental Health, Kitakyushu, Japan.
Purpose: Our purpose is to investigate the reasons why Lactobacillus iners is detected in abnormal vaginal microbial flora.
Methods: In this study, in vitro characteristics of four type strains (L. crispatus, L.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!