Ajdary, M. and Keyhanfar, F. and Aflatoonian, R. and Amani, A. and Amjadi, F.S. and Zandieh, Z. and Mehdizadeh, M. (2020) Design and evaluation of a novel nanodrug delivery system for reducing the side effects of clomiphene citrate on endometrium. DARU, Journal of Pharmaceutical Sciences, 28 (2). pp. 423-432.
|
Text
Design and evaluation of a novel nanodrug delivery system for reducing the side effects of clomiphene citrate on endometrium.pdf Download (928kB) | Preview |
Abstract
Background: Stimulation of ovulation with clomiphene citrate can cause side effects on endometrial receptivity. Formulation with nano-size may be an alternative therapy for women with ovulatory disorders. In this study, we investigated sustained-release clomiphene citrate by using Phosal-based formulation (PBF) and evaluate its decreased side effect on the endometrial receptivity. Methods: In the in-vitro study, CC loaded PBF was analyzed using Zetasizer, Fourier-transform infrared spectroscopy (FTIR), and Transmission electron microscopy (TEM). In the in-vivo study, 24 female mice were randomly divided into three groups: CC (5 mg/kg), CC/PBF (5 mg/kg) and SS (1 ml) daily administered and injected with 5 IU HCG and mated after two days. At day 4.5, pregnant mice were euthanized and endometrial tissue was extracted for quantitative polymerase chain reaction (Q-PCR) analysis. Results: The optimized PBF contained Phosal 50PG/glycerol in a 2:8 ratios (w/w) and the particle size of optimum formulation was 67 ± 0.30551 nm and the release of CC from CC-containing PBF was slightly faster in the first 24 h; wherein, 29 of CC was released, and 76 of CC was released up to 120 h. The mRNA levels of leukemia inhibitory factor (LIF), leukemia inhibitory factor receptor alpha (LIFR), HOXA10, Heparin-binding epidermal growth factor (HB-EGF), and epidermal growth factor (EGF) were significantly upregulated and MUC1 and PGR mRNA levels were significantly downregulated in the CC-containing PBF-treated animals compared with only CC group (P < 0.05). Conclusion: Sustained release formulation of clomiphene citrate increased its targeting efficiency and improved the impact of the CC on implantation. Figure not available: see fulltext. © 2019, Springer Nature Switzerland AG.
| Item Type: | Article |
|---|---|
| Additional Information: | cited By 1 |
| Uncontrolled Keywords: | chorionic gonadotropin; clomifene citrate; epidermal growth factor; glycerol; heparin binding epidermal growth factor; homeobox protein Hox-A10; leukemia inhibitory factor; leukemia inhibitory factor receptor alpha; messenger RNA; mucin 1; progesterone receptor, animal cell; animal experiment; animal tissue; Article; controlled study; down regulation; drug delivery system; drug design; drug screening; EGF gene; endometrium; female; Fourier transform infrared spectroscopy; gene control; HB EGF gene; HOXA10 gene; in vitro study; in vivo study; LIF gene; LIFR gene; male; mouse; MUC1 gene; nanopharmaceutics; nonhuman; particle size; PGR gene; randomization; real time polymerase chain reaction; sustained release formulation; transmission electron microscopy; upregulation |
| Subjects: | QV Pharmacology |
| Depositing User: | eprints admin |
| Date Deposited: | 08 May 2021 06:58 |
| Last Modified: | 08 May 2021 06:58 |
| URI: | http://eprints.iums.ac.ir/id/eprint/33517 |
Actions (login required)
 |
View Item |
