Intravaginal Drug Delivery Systems to Treat the Genitourinary Syndrome of Menopause: Towards the Design of Safe and Efficacious Estrogen-loaded Prototypes

Abdelgader, Ahmed Abdalla Bakheit; Govender, Mershen; Kumar, Pradeep; Choonara, Yahya E.

doi:10.1016/j.xphs.2023.02.021

Cited by 3 publications

(4 citation statements)

References 128 publications

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“…In the study by Jinying et al, the release behavior of cupric ion and indomethacin from Cu-IUDs was investigated in SUF with a pH value adjusted around 6.8-7.4 [31]. The postmenopausal period is characterized by microbiota imbalance [6], potentially leading to an elevated pH in the upper genital tract [47]. In our study, a constant pH value of 7 was maintained throughout the experimentation.…”

Section: In Vitro Drug Releasementioning

confidence: 89%

“…Systemic products may additionally induce breast tenderness, vaginal bleeding, nausea, and modest weight gain with other adverse effects including headaches, back pain, abdominal discomfort, and vaginal yeast infections. Notably, unopposed estrogen, without progesterone, triggers uterine lining thickening, fostering endometrial hyperplasia, carcinoma, polyps, and fibroids, attributable to an estrogen-progesterone imbalance [2,3,5,6].…”

Section: Introductionmentioning

confidence: 99%

“…The utilization of progestogens, therefore, offers a means to counteract the effects of estrogen on the endometrial tissue during GSM treatment, thereby reducing the risk of endometrial hyperplasia [5,6]. The oral route is the most common method for administering progestogens in postmenopausal hormone therapy.…”

Section: Introductionmentioning

confidence: 99%

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A Novel Intrauterine Device for the Spatio-Temporal Release of Norethindrone Acetate as a Counter-Estrogenic Intervention in the Genitourinary Syndrome of Menopause

Abdelgader,

Govender,

Kumar

et al. 2024

Pharmaceutics

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The genitourinary syndrome of menopause (GSM) is a widely occurring condition affecting millions of women worldwide. The current treatment of GSM involves the use of orally or vaginally administered estrogens, often with the risk of endometrial hyperplasia. The utilization of progestogens offers a means to counteract the effects of estrogen on the endometrial tissue, decreasing unwanted side effects and improving therapeutic outcomes. In this study, a norethindrone acetate (NETA)-loaded, hollow, cylindrical, and sustained release platform has been designed, fabricated, and optimized for implantation in the uterine cavity as a counter-estrogenic intervention in the treatment of GSM. The developed system, which comprises ethyl cellulose (EC) and polycaprolactone (PCL), has been statistically optimized using a two-factor, two-level factorial design, with the mechanical properties, degradation, swelling, and in vitro drug release of NETA from the device evaluated. The morphological characteristics of the platform were further investigated through scanning electron microscopy in addition to cytocompatibility studies using NIH/3T3 cells. Results from the statistical design highlighted the platform with the highest NETA load and the EC-to-PCL ratio that exhibited favorable release and weight loss profiles. The drug release data for the optimal formulation were best fitted with the Peppas–Sahlin model, implicating both diffusion and polymer relaxation in the release mechanism, with cell viability results noting that the prepared platform demonstrated favorable cytocompatibility. The significant findings of this study firmly establish the developed platform as a promising candidate for the sustained release of NETA within the uterine cavity. This functionality serves as a counter-estrogenic intervention in the treatment of GSM, with the platform holding potential for further advanced biomedical applications.

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Section: In Vitro Drug Releasementioning

confidence: 89%

Section: Introductionmentioning

confidence: 99%

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A Novel Intrauterine Device for the Spatio-Temporal Release of Norethindrone Acetate as a Counter-Estrogenic Intervention in the Genitourinary Syndrome of Menopause

Abdelgader,

Govender,

Kumar

et al. 2024

Pharmaceutics

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“…Nucleic acid nanomaterials can be harnessed to selectively inhibit the regulatory factors involved in estrogen synthesis, effectively reducing its production and release. Multiple studies have substantiated the utility of nanocarriers for delivering anti-estrogen drugs [ [99] , [100] , [101] ]. Nanoparticles and nanocapsules, among other carriers, have found extensive application in anti-estrogen drug delivery.…”

Section: Application Of Nanotechnology In the Treatment Of Female Rep...mentioning

confidence: 99%

The utilization of nanotechnology in the female reproductive system and related disorders

Luo,

Jia,

Xing

et al. 2024

Heliyon

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Advanced drug delivery technologies for postmenopausal effects

Md,

Kotta

2024

Journal of Controlled Release

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Intravaginal Drug Delivery Systems to Treat the Genitourinary Syndrome of Menopause: Towards the Design of Safe and Efficacious Estrogen-loaded Prototypes

Cited by 3 publications

References 128 publications

A Novel Intrauterine Device for the Spatio-Temporal Release of Norethindrone Acetate as a Counter-Estrogenic Intervention in the Genitourinary Syndrome of Menopause

A Novel Intrauterine Device for the Spatio-Temporal Release of Norethindrone Acetate as a Counter-Estrogenic Intervention in the Genitourinary Syndrome of Menopause

The utilization of nanotechnology in the female reproductive system and related disorders

Advanced drug delivery technologies for postmenopausal effects

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