Preparation and characterization of intravaginal vardenafil suppositories targeting a complementary treatment to boost in vitro fertilization process

Gomaa, Eman Zakaria; Lila, Amr S. Abu; Hasan, Azza A.; Ghazy, Fakhr-eldin S.

doi:10.1016/j.ejps.2017.09.044

“…Our findings of the CIS well comply with these previous results proposing the potential intervention of first uterine pass effect of SIL following intravaginal application. The counter-current transport from vaginal veins to the uterine artery is one of the suggested mechanisms which elucidates the preferable distribution to the uterus following intravaginal application (Taurin et al., 2017 ; Gomaa et al., 2018 ). Our study indicated that intravaginal administration of CIS for uterine SIL targeting was more beneficial than both intravaginal FIS and oral administration and could be considered as a promising approach where increased uterine exposure (as demonstrated in histopathological study) coupled with decreased systemic levels were attained.…”

Section: Methodsmentioning

confidence: 99%

Novel in situ gelling vaginal sponges of sildenafil citrate-based cubosomes for uterine targeting

Aboud

¹

,

Hassan

²

,

Ali

³

et al. 2018

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Sildenafil citrate (SIL), a type 5-specific phosphodiesterase inhibitor, demonstrates valuable results in the management of infertility in women; however, the absence of vaginal dosage form in addition to the associated oral adverse effects minimize its clinical performance. The present study is concerned with SIL uterine targeting following intravaginal administration via optimization of cubosomal in situ gelling sponges (CIS). An emulsification method was employed for preparation of cubosomal dispersions incorporating glyceryl monooleate as a lipid phase and poloxamer 407 as a surfactant with or without polyvinyl alcohol as a stabilizer. Cubosomes were estimated regarding entrapment efficiency (EE%), particle size, and in vitro drug release. Chitosan (2% w/w) was incorporated into the optimum formulation and then lyophilized into small sponges. For the CIS, in vivo histopathological and pharmacokinetic studies were conducted on female Wistar rats and compared with intravaginal free SIL sponges (FIS) and oral SIL solution. SIL-loaded cubosomes showed EE% ranging between 32.15 and 72.01%, particle size in the range of 150.81–446.02 nm and sustained drug release over 8 h. Histopathological study revealed a significant enlargement in endometrial thickness with congestion and dilatation of endometrial blood vessels in intravaginal CIS compared to intravaginal FIS and oral-treated groups. The pharmacokinetic study demonstrated higher AUC0–∞ and Cmax with oral administration compared to intravaginal CIS or intravaginal FIS indicating potential involvement of first uterine pass effect after intravaginal administration. Finally, intravaginal CIS could be considered as a promising platform for SIL uterine targeting with minimized systemic exposure and side effects.

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“…Twenty suppositories of each formulation were weighed to determine the average weight (n = 20). Not more than two suppositories varied from the average weight by more than 5%, and no suppository differed from the average weight by more than 10% [26].…”

Section: Preparation Of Suppositorymentioning

confidence: 88%

“…The resistance offered by the suppository to break or collapse is referred to as hardness [26]. The hardness test was done for ten suppositories using an Erweka hardness tester (Pharma Test, Germany) at room temperature (25 ± 0:5 °C).…”

Section: Hardness Testmentioning

confidence: 99%

An Efficient Herbal Approach for Treating Fungal Infection in Cervical Cancer Patients by Developing and Optimizing a Vaginal Suppository

Ghazwani

¹

,

Hani

²

,

Osmani

³

et al. 2021

International Journal of Polymer Science

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Aim. The study is aimed at developing curcumin suppositories as a promising approach for natural antifungal management of vaginal candidiasis in cervical cancer patients to eradicate side effects produced by current antifungal drugs. The objective of the study was to optimize the suppositories using optimal (custom) design employing Design-Expert 13 software to recognize the concentration of polyethylene glycols (PEG) and Poloxamer 407 and obtain a stable suppository. Methodology. Combinations of PEG 1500 (10%–40%), PEG 6000 (40%–60%), and Poloxamer 407 (5%–30%) were entered as factors, and the responses evaluated were hardness, deformation time, and % drug release. In addition, the formulation was also evaluated for visual examination, weight variation, pH determination, drug content, hardness test, disintegration time, melting zone, deformation time, in vitro drug release, antifungal activity, and stability tests. Results. Suppositories were devoid of holes and cracks, with a characteristic odor and a dark yellowish-orange color. All formulations passed the weight variation test. Formulations exhibited pH ranging from 5.5 to 6.5. Drug content was observed to be 98.65 ± 0.041 % – 99.85 ± 0.041 % . The hardness of the formulation was between 2.9 and 4.2 kg/cm2. The disintegration time ranged from 11 ± 0.052 min to 20 ± 0.011 min . The melting point was between 41 ± 0 . 31 ° C and 58 ± 0 . 62 ° C . Deformation time ranged from 10 ± 0.45 to 35 ± 0.52 min . Most of the formulations resulted in 90% of drug release at 40 min, and the zone of inhibition noted was 19.6 ± 0.4 mm . All the selected factors have a significant effect on the response chosen for the study. Conclusion. The optimized curcumin vaginal suppository formulation can be an efficient herbal treatment devoid of side effects to treat vaginal candidiasis in cervical cancer patients.

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“…Blood samples collected from sacrificed rats were left at room temperature for 30 min, then centrifuged at 5000 rpm at 4 °C for 15 min to obtain serum ( Gomaa et al, 2018 , Abu Lila et al, 2020 ). cGMP Direct Immunoassay Kit (Abcam, MA, USA) according to general principle of ELISA technique and the manufacturer's recommended instructions was used for quantitative measurement of cGMP ( Itoh et al 2004 ).…”

Section: Methodsmentioning

confidence: 99%

Vardenafil oral jellies as a potential approach for management of pediatric irritable bowel syndrome

Gomaa

¹

,

Ayoub

²

2021

Saudi Pharmaceutical Journal

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Preparation and characterization of intravaginal vardenafil suppositories targeting a complementary treatment to boost in vitro fertilization process

Cited by 16 publications

References 37 publications

Novel in situ gelling vaginal sponges of sildenafil citrate-based cubosomes for uterine targeting

Novel in situ gelling vaginal sponges of sildenafil citrate-based cubosomes for uterine targeting

An Efficient Herbal Approach for Treating Fungal Infection in Cervical Cancer Patients by Developing and Optimizing a Vaginal Suppository

Vardenafil oral jellies as a potential approach for management of pediatric irritable bowel syndrome

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