Sildenafil vaginal suppositories: preparation, characterization,<i>in vitro</i>and<i>in vivo</i>evaluation

Shanmugam, Sumathi; Kim, Younghun; Park, Jeong-Hee; Im, Ho Taek; Sohn, Young-Taek; Kim, Kyeong Soo; Kim, Yong‐Il; Yong, Chul Soon; Kim, Jong Oh; Choi, Han‐Gon; Woo, Jong Soo

doi:10.3109/03639045.2013.788011

Cited by 13 publications

(11 citation statements)

References 68 publications

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“…The female rats were divided into four groups of 10 rats each. The first group was used as a control while other groups received SIL with a dose of 16.6 mg/kg of body weight of rats either oral solution through oral gavage, intravaginal CIS, or intravaginal FIS for 14 days (Shanmugam et al., 2014 ).…”

Section: Methodsmentioning

confidence: 99%

“…Thirty female mature Wistar rats weighing 200-250 g obtained from the experimental animal care center, Faculty of Veterinary Medicine, Beni-Suef University, were divided into three groups each comprising 10 rats. SIL was administered in a dose of 16.6 mg/kg (Shanmugam et al., 2014 ). Group 1 received oral SIL solution (2.25 mg/ml) in purified water, group 2 received the optimized intravaginal CIS and group 3 received intravaginal FIS.…”

Section: Methodsmentioning

confidence: 99%

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

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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Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

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

et al. 2018

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“…It was noticed that the suppositories prepared using the glycerol-gelatin base shows almost the same hardness, weight variation and disintegration time than the suppositories prepared using the Witepsol, grade H15. 14 The drug release obtained from the prepared FLZ vaginal suppositories is shown in Figure 2. It was observed that the glycero-gelatin suppositories (FVS 3) released full amount of drug within 60.0 min of dissolution.…”

Section: Conflict Of Interestmentioning

confidence: 99%

“…The final solution was filtered through membrane filter (pore size 0.45 µ) and the presence of drug was determined using UV visible spectrophotometer after suitable dilutions with acetate buffer at 261 nm wavelength. 8,28 Three suppositories were taken from each batch for this study.…”

Section: Content Uniformitymentioning

confidence: 99%

“…[10][11][12][13] Hence, the vaginal drug delivery of FLZ is considered to be effective for the treatment of VVC due to its targeting to the specific site and safety in pregnant women. 9,14 Few formulations of FLZ for the vaginal drug delivery have also been prepared to solve the above mentioned problems such as vaginal films 5,8 vaginal gels [15][16][17][18] vaginal tablets, 19 etc. But, the main problems with vaginal films and vaginal gels are their low drug content, wetting and leakage.…”

Section: Introductionmentioning

confidence: 99%

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Development of Fluconazole Suppositories for the Treatment of Candida Infection of Genitourinary Tract

Reddy¹,

Kumar

Pydi³

et al. 2018

IJPER

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Background: Vulvovaginal candidiasis is a communal problem in virtually all the women which is caused by Candida albicans. Objective: Aim of the present study was to prepare and characterize vaginal suppositories of fluconazole for the treatment of vulvovaginal candidiasis. Methods: Fluconazole suppositories were prepared using water soluble and fatty bases. Bases and their proportions used were selected in such a way that they have flexibility in storage conditions unlike conventional suppositories. Suppositories were prepared and examined for physical characteristics and in vitro release studies. Results: Present study showed ultimate results with respect to the physical characteristics of suppositories and in vitro drug release studies. In vitro drug release from the prepared suppositories was in the following order FVS 3 (100.00 ± 3.7% in 1.0 h) > FVS 1 (86.29 ± 4.9% in 12.0 h) > FVS 2 (80.47 ± 2.4% in 12.0 h) > FVS 5 (22.51 ± 0.42% in 24.0 h) > FVS 4 (18.09 ± 1.31% in 24.0 h). These drug release results are supported by the disintegration time of suppositories. Lesser the disintegration time faster the drug release. Conclusion: Study concludes that it may be fruitful to explore the in vivo activities of suppositories prepared with the combination of agar and HPMC as it showed around 80% drug release over 12.0 h. Represented combination may also be more effective for the treatment of vulvovaginal candidiasis.

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

Gomaa

Lila

Hasan

et al. 2018

European Journal of Pharmaceutical Sciences

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Sildenafil vaginal suppositories: preparation, characterization,in vitroandin vivoevaluation

Abstract: This study demonstrated enhanced sildenafil exposure in the uterus following IVG administration of SVS, which could be used to target the uterus for therapeutic benefits.

Cited by 13 publications

References 68 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

Development of Fluconazole Suppositories for the Treatment of Candida Infection of Genitourinary Tract

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

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