Development and in vitro evaluation of a novel contraceptive vaginal mucoadhesive propranolol hydrochloride film

Borumand, M.; Mortazavi, Seyed Alireza; Azar, Zahra Jafari; Rad, Rayehe Teymouri

doi:10.1016/s1773-2247(14)50130-x

Cited by 8 publications

(5 citation statements)

References 27 publications

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“…The receptor compartment was filled with 50 mL of phosphate buffer (pH 4.6) at 37 ± 1 °C. At a predetermined time, 1 mL of permeation media was withdrawn, and an equal volume of fresh media was added into the receiver compartment (Borumand et al., 2014 ). Samples were removed at 1, 2, 3, 4, 5 and 6 hrs then tested through a UV spectrophotometer at λ max 289 nm.…”

Section: Methodsmentioning

confidence: 99%

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Utilization of propranolol hydrochloride mucoadhesive invasomes as a locally acting contraceptive: in-vitro, ex-vivo, and in-vivo evaluation

Teaima¹,

Eltabeeb

El-Nabarawi³

et al. 2022

Drug Delivery

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It was found that propranolol hydrochloride (PNL), which is a beta-blocker used for hypertension treatment, has a potent spermicidal activity through local anesthetic activity or beta-blocking effect on sperm cells subsequently it could be used as a contraceptive remedy. This study aimed to entrap PNL into invasomes (INVs) and then formulate it as a locally acting contraceptive gel. PNL-loaded mucoadhesive INVs were prepared via the thin-film hydration technique. The D-optimal design was utilized to fabricate INVs employing lipid concentration (X 1 ), terpenes concentration (X 2 ), terpenes type (X 3 ), and chitosan concentration (X 4 ) as independent variables, while their impact was observed for entrapment efficiency percent (Y 1 ; EE%), particle size (Y 2 ; PS), zeta potential (Y 3 ; ZP), and amount of drug released after 6 h (Y 4 ; Q6h). Design Expert® was bestowed to nominate the desired formula. The selected INV was subjected to further studies and formulated into a mucoadhesive gel for ex-vivo and in-vivo investigations. The optimum INV showed a spherical shape with EE% of 65.01 ± 1.24%, PS of 243.75 ± 8.13 nm, PDI of 0.203 ± 0.01, ZP of 49.80 ± 0.42 mV, and Q6h of 53.16 ± 0.73%. Differential scanning calorimetry study asserted the capability of INVs to entrap PNL. Permeation studies confirmed the desired sustained effect of PNL-loaded INVs-gel compared to PNL-gel, INVs, and PNL solution. Sperm motility assay proved the potency of INVs-gel to inhibit sperm motility. Besides, the histopathological investigation verified the tolerability of the prepared INVs-gel. Taken together, the gained data justified the efficacy of PNL-loaded INVs-gel as a potential locally acting contraceptive.

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Section: Methodsmentioning

confidence: 99%

“…It is worth mentioning that PNL has been fabricated as spermicidal vaginal gel and vaginal film (Tasdighi et al., 2012 ; Borumand et al., 2014 ). According to our understanding, no paper has been published yet regarding loading PNL in nano-system that might sustain PNL spermicidal activity.…”

Section: Introductionmentioning

confidence: 99%

Utilization of propranolol hydrochloride mucoadhesive invasomes as a locally acting contraceptive: in-vitro, ex-vivo, and in-vivo evaluation

Teaima¹,

Eltabeeb

El-Nabarawi³

et al. 2022

Drug Delivery

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“…The polymeric films were prepared by solvent casting method [20]. For preparing blank fenugreek gum or aminated fenugreek gum films different concentrations of polymer (Table 1) were dissolved in distilled water on a magnetic stirrer (Remi equipments, Mumbai India).…”

Section: Preparation Of Film Formulationmentioning

confidence: 99%

Fenugreek gum derivatives with improved bioadhesion and controlled drug release: In vitro and in vivo characterization

Bassi

Kaur

2015

Journal of Drug Delivery Science and Technology

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“…Propranolol hydrochloride was developed as a hollow type suppository using different hydrophilic (Polyethylene glycol) and lipophilic (Witepsol H 37) bases and proved its efficacy in humans [27]. Moreover, propranolol hydrochloride was developed as a film by solvent casting method using Eudragit RS PO and HPMC 15000, which showed good mucoadhesive properties to vaginal walls [28]. In addition, propranolol hydrochloride was developed as a gel using sodium alginate at 6.5% w/w and proved its mucoadhesive property toward vaginal walls that might sustain its spermicidal activity [29].…”

Section: Pharmaceutical Dosage Forms Of Spermicidesmentioning

confidence: 99%

A Review on Advances in the Development of Spermicides Loaded Vaginal Drug Delivery System: State of the Art

Abdellatif

ELTABEEB²,

El-Nabarawi³

et al. 2022

Int J App Pharm

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Spermicides are bio-actives that might immobilize/kill the sperm in the vaginal tissues inducing contraception in the female genitalia. To inhibit sperm viability, the spermicidal drug might have to inhibit the penetration of sperm through the cervical tube of the uterus as well as attack sperm present in the vaginal walls. There are several classes of spermicidal agents, such as bactericides, sulfhydryl binding agents, natural compounds, and synthetic products. There are several classes of spermicidal agents that are widely reported. Spermicides could be available in different dosage forms as foams, gels, creams, films, sponges, and nanofibers. Available pharmaceutical spermicides showed particular importance for production on a large scale due to the continuous need for contraception. The upscaling of a process can be performed using a quality by design approach to ensure the achievement of the similarity principle between lab-scale and industrial scale. In addition, risk evaluation is performed to recognize all high-risk factors that can negatively affect the product to build the design space. Furthermore, the knowledge of the critical quality attributes enables the selection of the appropriate settings on a larger scale to establish a product of good quality and good packaging.

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Development and in vitro evaluation of a novel contraceptive vaginal mucoadhesive propranolol hydrochloride film

Cited by 8 publications

References 27 publications

Utilization of propranolol hydrochloride mucoadhesive invasomes as a locally acting contraceptive: in-vitro, ex-vivo, and in-vivo evaluation

Utilization of propranolol hydrochloride mucoadhesive invasomes as a locally acting contraceptive: in-vitro, ex-vivo, and in-vivo evaluation

Fenugreek gum derivatives with improved bioadhesion and controlled drug release: In vitro and in vivo characterization

A Review on Advances in the Development of Spermicides Loaded Vaginal Drug Delivery System: State of the Art

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