Formulation and development of vaginal films of poorly water soluble drug, metronidazole, using mixed solvency concept and their evaluations

Gahlot, Neha; Maheshwari, R. K.

doi:10.22270/jddt.v8i6.2085

Cited by 7 publications

(6 citation statements)

References 12 publications

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“…The advantages of gels and solid pharmaceutical dosage forms are amalgamated in the film dosage form where versatility of polymers provides the platform to develop films of desired characteristics [ 89 ]. Application of these films has been extended to evaluate against vaginal bacterial [ 90 ], viral [ 89 , 91 ] and fungal infections [ 92 ].…”

Section: Novel Approaches For Vaginal Drug Delivery For Microbial mentioning

confidence: 99%

Promising Drug Delivery Approaches to Treat Microbial Infections in the Vagina: A Recent Update

et al. 2020

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An optimal host–microbiota interaction in the human vagina governs the reproductive health status of a woman. The marked depletion in the beneficial Lactobacillus sp. increases the risk of infection with sexually transmitted pathogens, resulting in gynaecological issues. Vaginal infections that are becoming increasingly prevalent, especially among women of reproductive age, require an effective concentration of antimicrobial drugs at the infectious sites for complete disease eradication. Thus, topical treatment is recommended as it allows direct therapeutic action, reduced drug doses and side effects, and self-insertion. However, the alterations in the physiological conditions of the vagina affect the effectiveness of vaginal drug delivery considerably. Conventional vaginal dosage forms are often linked to low retention time in the vagina and discomfort which significantly reduces patient compliance. The lack of optimal prevention and treatment approaches have contributed to the unacceptably high rate of recurrence for vaginal diseases. To combat these limitations, several novel approaches including nano-systems, mucoadhesive polymeric systems, and stimuli-responsive systems have been developed in recent years. This review discusses and summarises the recent research progress of these novel approaches for vaginal drug delivery against various vaginal diseases. An overview of the concept and challenges of vaginal infections, anatomy and physiology of the vagina, and barriers to vaginal drug delivery are also addressed.

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Section: Novel Approaches For Vaginal Drug Delivery For Microbial mentioning

confidence: 99%

Promising Drug Delivery Approaches to Treat Microbial Infections in the Vagina: A Recent Update

et al. 2020

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“…The physiologically active natural polyphenol curcumin [1, 7-bis (4-hydroxy-3-methoxyphenyl)-1, 6-heptadiene-3, 5-Dione], also known as diferuloylmethane, is obtained from the rhizome of C. longa (Zingiberaceae family). [7] Mixed solvency concept [8][9][10][11] Any weak solvent (for a specific solute) can be made strong by choosing the right solubilizing agent. For instance, oil-soluble excipients such as polyvinylpyrrolidone (PVP), vanillin, butylated hydroxyanisole, butylated hydroxytoluene, propyl gallate, benzoic acid, methylparaben, and propylparaben, when used in the right concentrations, can improve the oil solubility.…”

Section: Medicinal Plantsmentioning

confidence: 99%

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2022

AJP

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Background: Since the beginning of time, humankind has employed herbal and medicinal plants as a source of food and medicine. Plant bioactive chemicals are currently of great research interest. However, extracting them as part of phytochemical and/or biological studies brings unique problems. Many techniques for the extraction of bioactive components have been devised by herbalists or scientists to indemnify the effectiveness and efficacy of the raw medications used to treat illness. The mode of extraction of active phytochemicals is receiving a lot of attention to reduce the costs associated with synthesis and separation. As a result, the extraction of active compounds from plants requires a proper procedure for extraction and techniques that provide extracts and fractions high in bioactive components, and also the solvents used in extraction do not harm humans as well as nature. As a result, they have a significant impact on yield, the nature of phytochemical content, and so on. Objectives: The purpose of this paper is to discuss and describe that solvents for extraction which shall be ecofriendly, safe, and also can be recovered easily by evaporation and preparation of the formulation using blends derived by idea of mixed solvency concept. Materials and Methods: Before extraction and formulation purity, tests were done on turmeric powder. Then, extraction was done using solvents prepared using mixed solvency such as camphor in ethanol (25% w/v and 50% w/v) and thymol in ethanol (25% w/v and 50% w/v). In addition, identification tests were done on the obtained extract. The comparative study was done on extraction yields, to establish a comparison between the yield obtained using conventional solvent and solvents prepared using the mixed solvency concept. In addition to that, a topical formulation was also prepared for the obtained extract. For formulation development solubility, studies of turmeric extract were done in various oils, ethanol, and blends (constituted in ethyl oleate with the combination of additives such as methyl paraben, propyl paraben, glyceryl monostearate, benzyl benzoate, and benzoic acid). The formulation so formed was a 0.9% curcumin oily solution and the evaluation tests such as viscosity, drug excipients interaction studies, and in vitro release studies were also done for the same. Results: In the extraction, it was discovered that adding camphor and thymol to ethanol improves the yield of turmeric extract, as compared to ethanol. Solubility studies were done for the preparation of topical solution and topical emulgel. The maximum solubility of turmeric extract was perceived in an oily blend which was formed by the purport of the mixed solvency concept). As a result, the oil base chosen for the formulation was an oily blend rather than a single oil or ethanol. In which the formulation produced positive outcomes. Evaluation studies such as freeze thaw, in vitro drug release, and antibacterial activity were performed for the formulation and it showed virtuous results.

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“…They are usually soft, flexible, preferably colorless and odorless, and disperse or dissolve upon coming in contact with vaginal fluids to adhere and retain in the vaginal mucosa for prolonged durations [264]. Several polymers have been investigated over the years for formulating vaginal films, the most commonly used ones being polyvinyl alcohol [265][266][267][268][269][270][271] and cellulose derivatives [272][273][274] or a combination of both [194,249,253,[275][276][277][278]. Other polymers have also been explored with or without the previously mentioned common options [223,263,279,280].…”

Section: Vaginal Filmsmentioning

confidence: 99%

“…[297]; deodorizing [298]; contraception, infections, itch relief, cleansing, and lubrication [299]; Lactobacillus for prevention of infections or restoration of flora [300]; pH regulation, drug and hormone delivery [301] and more. A notable mention is the application of the mixed solvency concept by Gahlot&Maheshwari for the preparation of metronidazole vaginal films for bacterial vaginosis (BV) [274]. They were able to solubilize the poorly water-soluble drug using a combination of aqueous solubilizers, niacinamide: sodium benzoate: urea: caffeine (15:10:10:5), which according to mixed solvency concept exhibit a synergistic solvent action in combination while also minimizing the amount of each individual excipient in the formulation [274].…”

Section: Vaginal Filmsmentioning

confidence: 99%

“…A notable mention is the application of the mixed solvency concept by Gahlot&Maheshwari for the preparation of metronidazole vaginal films for bacterial vaginosis (BV) [274]. They were able to solubilize the poorly water-soluble drug using a combination of aqueous solubilizers, niacinamide: sodium benzoate: urea: caffeine (15:10:10:5), which according to mixed solvency concept exhibit a synergistic solvent action in combination while also minimizing the amount of each individual excipient in the formulation [274]. In recent advancement of vaginal film formulations, Notario-Pérez et al developed "smart microbicide" films that are pH-sensitive and could change the release behavior of the drug to a rapid release in vaginal pH conditions after ejaculation (pH 7-8) from a sustained-release profile under typical vaginal conditions (pH 4-5) [302].…”

Section: Vaginal Filmsmentioning

confidence: 99%

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Recent Advances in Polymer-Based Vaginal Drug Delivery Systems

et al. 2021

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The vagina has been considered a potential drug administration route for centuries. Most of the currently marketed and investigated vaginal formulations are composed with the use of natural or synthetic polymers having different functions in the product. The vaginal route is usually investigated as an administration site for topically acting active ingredients; however, the anatomical and physiological features of the vagina make it suitable also for drug systemic absorption. In this review, the most important natural and synthetic polymers used in vaginal products are summarized and described, with special attention paid to the properties important in terms of vaginal application. Moreover, the current knowledge on the commonly applied and innovative dosage forms designed for vaginal administration was presented. The aim of this work was to highlight the most recent research directions and indicate challenges related to vaginal drug administrations. As revealed in the literature overview, intravaginal products still gain enormous scientific attention, and novel polymers and formulations are still explored. However, there are research areas that require more extensive studies in order to provide the safety of novel vaginal products.

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Formulation and development of vaginal films of poorly water soluble drug, metronidazole, using mixed solvency concept and their evaluations

Cited by 7 publications

References 12 publications

Promising Drug Delivery Approaches to Treat Microbial Infections in the Vagina: A Recent Update

Promising Drug Delivery Approaches to Treat Microbial Infections in the Vagina: A Recent Update

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Recent Advances in Polymer-Based Vaginal Drug Delivery Systems

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