Mucoadhesive In Situ Gelling Liquid Crystalline Precursor System to Improve the Vaginal Administration of Drugs

Araújo, Patricia Rocha de; Calixto, Giovana Maria Fioramonti; Silva, Isabel Cristiane da; Zago, Lucas Henrique de Paula; Oshiro, João Augusto; Pavan, Fernando Rogério; Ribeiro, Anderson Orzari; Fontana, Carla Raquel; Chorilli, Marlus

doi:10.1208/s12249-019-1439-3

Cited by 28 publications

(13 citation statements)

References 51 publications

(48 reference statements)

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“…7a, b). The ability of the BS molecule to interact with mucin could imply an increase of the residence time at the application site and, consequently, a longer contact period with the vaginal mucosa [67]. Thus, the decrease of the leukocyte influx induced by C. albicans 2 strain when preventive and preventivesimultaneous protocols were applied could be explained by the interaction of BS with the mucin secreted by the vaginal epithelium, that could delay the contact of the fungus with the epithelium.…”

Section: Discussionmentioning

confidence: 99%

Biosurfactant from vaginal Lactobacillus crispatus BC1 as a promising agent to interfere with Candida adhesion

et al. 2020

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Background: Lactobacillus spp. dominating the vaginal microbiota of healthy women contribute to the prevention of urogenital and sexually transmitted infections. Their protective role in the vagina can be mediated by Lactobacillus cells themselves, metabolites or bacterial components, able to interfere with pathogen adhesion and infectivity. Vulvovaginal candidiasis (VVC) is a common genital infection, caused by the overgrowth of opportunistic Candida spp. including C. albicans, C. glabrata, C. krusei and C. tropicalis. Azole antifungal drugs are not always efficient in resolving VVC and preventing recurrent infections, thus alternative anti-Candida agents based on vaginal probiotics have gained more importance. The present work aims to chemically characterize the biosurfactant (BS) isolated from a vaginal Lactobacillus crispatus strain, L. crispatus BC1, and to investigate its safety and antiadhesive/antimicrobial activity against Candida spp., employing in vitro and in vivo assays. Results: BS isolated from vaginal L. crispatus BC1 was characterised as non-homogeneous lipopeptide molecules with a critical micellar concentration value of 2 mg/mL, and good emulsification and mucoadhesive properties. At 1.25 mg/mL, the BS was not cytotoxic and reduced Candida strains' ability to adhere to human cervical epithelial cells, mainly by exclusion mechanism. Moreover, intravaginal (i.va.) inoculation of BS in a murine experimental model was safe and did not perturb vaginal cytology, histology and cultivable vaginal microbiota. In the case of i.va. challenge of mice with C. albicans, BS was able to reduce leukocyte influx. Conclusions: These results indicate that BS from vaginal L. crispatus BC1 is able to interfere with Candida adhesion in vitro and in vivo, and suggest its potential as a preventive agent to reduce mucosal damage occasioned by Candida during VVC.

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Section: Discussionmentioning

confidence: 99%

Biosurfactant from vaginal Lactobacillus crispatus BC1 as a promising agent to interfere with Candida adhesion

et al. 2020

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“…Furthermore, lyotropic liquid crystals can also be usefully employed as mucoadhesive delivery systems, providing longer retention times at the application site. An example of the topical administration of liquid crystalline systems is found in the work of de Araújo et al on the vaginal administration of drugs [105]. This method may be also suitable to delivery oils and drugs at the same time.…”

Section: Future Perspectives and Conclusionmentioning

confidence: 99%

Ozonated Oils as Antimicrobial Systems in Topical Applications. Their Characterization, Current Applications, and Advances in Improved Delivery Techniques

Ugazio

Tullio²,

Binello

et al. 2020

Molecules

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The search for a wide spectrum of antimicrobial agents that can avoid resistance while maintaining reasonable side effects has led to ozonated oils experiencing an increase in scientific interest and clinical applications. The treatment of vegetable oils with ozone leads to the creation of a reservoir of ozone that slowly releases into the skin thanks to the fact that ozone can be held as ozonides of unsaturated fatty acids. Interest in the use of ozonated oils has meant that several ozonated-vegetable-oil-containing products have been commercialized as cosmetic and pharmaceutical agents, and in innovative textile products with antibacterial activity. New approaches to the delivery of ozonated oils have very recently appeared in an attempt to improve their characteristics and reduce drawbacks, such as an unpleasant odor, high viscosity and undesired effects on skin, including irritation and rashes. The present review focuses on the current status of delivery agents that use ozonated oils as antimicrobial agents in topical (dermal, skin, and soft tissues) treatments. Challenges and future opportunities for these delivery systems will also be discussed.

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“…Furthermore, the formation of a depot system with the mucoadhesive components which allowed a gradual release of HYP. Cytotoxicity assay performed on the liquid crystal precursor system incorporated with HYP demonstrated a decreased in cytotoxicity upon dilution with vaginal simulated fluid with cell viability above 80% [165]. Table 7 represents the discussed liquid crystalline precursor systems designed for vaginal drug delivery.…”

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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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Mucoadhesive In Situ Gelling Liquid Crystalline Precursor System to Improve the Vaginal Administration of Drugs

Cited by 28 publications

References 51 publications

Biosurfactant from vaginal Lactobacillus crispatus BC1 as a promising agent to interfere with Candida adhesion

Biosurfactant from vaginal Lactobacillus crispatus BC1 as a promising agent to interfere with Candida adhesion

Ozonated Oils as Antimicrobial Systems in Topical Applications. Their Characterization, Current Applications, and Advances in Improved Delivery Techniques

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

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