Title : Biopolymer-based vaginal drug delivery system
Abstract:
Infectious diseases of the female reproductive system (including bacterial vaginosis, candidiasis, viral infections, as well as vaginal dysbiosis) are one of the most common conditions that every woman faces at some point during her life.
Features of the vaginal anatomy, histological structure of the mucosa, biological properties of vaginal discharge, significantly limit the effectiveness of drugs used for vaginal administration based on traditional dosage forms (tablets, capsules, suppositories, ointments, gels and solutions). Limitations of solid forms are associated with a suboptimal dissolution profile in the vagina and surface distribution of the therapeutic agent. Due to the small volume of fluid in the vagina, solid forms cannot provide the necessary concentrations of administered active substances or bacteria uniformly over the entire surface of the vaginal mucosa. Gels and solutions are prone to leakage, requiring a horizontal position before and after administration, which reduces compliance with therapy, and, as a consequence, the effectiveness of therapy.
The aim of this study was to develop a cryostructured a solid dosage form for vaginal delivery of active ingredients based on the use of a biodegradable polysaccharide as a structural component, which has the following set of properties and characteristics that increase the effectiveness of therapy while ensuring ease of use of the device:
- In the initial state (before contact with water or an aqueous solution before inserting the device into the vagina), the device has a stable solid form, resembling a hygienic tampon, convenient for insertion into the vagina.
- Upon interaction with water or an aqueous solution, the device is effectively wetted, forming a three-dimensional hydrogel structure while retaining its shape up to 48 h, ensuring hygienic insertion of the device into the vaginal cavity using a suitable applicator device.
- Upon subsequent intravaginal mechanical action, the hydrogel disintegrates forming a gel-like mass that ensures the uniform distribution of the therapeutic agent in the vaginal cavity.
- The device is characterized by the necessary adhesion to the walls of the vaginal epithelium, providing sufficient exposure time to the therapeutic agent in the vaginal cavity.
- The device is characterized by structural strength in the initial state (before contact with water or an aqueous solution), and provides nutritional support for lactobacilli of the vaginal microflora after insertion of the device.
To date, the development of the first prototype of the therapeutic agent has been completed - A device that combines the properties of a pro - and prebiotic, allowing for the rapid and reliable restoration of vaginal normocenosis. In vitro studies have been conducted on a biopolymer matrix of biopolysaccharides with a probiotic included in its composition - the vaginal strain of L. Crispatus. The prebiotic activity of the matrix itself has been proven, the following have been studied: the survival and release of L. Crispatus from the product, the peroxidase activity of the product with L. Crispatus, the release of lactic acid, antagonistic activity against C. albicans, E. coli, G. Vaginalis, and the adhesive properties of the product.
Audience Take Away:
- This research could be used to expand for research, which looking for solution, how increase sufficient exposure time to the therapeutic agent in the vaginal cavity. The device in one of the embodiments may not contain active ingredients, i.e. may be an unfilled biopolymer matrix, which can also be used as a medical device. In another version of the invention, the device is a biopolymer matrix containing one or more active ingredients, wherein the active ingredients can be introduced into the matrix at the initial stage of producing the device: when mixing the matrix components with the active ingredients before freezing and freeze-drying, and at subsequent stages of production or use of the finished product.
- A practical solution to a problem. This research can be used as practical solution to include active substances, including biotechnological ones, the use of which is currently limited due to the lack of adequate delivery methods, insufficient exposure time during intravaginal administration, and the creation of new drugs for intravaginal treatment of gynecological diseases due to: The ability to control the time of matrix biodegradation up to 48 hours; the ability to work with thermolabile active substances; the ability to vary the form of a lyophilizate suppository for a specific nosology.
