In vivo evaluation of the vaginal distribution and retention of a multi-particulate pellet formulation (original) (raw)
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International Journal of Pharmacy and Pharmaceutical Sciences, 2022
Vaginal drug administration can improve prophylaxis and treatment of many conditions affecting the female reproductive tract, which includes fungal and bacterial infections, sexually transmitted diseases and cancer also. This is the best route for the administration of proteins, peptides, and also other therapeutic drugs like macro-molecules. For the administration of drugs like contraceptives, steroids, metronidazole, anti-retroviral, vaginal drug delivery is the most preferable route. However, achieving sufficient drug concentration in the vagina can be challenging because of its low permeability. The benefits of the vaginal drug delivery system are it increases the bioavailability, least systemic side effects; easiness of use and self-medication is possible. However vaginal drug delivery system is considered as a less effective route because of the unfortunate absorption of drugs across the vaginal epithelium. The traditional commercial preparations, such as creams, foams, gels, irrigations and tablets, are known to reside in the vaginal cavity for a relatively short period of time owing to the self-cleaning action of the vaginal tract and often require multiple daily doses to ensure the desired therapeutic effect. With the rapidly developing field of nanotechnology, the use of specifically designed carrier systems such as Nanoparticle-based drug delivery has been proven an excellent choice for vaginal application to overcome the challenges associated with the low permeability.
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The vagina has been studied as a favorable site for local and systemic delivery of drugs for female-related conditions. There are a large number of vaginal medications on the market and most of them require frequent application due to their short vaginal residence time. A prolonged vaginal residence time of formulations is therefore a key parameter for improved therapeutic efficacy. Promising approaches to prolong the residence time base on mucoadhesion, in- situ sol-gel transition and mechanical fixation. Mucoadhesive drug delivery systems can be tailored to adhere to the vaginal tissue. In-situ gelling systems offer the advantage of increased viscosity in vaginal cavity and consequently reduce outflow from the vagina. Mechanical fixation needs specially shaped drug delivery systems and reduce the frequency of administration significantly. Within this review an overview on these different strategies and systems is provided. Furthermore, the techniques to evaluate the potential of t...