Systems Approach to Vaginal Delivery of Drugs II: In Situ Vaginal Absorption of Unbranched Aliphatic Alcohols

Hwang, Shyh‐Lung; Owada, Eiji; Yotsuyanagi, Toshihisa; Suhardja, L.; Ho, Norman F.H.; Flynn, Gordon L.; Higuchi, William I.

doi:10.1002/jps.2600651105

Cited by 45 publications

(8 citation statements)

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“…Bioadhesive polymers that have been used for intravaginal formulations include polycarbophil, hydroxypropylcellulose and polyacrylic acid (70). The first bioadhesive systems for vaginal drug delivery were in the form of tablets for the delivery of bleomycin, an anti-caner agent (70)(71)(72)(73)(74)(75). Attempts have also been made to delivery of microbicides using bioadhesive microparticulate vaginal systems (73)(74)(75)(76)(77)(78)99).…”

Section: Bioadhesive Intravaginal Systemsmentioning

confidence: 99%

A Review of Current Intravaginal Drug Delivery Approaches Employed for the Prophylaxis of HIV/AIDS and Prevention of Sexually Transmitted Infections

et al. 2008

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Abstract. The objective of this review is to describe the current status of several intravaginal anti-HIV microbicidal delivery systems these delivery systems and microbicidal compounds in the context of their stage within clinical trials and their potential cervicovaginal defence successes. The global Human Immuno-Deficiency Virus (HIV) pandemic continues to spread at a rate of more than 15,000 new infections daily and sexually transmitted infections (STIs) can predispose people to acquiring HIV infection. Male-to-female transmission is eight times more likely to occur than female-to-male transmission due to the anatomical structure of the vagina as well as socio-economic factors and the disempowerment of women that renders them unable to refuse unsafe sexual practices in some communities. The increased incidence of HIV in women has identified the urgent need for efficacious and safe intravaginal delivery of anti-HIV agents that can be used and controlled by women. To meet this challenge, several intravaginal anti-HIV microbicidal delivery systems are in the process of been developed. The outcomes of three main categories are discussed in this review: namely, dual-function polymeric systems, non-polymeric systems and nanotechnology-based systems. These delivery systems include formulations that modify the genital environment (e.g. polyacrylic acid gels and lactobacillus gels), surfactants (e.g. sodium lauryl sulfate), polyanionic therapeutic polymers (e.g. carageenan and carbomer/lactic acid gels), proteins (e.g. cyanovirin-N, monoclonal antibodies and thromspondin-1 peptides), protease inhibitors and other molecules (e.g. dendrimer based-gels and the molecular condom). Intravaginal microbicide delivery systems are providing a new option for preventing the transmission of STIs and HIV.

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Section: Bioadhesive Intravaginal Systemsmentioning

confidence: 99%

A Review of Current Intravaginal Drug Delivery Approaches Employed for the Prophylaxis of HIV/AIDS and Prevention of Sexually Transmitted Infections

et al. 2008

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“…Lipophilic drugs of low molecular weight are readily absorbed then high molecular weight hydrophilic or lipophilic drugs. As vaginal fluid have some water content so it favors absorption of drugs having certain solubility in water (Hwang et al, 1976). Drugs like peptide, weak electrolyte are frequently absorbed in their unionized form (Brannon-Peppas, 1993).…”

Section: Pesseries and Suppositoriesmentioning

confidence: 99%

Advanced topical drug delivery system for the management of vaginal candidiasis

et al. 2014

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Vaginal candidiasis or vulvovaginal candidiasis (VC) is a common mucosal infection of vagina, mainly caused by Candida species. The major symptoms of VC are dyspareunia, pruritis, itching, soreness, vagina as well as vulvar erythema and edema. Most common risk factors that lead to the imbalance in the vaginal micro biota are the use of antibiotics, pregnancy, diabetes mellitus, immuno suppression as in AIDS or HIV patients, frequent sexual intercourse, spermicide and intra-uterine devices and vaginal douching. Various anti-fungal drugs are available for effective treatment of VC. Different conventional vaginal formulations (creams, gels, suppositories, powder, ointment, etc.) for VC are available today but have limited efficacy because of lesser residence time on vaginal epithelium due to self-cleansing action of vagina. So to overcome this problem, an extended and intimate contact with vaginal mucosa is desired; which can be accomplished by utilizing mucoadhesive polymers. Mucoadhesive polymers have an excellent binding capacity to mucosal tissues for considerable period of time. This unique property of these polymers significantly enhances retention time of different formulations on mucosal tissues. Currently, various novel formulations such as liposomes, nano-and microparticles, micro-emulsions, bio-adhesive gel and tablets are used to control and treat VC. In this review, we focused on current status of vaginal candidiasis, conventional and nanotechnology inspired formulation approaches.

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“…Drugs intended for vaginal delivery should show some degree of solubility in water as vaginal fl uid contains a large amount of water. A proposed physical model for the uptake of drugs across the vaginal epithelium suggests that the epithelium could be regarded as an aqueous diffusion layer in series with a membrane consisting of aqueous pores and lipoidal pathways (Hwang and Owada 1976 ). The external cell layers and the basal cell layers of the vagina retain most of the enzyme activity (Woolfson and Malcolm 2000 ).…”

Section: Physiochemical Propertiesmentioning

confidence: 99%