Water dispersible microbicidal cellulose acetate phthalate film

Abstract

Background: Cellulose acetate phthalate (CAP) has been used for several decades in the pharmaceutical industry for enteric film coating of oral tablets and capsules. Micronized CAP, available commercially as "Aquateric" and containing additional ingredients required for micronization, used for tablet coating from water dispersions, was shown to adsorb and inactivate the human immunodeficiency virus (HIV-1), herpesviruses (HSV) and other sexually transmitted disease (STD) pathogens. Earlier studies indicate that a gel formulation of micronized CAP has a potential as a topical microbicide for prevention of STDs including the acquired immunodeficiency syndrome (AIDS). The objective of endeavors described here was to develop a water dispersible CAP film amenable to inexpensive industrial mass production.

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

“…Monocaprin hydrogel formulations possess potent microbicidal activity against HIV, HSV, Chlamydia trachomatis and Neisseria gonorrhea (121,122) (Table III). In vitro studies have shown that monocaprin gels formulated using sodium carboxymethylcellulose and polyvinylpyrrolidone or carbomer and hydroxypropylmethylcellulose, are virucidal to HSV-1 and less cytotoxic than nonoxynol-9 (123).…”

Biocompatibility of Solid-Dosage Forms of Anti-Human Immunodeficiency Virus Type 1 Microbicides with the Human Cervicovaginal Mucosa Modeled Ex Vivo

“…CAP belongs to the category of anionic polymer vaginal microbicide candidates (31,42). Whether in soluble or micronized (Aquateric) form, CAP efficiently inactivates HIV-1 through multiple specific mechanisms (31,32). With in vitro-reconstructed human vaginal-ectocervical epithelium ex-pressing a stratified nonkeratinized squamous phenotype (VEC-100; MatTek Corporation, Ashland, MA) (4), we assessed the biocompatibility of CAP and OTC film and gel formulations at concentrations intended for clinical use.…”

Safety and Pharmacokinetics of Quick-Dissolving Polymeric Vaginal Films Delivering the Antiretroviral IQP-0528 for Preexposure Prophylaxis

“…They are used to orally deliver pain medications, vitamins, and supplements (65)(66)(67). Microbicide drugs, such as dapivirine, retrocyclin-101, cellulose acetate phthalate, and dapivirine in combination with TFV, have been formulated into films for vaginal use, and VCF containing nonoxynol-9, a VCF lubricating film, and a vaginal cleansing film (Apothecus Pharmaceuticals) are all available commercially (25,(28)(29)(30)(31)(32). It is important to evaluate the safety of topical PrEP products, as any breach to the integral mucosal barrier and the associated inflammation promote the recruitment of local CD4 T cells and facilitate HIV infection (68).…”

“…Vaginal films to treat bacterial vaginosis and vaginal candidiasis have also been developed (26,27). A number of promising ARVs and/or microbicides, such as dapivirine, TFV, dapivirine in combination with TFV and maraviroc, retrocyclin-101, and cellulose acetate phthalate, have been formulated into films (28)(29)(30)(31)(32)(33)(34). A few studies have evaluated the safety, pharmacokinetics (PK) and pharmacodynamics of films in macaques and humans (29,35).…”