Garg S, Anderson R A, Chany C J, Waller D P, Diao X H, Vermani K, Zaneveld L J
Section of Ob/Gyn Research, Rush University, Rush Presbyterian St. Luke's Medical Center, Chicago, IL, USA.
Contraception. 2001 Jul;64(1):67-75. doi: 10.1016/s0010-7824(01)00217-7.
Vaginal prophylactic methodology may prevent heterosexual transmission of the HIV and other sexually transmitted disease-causing organisms as well as unplanned pregnancies. A new delivery system (ACIDFORM) was designed with acid-buffering, bioadhesive, and viscosity-retaining properties to (1) maintain the acidic vaginal milieu (the low pH inactivates many pathogens and spermatozoa), (2) form a protective layer over the vaginal/cervical epithelium (minimizing contact with pathogenic organisms), and (3) provide long-term vaginal retention. A Phase I clinical study with ACIDFORM provided initial information about its safety and showed the formation of a layer over the vaginal/cervical epithelium [1; Amaral et al., Contraception 1999;60:361-6]. To study the properties of the gel (without active ingredient) in more detail, ACIDFORM's acid-buffering, bioadhesive, viscosity-retaining, and spermicidal properties were compared in vitro to marketed formulations, and its long-term stability was assessed. ACIDFORM, either when titrated with NaOH or when mixed directly with semen, is highly acid buffering and much more effective than Aci-Jel, a commercial acid-buffering vaginal product. ACIDFORM adheres well to two model membranes (excised sheep vagina and cellophane) and is more bioadhesive than Conceptrol, Advantage S, Replens, Aci-Jel, and K-Y jelly. On dilution, ACIDFORM also retains its viscosity better than these marketed products. ACIDFORM is spermicidal and is stable for at least 2 years. These results suggest that ACIDFORM has advantages over presently marketed vaginal delivery systems. The gel may either be useful by itself as an antimicrobial contraceptive product or as a formulation vehicle for an active ingredient with antimicrobial and/or contraceptive properties.
阴道预防方法可以预防艾滋病毒及其他性传播致病微生物的异性传播，以及意外怀孕。一种新型给药系统（ACIDFORM）被设计成具有酸缓冲、生物粘附和粘度保持特性，以（1）维持阴道酸性环境（低pH值可使许多病原体和精子失活），（2）在阴道/宫颈上皮上形成一层保护层（使与致病生物的接触最小化），以及（3）实现长期阴道滞留。一项关于ACIDFORM的I期临床研究提供了其安全性的初步信息，并显示在阴道/宫颈上皮上形成了一层[1；阿马拉尔等人，《避孕》1999年；60:361 - 6]。为了更详细地研究该凝胶（不含活性成分）的特性，在体外将ACIDFORM的酸缓冲、生物粘附、粘度保持和杀精特性与市售制剂进行了比较，并评估了其长期稳定性。ACIDFORM在用氢氧化钠滴定或直接与精液混合时，具有高度的酸缓冲能力，比市售的酸缓冲阴道产品Aci - Jel更有效。ACIDFORM能很好地粘附于两种模型膜（切除的羊阴道和玻璃纸），并且比Conceptrol、Advantage S、Replens、Aci - Jel和K - Y胶冻具有更强的生物粘附性。稀释时，ACIDFORM的粘度也比这些市售产品保持得更好。ACIDFORM具有杀精作用，并且至少稳定2年。这些结果表明，ACIDFORM比目前市售的阴道给药系统具有优势。该凝胶本身可作为一种抗菌避孕产品，也可作为具有抗菌和/或避孕特性的活性成分的制剂载体。
