The worldwide impact of HIV/AIDS is well recognized. This book provides for the first time a thorough and critical overview of current aspects, recent developments, and trends in the formulation and drug delivery concerning anti-HIV microbicides by leading scientists in the field. Additionally, pertinent regulatory aspects and socioeconomical issues related to the subject are discussed. In the absence of a cure, prophylaxis represents a cornerstone in the battle against infection. One promising strategy comprises the use around the time of sexual intercourse of vaginal/rectal products containing antiviral compounds, termed microbicides. It is now recognized that specific development of drug dosage forms and/or drug delivery systems is an indispensable aspect for the success of microbicides. Different groups strived over the last decade to optimize the biophysical and technological performance of traditional dosage forms (gels, tablets, and suppositories) to fulfill the specificities of microbicides use, without neglecting users’ preferences and affordability issues. Moreover, new formulation approaches, such as vaginal rings and films, nanotechnology-based systems, stimuli-sensitive formulations, targeted drug delivery systems, among others have been proposed and are currently undergoing pre-clinical or even clinical testing.