Imiquimod: An immune response modifier☆,☆☆,★

Small-molecule therapeutics include commonly used systemic agents, such as methotrexate, sulfasalazine, mycophenolate mofetil, azathioprine, and cyclophosphamide; newer agents, such as glatiramer; and topical agents, such as imiquimod and pimecrolimus. Although biologics have attracted considerable attention recently, immunomodulators remain critical therapeutic options for patients. In part, this is because they have been shown, in some cases, to be as effective as biologics or synergistic in efficacy when combined with biologics. Topicals also lack the systemic side effects. This chapter reviews the mechanisms, side effects, and clinical uses of these agents.

Taste sensations are considered to be an important factor for detecting and digesting food to maintain good nutrition and leading a healthy lifestyle. Many medications produce altered taste perceptions, which then leads to a direct effect on food-related behaviors. Considering that taste disturbances of patients with have long been observed but never understood, ongoing taste research has identified cellular mechanisms of a variety of drugs that cause taste impairments in cancer patients. These findings facilitate a better understanding of the paradigm that immune responses initiated by drugs can alter taste signal transduction pathways during sensory information processing in taste buds. Inevitably, these findings also may facilitate the development of taste modifiers, which ameliorate taste disturbances associated with the chemotherapy on the compensation of taste sensations for losses in medications.

Small-molecule therapeutics include commonly used systemic agents, such as methotrexate, sulfasalazine, mycophenolate mofetil, azathioprine, and cyclophosphamide; newer agents, such as glatiramer; and topical agents, such as imiquimod and pimecrolimus. Although biologics have attracted considerable attention recently, immunomodulators remain important therapeutic options for patients. In part, this is because they have been shown to be, in some cases, as effective as biologics or synergistic in efficacy when combined with biologics. This chapter reviews the mechanisms, side effects, and clinical uses of these agents.

The human papillomavirus (HPV) infection, which is strongly related to cervical cancer, can be reduced by the topical application of imiquimod. Some strategies have been used to increase the adhesion and penetration of drugs through the vaginal mucosa. Two of them are the development of mucoadhesive semisolid formulations and the development of polymeric nanocarriers. In this paper, we hypothesize that the combined use of these two strategies results in a better performance of the formulation to retain imiquimod into the vaginal tissue. Aiming this, two different systems are proposed: (a) chitosan-coated poly(ε-caprolactone)-nanocapsules incorporated into hydroxyethylcellulose gel (HEC-NC_imiq-chit), and (b) poly(ε-caprolactone)-nanocapsules incorporated into chitosan hydrogel (CHIT-NC_imiq). These formulations were submitted to three main tests: mucoadhesivity by interaction, permeation and washability test (or retention test). We developed an integrative index that allows comparing the global performance of the proposed formulations by considering jointly the results of these three tests. Thus, when considered the integrative indexes for the formulations, our results show that CHIT-NC_imiq presents the best performance for the treatment of HPV.