Rathi Ritu, Kumar Alpesh, Vishvakarma Vivekanand, Huanbutta Kampanart, Singh Inderbir, Sangnim Tanikan
Chitkara College of Pharmacy, Chitkara University, Rajpura 140401, India.
School of Pharmacy, Eastern Asia University, Pathumthani 12110, Thailand.
Pharmaceutics. 2022 Oct 17;14(10):2210. doi: 10.3390/pharmaceutics14102210.
The rectal route is an effective route for the local and systemic delivery of active pharmaceutical ingredients. The environment of the rectum is relatively constant with low enzymatic activity and is favorable for drugs having poor oral absorption, extensive first-pass metabolism, gastric irritation, stability issues in the gastric environment, localized activity, and for drugs that cannot be administered by other routes. The present review addresses the rectal physiology, rectal diseases, and pharmaceutical factors influencing rectal delivery of drugs and discusses different rectal drug delivery systems including suppositories, suspensions, microspheres, nanoparticles, liposomes, tablets, and hydrogels. Clinical trials on various rectal drug delivery systems are presented in tabular form. Applications of different novel drug delivery carriers viz. nanoparticles, liposomes, solid lipid nanoparticles, microspheres, transferosomes, nano-niosomes, and nanomicelles have been discussed and demonstrated for their potential use in rectal administration. Various opportunities and challenges for rectal delivery including recent advancements and patented formulations for rectal drug delivery have also been included.
直肠给药途径是活性药物成分局部和全身递送的有效途径。直肠环境相对稳定，酶活性低，有利于口服吸收差、首过代谢广泛、有胃刺激、在胃环境中稳定性差、局部活性的药物，以及不能通过其他途径给药的药物。本综述阐述了直肠生理学、直肠疾病以及影响药物直肠递送的药学因素，并讨论了不同的直肠给药系统，包括栓剂、混悬剂、微球、纳米粒、脂质体、片剂和水凝胶。以表格形式呈现了各种直肠给药系统的临床试验。讨论并展示了不同新型药物递送载体，即纳米粒、脂质体、固体脂质纳米粒、微球、传递体、纳米囊泡和纳米胶束在直肠给药中的潜在应用。还包括了直肠给药的各种机遇和挑战，包括直肠给药的最新进展和专利制剂。
