Advancements in Rectal Drug Delivery: Clinical and Pharmaceutical Insights

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Abstract: The rectal route serves as a valuable and effective method for both localized and sys-temic drug administration, offering several advantages compared to other delivery pathways. This route benefits from a relatively stable rectal environment with low enzymatic activity, mak-ing it particularly suitable for drugs that face challenges such as poor oral bioavailability, exten-sive first-pass metabolism, gastrointestinal instability, or gastric irritation. It is also an ideal op-tion for individuals who have difficulty swallowing, suffer from nausea or vomiting, or need tar-geted drug delivery to the lower gastrointestinal tract. Several physiological and pharmaceutical factors influence how well drugs are absorbed and how effective they are when administered rec-tally. This review delves into the anatomy and physiology of the rectum, common rectal disor-ders, and key formulation aspects that impact rectal drug delivery. It also discusses various rectal dosage forms, including suppositories, suspensions, microspheres, nanoparticles, liposomes, tab-lets, and hydrogels, and explains their mechanisms of action and potential therapeutic uses. Moreover, the review includes a comprehensive table summarizing clinical trials that assess the safety and effectiveness of rectal formulations, offering insights into the latest developments and future directions in this field.

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