Approaches to the Development of a Low-dose Naltrexone Preparation in the Form of a Nasal Spray (Review)

Introduction. Naltrexone hydrochloride belongs to µ-opioid receptor antagonists and is widely used in the treatment of alcohol and drug addiction at an oral dose of 50 mg/day. It is also a blocker of other receptors – opioid growth factor and Toll-like factor, which is especially evident at doses of 1.5–5 mg/day. This allows it to be used to treat diseases associated with impaired immunity.

Text. To date, there is a significant amount of data indicating the effectiveness of naltrexone hydrochloride administered orally in doses from 1.5 to 5.0 mg per day for the treatment of significant diseases such as AIDS, cancer, autism, multiple sclerosis, etc. However, on the pharmaceutical market still lacks a drug that provides such doses. Due to the fact that oral administration of naltrexone is associated with its first-pass hepatic metabolism and the formation of significant amounts of substances that cause side effects of neuropsychiatric effects and gastrointestinal disorders, as well as the possible effect of naltrexone and its metabolites by other drugs, which in large amounts are used for these diseases, the creation of a parenteral dosage form is relevant.

Conclusion. The review presents current research in the field of low-dose naltrexone application, its mechanisms of action, and considers possible areas of application in medical practice. The disadvantages of oral administration are noted and an alternative route of administration such as intranasal is considered. Approaches to the development of a finished dosage form – nasal spray, are implemented when selecting the optimal content of the active substance and auxiliary components of the drug. The most promising is the creation of a drug based on thermoreversible polymers with a naltrexone hydrochloride content of up to 3,0 %.

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