Irinotecan hydrochloride liposome, and preparation process therefor and use thereof

By combining microfluidic devices and tangential flow filtration membrane encapsulation devices, irinotecan hydrochloride liposomes with uniform and stable particle size were prepared, solving the problems of difficult particle size control and easy equipment clogging in the prior art, and improving the therapeutic effect and stability of the drug.

WO2026139095A1PCT designated stage Publication Date: 2026-07-02JIANG SU PHARMAMAXCORP
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Patent Information

Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
JIANG SU PHARMAMAXCORP
Filing Date
2026-02-10
Publication Date
2026-07-02

AI Technical Summary

Technical Problem

Existing irinotecan hydrochloride formulations suffer from problems such as difficulty in particle size control, easy equipment clogging, and poor stability, resulting in rapid drug clearance in the body and poor efficacy.

Method used

Irinotecan hydrochloride liposomes with a particle size of 90–115 nm and a dispersibility index of <0.2 were prepared by mixing water and oil phases using a microfluidic device, using sucrose octetrate triethylamine as the aqueous phase, and combining it with a tangential flow filtration membrane device to control the oil-water ratio and temperature.

Benefits of technology

It achieves high encapsulation efficiency (≥95%) and good particle size control, prolongs the drug's retention time in the body, improves the permeability and therapeutic effect of tumor tissue, has good stability, and is suitable for large-scale production.

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Abstract

The present invention belongs to the technical field of pharmaceutical preparations, and specifically relates to an irinotecan hydrochloride liposome, and a preparation process therefor and the use thereof. The preparation process of the present invention comprises the following steps: (1) adjusting the concentrations of triethylammonium sucrose octasulfate in an internal aqueous phase and the total lipids, and mixing an oil phase and an aqueous phase at a certain flow rate and ratio by means of a microfluidic device to prepare a blank liposome; (2) removing free triethylammonium sucrose octasulfate and organic solvent outside the blank liposome by using an HEPES buffer, and performing concentration; and (3) preparing a drug-loaded liposome by using an active loading method. The solution of the present invention can greatly improve the encapsulation efficiency of the irinotecan hydrochloride liposome and accurately control the particle size of the liposome. The finally prepared liposome has a particle size of 90 nm-115 nm, an encapsulation efficiency of 95%, and a better stability.
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