In situ gel is a kind of preparation that is administered in a low viscosity state. Under the influence of external stimuli at the administration site, the phase changes from liquid to solid/semi-solid gel, forming a local drug repository. As a new drug delivery technology, in situ gel preparation has the advantages of simple preparation process, long residence time at the drug application site, and significant sustained release effect.

In situ gel marketing case sharing: Uzedy Risperidone injection suspension

Uzedy Risperidone injection suspension is a long-acting subcutaneous antipsychotic drug (LASCA) approved by the US FDA in April 2023 for the treatment of adult schizophrenia. This preparation is injected subcutaneously using a pre filled ready to use syringe, equipped with a short needle, a thin needle tube, and a low-dose capacity. The injection site is the abdomen or upper arm. Uzedy does not require loading doses or oral supplements, and can reach clinically significant plasma concentrations of Risperidone and its active metabolites within 6-24 hours after subcutaneous administration.

This formulation combines Risperidone with innovative copolymer drug delivery technology to create a suspension suitable for subcutaneous administration. The prescription information is as follows:

From Uzedy's prescription, it can be seen that the sustained-release material used is mainly a combination of mPEG and PDLLA block copolymers, including diblock copolymers (DB) and triblock copolymers (TB), which are derived from MedinCell's BEPO Technology.

BEPO is an in situ gel technology (ISFD) based on solvent exchange. After contacting with body fluid, the solvent in the system diffuses, and the polymer designed to be insoluble in water precipitates out, thus realizing the physical encapsulation of active drug ingredients. The following figure shows the process of forming a reservoir by injecting a solution of copolymer in dimethyl sulfoxide (DMSO) into a buffer medium.

By using BEPO technology, the release characteristics of various drugs (including macromolecular drugs) can be adjusted by adjusting parameters in the formula, such as the composition, molecular weight, and relative ratio of DB and TB, the mass fraction of PEG and PDLLA in each copolymer, or the relative ratio between active ingredients, polymers, and solvents.

Release curves of Bupivacaine in formulations with fixed Bupivacaine content, the same TB: DB combination and ratio, and different total polymer content

Cumulative release of Bupivacaine from drug depots prepared with the same TB and DB combination, the same polymer and active ingredient content, and different TB: DB ratios

Polyethylene glycol polyester block copolymers have been widely studied as functional excipients in the field of drug delivery due to their biocompatibility, biological absorbency, and relatively simple synthesis process, and are suitable for various application scenarios. In these systems, the average molecular weight, relative ratio, and structural design of polyethylene glycol (PEG) and polyester components are crucial for regulating the physicochemical properties of the final delivery system, thereby affecting the release kinetics of drugs.

Ai Weituo mPEG PLA samples are available for free application, with limited quantities available on a first come, first served basis!

New product sample giveaway | mPEG PLA block copolymer free application, empowering your drug delivery

Iveto provides in situ gel key excipients supply and special excipients customization services. At present, many in situ gel excipients are undergoing CDE registration. At the same time, Aiweituo product team can provide in situ gel preparation analysis, product introduction and other technical publicity services. Customers are welcome to contact us.

List of auxiliary materials for IVTO in-situ gel

Aiweituo in-situ gel line can preach PPT

Prescription and Application Analysis of In situ gel Preparations on the Market in the World

Abstract:

1. Definition and advantages of in situ gel preparations;

2. List of prescription of marketed in situ gel preparations;

3. Introduction of in situ gel sustained release mechanism;

4. Introduction to key sustained-release excipients and solvents of in situ gel preparations

(Stay tuned for more related PPTs...)