Hydrophobic ion-pairing assembled liposomal Rhein with efficient loading for acute pancreatitis treatment

Abstract

Aim

The present study aimed to develop liposomal Rhein by employing a hydrophobic ion-pairing technique (HIP) for improved pancreatitis therapy.

Methods

F127 modified liposomal Rhein (F127-RPC-Lip) was prepared using a two-step process consisting of complexation first, followed by a film-ultrasonic dispersion step. The drug-phospholipid interaction was characterised by FT-IR and P-XRD. Particle size and morphology were investigated using DLS and TEM, respectively. Biodistribution and therapeutic efficacy of F127-RPC-Lip were evaluated in a rat model of acute pancreatitis.

Results

F127-RPC-Lip achieved efficient drug encapsulation after complexation with lipids through non-covalent interactions and had an average hydrodynamic diameter of about 141 nm. F127-RPC-Lip demonstrated slower drug release (55.90 ± 3.60%, w/w) than Rhein solution (90.27 ± 5.11%) within 24 h. Compared with Rhein, F127-RPC-Lip exhibited prolonged systemic circulation time, superior drug distribution, and attenuated injury in the pancreas of rats post-injection.

Conclusions

HIP-assembled liposomes are a promising strategy for Rhein in treating pancreatitis.

Keywords:

• Hydrophobic ion pairing
• liposome
• drug-loading capacity
• Rhein
• pancreatitis therapy

Disclosure statement

No potential conflict of interest was reported by the author(s).

Additional information

Funding

The present study was supported by the National Natural Science Foundation of China (81703422 and 81703433), the Project of the Basic Research Fund of the Henan Institute of Medical and Pharmacological Sciences (yyyjk201801), and the Key Scientific and Technological Project of Henan Province (202102310160).