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Preparation and characterization of Pingyangmycin-loaded bovine serum albumin microspheres for embolization therapy
Changguang Wang1, Jie Liu, Qinghong Gao
1West China College of Pharmacy, Sichuan University, Chengdu 610041, China.
Abstract:
Bovine serum albumin microspheres (BSA-MSs) containing Pingyangmycin hydrochloride (PYM) were prepared for the interventional embolization by an emulsification-crosslinking method. The average diameter of the MSs was 83.6 microm with 80% ranging from 35 to 200 microm. The MSs showed a rather high entrapment efficiency (EE%) of 87.6+/-5.7% and the drug loading efficacy (DL%) was 20.2+/-1.3%. The drug release behaviors were evaluated both in vitro and in vivo, using UV-spectroscopy and HPLC, respectively. The in vitro results showed a significantly delayed release of drug for 10 days. The central auricular artery of rabbit was chosen as an embolization sites to study the in vivo drug release and the pharmacokinetics of the MSs compared with PYM injections. Experiments performed by artery perfusion and embolization in rabbits central auricular artery revealed that the PYM loaded BSA-MSs (PYM-BSA-MSs) could obviously prolong in vivo drug release, extend the mean residence time (MRT) and had equal bioavailability compared with plain PYM injections. These results demonstrated that by embolization of the central auricular artery with PYM-BSA-MSs, the local drug concentration could maintain at a relative high level for a longer time, thus achieve the aim of tumor targeting therapy. PYM-BSA-MSs are excellent potential alternatives of interventional embolization materials for the treatment of maxillofacial region tumors.
Insights
Bovine serum albumin microspheres (BSA-MSs) loaded with Pingyangmycin hydrochloride (PYM) offer sustained drug release for interventional embolization. These PYM-BSA-MSs show promise for targeted tumor therapy in the maxillofacial region.
Area of Science:
- Biomaterials Science
- Drug Delivery Systems
- Oncology Therapeutics
Background:
- Interventional embolization requires effective drug delivery systems for localized cancer treatment.
- Bovine serum albumin microspheres (BSA-MSs) offer biocompatibility and controlled release potential.
- Pingyangmycin hydrochloride (PYM) is an anti-tumor agent suitable for localized delivery.
Purpose of the Study:
- To prepare and characterize BSA-MSs loaded with PYM (PYM-BSA-MSs) for interventional embolization.
- To evaluate the in vitro and in vivo drug release profiles and pharmacokinetics of PYM-BSA-MSs.
- To assess the potential of PYM-BSA-MSs for targeted tumor therapy in maxillofacial region tumors.
Main Methods:
- BSA-MSs containing PYM were prepared using an emulsification-crosslinking method.
- Microsphere size, entrapment efficiency (EE%), and drug loading efficacy (DL%) were determined.
- In vitro drug release was assessed using UV-spectroscopy, and in vivo studies utilized HPLC in rabbit models.
Main Results:
- The prepared PYM-BSA-MSs had an average diameter of 83.6 micrometers and high EE% (87.6+/-5.7%) and DL% (20.2+/-1.3%).
- In vitro studies demonstrated a significantly delayed drug release over 10 days.
- In vivo studies in rabbits showed prolonged drug release, extended mean residence time (MRT), and comparable bioavailability to PYM injections.
Conclusions:
- PYM-BSA-MSs provide sustained local drug release and maintain high drug concentrations for extended periods.
- These microspheres are effective for interventional embolization, offering a potential for targeted tumor therapy.
- PYM-BSA-MSs represent a promising alternative for treating maxillofacial region tumors via embolization.
