Proof-of-Concept of Polymeric Sol-Gels in Multi-Drug Delivery and Intraoperative Image-Guided Surgery for Peritoneal Ovarian Cancer

Pharm Res. 2016 Sep;33(9):2298-306. doi: 10.1007/s11095-016-1968-3. Epub 2016 Jun 9.

Abstract

Purpose: The purpose of this study is to investigate a sol-gel transition property and content release profiles for thermosensitive poly-(D,L-lactide-co-glycolide)-block-poly-(ethylene glycol)-block-poly-(D,L-lactide-co-glycolide) (PLGA-b-PEG-b-PLGA) hydrogels carrying paclitaxel, rapamycin, and LS301, and to present a proof-of-concept that PLGA-b-PEG-b-PLGA hydrogels carrying paclitaxel, rapamycin, and LS301, called TheranoGel, exhibit excellent theranostic activity in peritoneal ES-2-luc ovarian cancer xenograft mice.

Methods: Thermosensitive PLGA-b-PEG-b-PLGA hydrogels carrying paclitaxel, rapamycin, and LS301, individually or in combination, were prepared via a lyophilization method, characterized with content release kinetics, and assessed with theranostic activity in ES-2-luc xenograft mice.

Results: A thermosensitive PLGA-b-PEG-b-PLGA sol-gel system was able to entrain 3 poorly water-soluble payloads, paclitaxel, rapamycin, and LS301 (TheranoGel). TheranoGel made a sol-to-gel transition at 37°C and slowly released 3 drugs at a simultaneous release rate in response to the physical dissociation of hydrogels in vitro. TheranoGel enabled loco-regional delivery of multi-drugs by forming a gel-depot in the peritoneal cavity of ES-2-luc xenograft mice. An intraperitoneal (IP) administration of TheranoGel resulted in excellent therapeutic and diagnostic activities, leading to the improved peritoneal surgery in ES-2-luc xenograft mice.

Conclusions: TheranoGel prepared via a facile lyophiliation method enabled successful IP delivery of multi-drugs and exhibited excellent theranostic activity in vivo.

Keywords: hydrogels; intraperitoneal; ovarian cancer; theranostics; thermosensitive.

MeSH terms

  • Animals
  • Drug Carriers / chemistry
  • Drug Delivery Systems / methods
  • Female
  • Hydrogels / chemistry*
  • Injections, Intraperitoneal / methods
  • Mice
  • Mice, Nude
  • Ovarian Neoplasms / diet therapy*
  • Paclitaxel / administration & dosage
  • Paclitaxel / chemistry*
  • Peritoneal Neoplasms / drug therapy*
  • Polyesters / administration & dosage
  • Polyesters / chemistry*
  • Polyethylene Glycols / administration & dosage
  • Polyethylene Glycols / chemistry*
  • Polymers / chemistry*
  • Sirolimus / administration & dosage
  • Sirolimus / chemistry
  • Surgery, Computer-Assisted / methods

Substances

  • Drug Carriers
  • Hydrogels
  • Polyesters
  • Polymers
  • poly(lactide-co-glycolide)-block-poly(ethylene glycol)-block-poly(lactide-co-glycolide)
  • Polyethylene Glycols
  • Paclitaxel
  • Sirolimus