Title : The future of type 2 diabetes management: From trial and error to a QbD driven approach to zein microparticle therapeutics
Abstract:
Introduction- Diabetes mellitus, a growing global health concern, necessitates innovative drug delivery strategies to overcome limitations associated with conventional therapies, such as poor bioavailability and systemic toxicity. Nanotechnology offers promising solutions, particularly biopolymer based microparticles, which enable controlled and targeted drug release. This study investigates the development and optimization of diacerein- loaded zein microparticles as a novel approach to enhance antidiabetic activity.
Aim- To develop and optimize, using Quality by Design (QbD) principles, diacerein loaded zein microparticles for improved antidiabetic activity through sustained drug release and enhanced bioavailability.
Methods- Zein microparticles were developed using an antisolvent precipitation method. Critical process parameters were identified through one factor at a time (OFAT) analysis. After analyzing all the critical variables, the key parameters were selected and zein microparticles were statistically optimized through Box-Behnken design. The optimized diacerein-loaded zein microparticles were further characterized for particle size, zeta potential, Polydispersity index (PDI), morphology (scanning electron microscope), entrapment efficiency, and crystalline structure (X-ray diffraction pattern). The invitro release studies were conducted in simulated interstitial fluid (SIF) and simulated gastric fluid (SGF) to assess drug release kinetics. In invivo antidiabetic activity was evaluated in wistar rats.
Results- The compatibility analysis conducted through FTIR studies revealed no component interactions. The microparticles exhibited an average particle size of 1762.7 ± 15.72 nm with a polydispersity index (PDI) of 20.0 ± 2% and the zeta potential was -18.9± 2.35 mV. The microscopic analysis revealed a spherical morphology of microparticles. The invitro release studies demonstrated slow and sustained release of diacerein over a period of 24 hours, following the Higuchi kinetic model. In vivo studies showed a significant blood glucose-lowering effect in wistar rats.
Conclusion- This study revealed that zein microparticles effectively protect diacerein from gastrointestinal degradation and facilitates sustained release, thereby enhancing oral bioavailability and antidiabetic efficacy. The developed zein microparticle system represents a promising, scalable, and therapeutically efficient platform for controlled oral delivery of drugs. This approach holds significant potential for improving patient compliance and therapeutic outcomes in diabetes management
