Abstract
AbstractA novel formulation of paclitaxel (PTX) has been developed by providing multilayer assembly over drug loaded porous CaCO3 microparticles (CaCO3 MP) using combination of biocompatible and biodegradable polyelectrolytes (PE’s). PTX was encapsulated into the nanopores of preformed CaCO3 MP prepared by the co-precipitation method. Infrared (IR) and X-ray diffraction (XRD) provides evidences that PTX has been encapsulated into nanopores of CaCO3 MP and not crystallized on the surface. PTX loaded CaCO3 MP (CaCO3-PTX) was found to be highly stabilized against thermal decomposition as evinced by thermo gravimetric analysis (TGA) indicating decomposition at 600°C and 250°C for CaCO3-PTX and PTX respectively. The multilayer assembly over CaCO3-PTX was effectuated by alternate deposition of protamine sulfate (PRM) and sodium alginate (SA) using LBL technique followed by subsequent core removal [PTX- (PRM/SA)5]. The pay load efficiency of PTX in this system was found to be 78.98±2.14%. The developed system was further evaluated for surface morphology, size and size distribution, surface charge, core removal and layer-by-layer growth due to sequential adsorption of PE’s. The release data of PTX-(PRM/SA)5 was comparable with marketed formulation of PTX (PTX-M) and CaCO3-PTX when performed in simulated intestinal fluid (SIF pH=7.4). The release profile of PTX-(PRM/SA)5 indicates that PEs based multilayer matrix is capable to provide barrier to PTX release as it has been found to follow first order matrix diffusion kinetics with 64±4.8% release within 24 hrs. The t50% of PTX-M, CaCO3-PTX and PTX-(PRM/SA)5 was found to be 70, 90 and 480 minutes respectively. This alternative delivery system of PTX disguised in the form of LBL assembly could have immense application for the treatment of metastasized mammary glands vis-à-vis existing formulation of PTX which is by and large criticized for having certain toxic excipients to be given parentrally. Moreover, the proposed system provides ample of opportunity to modify the surface for targeted application of PTX.
Highlights
AND OBJECTIVERecently an extensive effort has been made in the development of smart, functional, organized delivery system by layer-by-layer (LBL) self-assembling technique for micro/nano-encapsulation of bioactives, Caruso [2001]; Decher and Schlenoff [2003]
Shape, surface morphology and narrow size distribution ranging from 4-6 μm of the CaCO3 microparticles and fabricated capsules were presented by the particle size analyzer and SEM photomicrographs
The release profile of PTX-(PRM/SA)5 indicates that PEs based multilayer matrix is capable to provide barrier to PTX release as it has been found to follow first order matrix diffusion kinetics (r2= 0.9973) with 72±4.8% release within
Summary
An extensive effort has been made in the development of smart, functional, organized delivery system by layer-by-layer (LBL) self-assembling technique for micro/nano-encapsulation of bioactives, Caruso [2001]; Decher and Schlenoff [2003]. The encapsulation of bioactive materials into porous microparticles of inorganic origin have a great potential to allocate the drug in their nanopores (nanoreservoir) and have features to impart biological stability along with sustained release properties. We have made an attempt to develop a novel formulation of paclitaxel (PTX) by providing multilayer assembly over drug loaded porous CaCO3 microparticles (CaCO3 MP) by using combination of biocompatible and biodegradable polyelectrolytes (PE’ s). Drug release profile of formulations in SIF (pH=7.4): F1:CaCO3-PTX; F-2: PTX (PRM/SA) and F-3: PTX-M
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