Controlled delivery of Imatinib mesylate from collagen coated poly(lactic acid) microspheres: In vitro release studies

The development of injectable microspheres for controlled drug delivery to the desired site is a major challenge. We demonstrated the possibility of entrapping an anticancer drug, Imatinib mesylate, in collagen coated biodegradable poly (lactic acid) microspheres with a mean diameter of 10-20 µm. The collagen coating on polymeric matrix surfaces through various surface modification techniques was the current scenario to improve bio-integration of the polymers with the in-vivo system. Here protein adsorption principle is used and various characterization techniques like FTIR, DSC and SEM analysis are used to confirm collagen coating. The reduction in burst release of the Imatinib from the PLA microspheres further confirms its presence and role in controlled release.  This collagen coated PLA microspheres may have potential for the targeted delivery of Imatinib mesylate to treat gastrointestinal stromal tumors, chronic myeloid leukemia cancer

Aripiprazole loaded PLGA nanoparticles for controlled release studies: Effect of Co-polymer ratio

Poly (lactic-co-glycolic acid) nanoparticles loaded with Aripiprazole has been developed as a new therapeutic strategy to achieve its controlled release profile suitable for parenteral administration. Nanospheres composed of different lactic/glycolic acid ratios and drug compositions were synthesized and loaded with Aripiprazole by emulsion/solvent evaporation method and subsequently characterized by particle-size distribution, scanning electron microscopy, encapsulation efficiency and in–vitro drug release studies. Specific drug-polymer interactions are engineered by optimizing the lactide to glycolide ratio (L:G ratio) and including specific polymer hydrophobicity

Controlled delivery of Imatinib mesylate from collagen coated poly(lactic acid) microspheres: In vitro release studies

The development of injectable microspheres for controlled drug delivery to the desired site is a major challenge. We demonstrated the possibility of entrapping an anticancer drug, Imatinib mesylate, in collagen coated biodegradable poly (lactic acid) microspheres with a mean diameter of 10-20 µm. The collagen coating on polymeric matrix surfaces through various surface modification techniques was the current scenario to improve bio-integration of the polymers with the in-vivo system. Here protein adsorption principle is used and various characterization techniques like FTIR, DSC and SEM analysis are used to confirm collagen coating. The reduction in burst release of the Imatinib from the PLA microspheres further confirms its presence and role in controlled release.  This collagen coated PLA microspheres may have potential for the targeted delivery of Imatinib mesylate to treat gastrointestinal stromal tumors, chronic myeloid leukemia cancer

FABRICATION OF DRUG DELIVERY SYSTEM FOR CONTROLLED RELEASE OF CURCUMIN, INTERCALATED WITH MAGNETITE NANOPARTICLES THROUGH SODIUM ALGINATE/POLYVINYLPYRROLIDONE-CO-VINYL ACETATE SEMI IPN MICROBEADS

Objective: The aim of the present work is to fabricate curcumin (CUR) encapsulated microbeads in the polymer matrix of sodium alginate (SA)/poly(vinylpyrrolidone)-co-vinyl acetate (PVP-co-VAc) intercalated with magnetite nanoparticles (MNPs) using glutaraldehyde (GA)/calcium chloride CaCl2 as the crosslinker. Methods: Magnetite nanoparticles (MNPs) were synthesized by a modified co-precipitation method. Curcumin encapsulated SA/PVP-co-VAc microbeads, intercalated with MNPs were prepared by simple ionotropic gelation technique. The formation of microbeads and uniform distribution of curcumin were characterized using spectroscopic methods. In addition, swelling and drug release kinetic studies of the microbeads were performed in simulated intestinal fluid (pH 7.4) and simulated gastric fluid (pH 1.2) at 37 °C. Results: Microbeads formation was confirmed by Fourier Transform Infrared (FTIR). Differential Scanning Calorimetry (DSC) studies reveal that the peak at 181 °C of CUR was not observed in CUR loaded microbeads, which confirms that CUR was encapsulated at the molecular level in the polymer matrix. The X-Ray diffraction (X-RD) diffractograms of CUR shows 2Ө peaks between 12-28 °, which indicated the crystalline nature of CUR, these peaks are not found in CUR loaded microbeads, suggesting that the drug has been molecularly dispersed in the polymer matrix. The X-RD 2Ө peaks of MNPs are observed in the MNPs loaded microbeads, which confirms that MNPs are successfully loaded in the microbeads. The swelling studies and in vitro release studies were performed at pH 1.2 and 7.4. The results reveal that at pH 7.4 highest swelling and release was observed, which confirms that the developed microbeads are pH sensitive and are suitable for intestinal drug delivery. The drug release kinetics fit into the Korsmeyer-Peppas equation, indicating non-Fickian diffusion. Conclusion: The results concluded that the present system as dependent on pH of the test medium and hence suggest suitability for intestinal drug delivery

SODIUM ALGINATE/GELATIN MICROBEADS-INTERCALATED WITH KAOLIN NANOCLAY FOR EMERGING DRUG DELIVERY IN WILSON’S DISEASE

Objective: The aim of the present study was to fabricate and evaluate the drug release studies using Sodium Alginate (SA) and Gelatin (GE) microbeads intercalated with Kaolin (KA) nanoclay for sustained release of D-Penicillamine (D-PA). Methods: Sodium alginate/gelatin/Kaolin blend microbeads were prepared by an extrusion method by using glutaraldehyde (GA) as a crosslinker. The obtained microbeads were characterized by Fourier transform infrared (FTIR) spectroscopy, scanning electron microscopy (SEM) and X–ray diffraction (XRD). Drug release kinetics of the microbeads was investigated in simulated intestinal fluid (pH 7.4) at 37 °C. Results: Microbeads formation was confirmed by FTIR spectroscopy. X-RD reveals that the KA should be intercalated with the drug and also it confirms the molecular level dispersion of D-Penicillamine into microbeads. Scanning Electron Microscopy (SEM) studies reveal that the beads were in spherical shape with some wrinkled depressions on the surface. The in vitro release study indicates the D-Penicillamine released in a controlled manner. The in vitro release kinetics was assessed by Korsmeyer-Peppas equation and the ‘n’ value lies in between 0.557-0.693 indicates Non-Fickian diffusion process. Conclusion: The results suggest that the developed KA intercalated microbeads are good potential drug carrier for the controlled release of D-PA

Aripiprazole loaded PLGA nanoparticles for controlled release studies: Effect of Co-polymer ratio

Poly (lactic-co-glycolic acid) nanoparticles loaded with Aripiprazole has been developed as a new therapeutic strategy to achieve its controlled release profile suitable for parenteral administration. Nanospheres composed of different lactic/glycolic acid ratios and drug compositions were synthesized and loaded with Aripiprazole by emulsion/solvent evaporation method and subsequently characterized by particle-size distribution, scanning electron microscopy, encapsulation efficiency and in–vitro drug release studies. Specific drug-polymer interactions are engineered by optimizing the lactide to glycolide ratio (L:G ratio) and including specific polymer hydrophobicity

DEVELOPMENT AND CHARACTERIZATION OF POLYCAPROLACTONE (PCL)/POLY ((R)-3-HYDROXYBUTYRIC ACID) (PHB) BLEND MICROSPHERES FOR TAMOXIFEN DRUG RELESE STUDIES

Objective: The objective of this study was to formulate and evaluate the drug release studies using Poly (ε-caprolactone) (PCL)/and Poly (R)-3-hydroxy butyric acid (PHB) blend microspheres for controlled release of Tamoxifen, an anticancer drug.Methods: Poly (ε-caprolactone), Poly ((R)-3-Hydroxybutyric acid) blend microspheres were prepared through a modified Water/Oil/Water (W/O/W) double emulsion-solvent diffusion method using Dichloromethane as solvent. Tamoxifen (TAM), an anti Cancer drug, was used for encapsulation within PCL/PHB blend microspheres. Morphology, size, encapsulation efficiency and drug release from these microspheres were evaluated by different characterization techniques such as Fourier transform infrared spectroscopy (FT-IR), Differential scanning calorimetry(DSC), Scanning electron microscopy(SEM), X-ray diffraction studies(X-RD) and dissolution test studies respectively.Results: Drug loaded microspheres were analyzed by FT-IR, which indicates the interaction between drug and polymers. DSC thermograms on drug-loaded microspheres confirmed the polymorphism of Tamoxifen and indicated a molecular level dispersion of drug in the microspheres. SEM confirmed the spherical nature and smooth surface of the microspheres produced. X-RD study was performed to understand the crystalline nature of the drug after encapsulation into the microspheres and confirmed the complete dispersion of the drug in the polymer matrix. In-vitro release studies conducted in different pH which indicated a dependence of release rate on the amount of drug loading and the amount of PCL/PHB, but slow release rates were extended up to 12 h. Kinetic analysis of dissolution data showed a good fit in Peppas equation confirming diffusion controlled drug release.Conclusions: The research findings obtained from the studies were found to be satisfactory. It can be concluded that biodegradable polymer blend (PCL/PHB) microspheres can be effectively used for preparation of controlled release matrices. Â