QbD enabled Process Variable Study to Develop Sustained Release Chitosan-Alginate Embedded Delivery System for Improved Patient Compliance

Abstract The current investigation entail systematic Quality by Design (QbD)-enabled approach for the development of Sustained released embedded drug delivery systems of L-Arginine employing ionic gelation technique to attain improved patient compliance. Hence, in this QbD enabled systematic approach; quality target product profile (QTTP) was defined and critical quality attributes (CQAs) were identified. Further the risk assessment studies were undertaken through Ishikawa fish bone diagram to locate the critical material attributes (CMAs) and/or critical process parameters (CPPs) for the formulation of beads that may affect CQAs of drug product. A face centered central composite design (CCD) for two factors at three levels each with α =1 was employed for the optimization process to checkout the impact of concentration of sodium alginate and concentration of chitosan as CMAs which wereprior identified from risk assessment study and further evaluated for CQAs viz. bead size, swelling index and percent drug entrapment. The optimum formulation was embarked upon by using mathematical model being developed yielding desired CQAs. Thereby chitosan coated calcium-alginate delivery system was successfully developed by strategically employing QbD approach.In a nutshell, the presentinvestigation reports the successful development of optimized chitosan coated alginate beads employing QbD approach which can serve as a platform for other drugs too.

Sodium alginate-guar gum and carbopol based methotrexate loaded mucoadhesive microparticles for colon delivery: An in vitro evaluation

Methotrexate (MTX) is famous for its therapeutic potential against different cancers including colorectal cancer. Goal of the present investigation was to formulate MTX loaded mucoadhesive microparticles for colon targeting. The optimized formulation (MTX-MS2) was composed of mucoadhesive polymers (sodium alginate, guar gum and carbopol 940) in an appropriate ratio. MTXMS2 was developed by ionic-gelation method. The suitable particle size and zeta potential were found to be 21.10 ± 0.18 µm and 3.01 ± 0.16 mV for MTX-MS2 respectively. The % yield (98.60 ± 2.12), % entrapment efficiency (97.98 ± 1.22) and % drug loading (1.04 ± 0.03) were estimated for MTXMS2. The swelling index (0.99 ± 0.04 θ) and mucoadhesion (97.29 ± 4.61%) were significantly (***P ˂ 0.01) achieved with MTX-MS2 as compared to other formulations. The optimum drug release (96.07 ± 4.52%) was significantly achieved with MTX-MS2 at simulated gastric fluid (pH 7.4) for 36 h in a sustained manner. This profile may be attributed towards excellent mucoadhesivness of the polymers used in the formulation. Therefore, the current investigation suggests that mucoadhesive carrier system could be promising approach for colon delivery. Thus, the proposed work would be helpful for the treatment of colorectal canc

Preparation and characterization of naftifine-loaded poly(vinyl alcohol)/sodium alginate electrospun nanofibers

In this study, naftifine (a topical antifungal drug) loaded poly(vinyl) alcohol (PVA)/sodium alginate (SA) nanofibrous mats were prepared using the single-needle electrospinning technique. The produced nanofibers were crosslinked with glutaraldehyde (GTA) vapor. The morphology and diameter of the electrospun nanofibers were studied by scanning electron microscopy (SEM). SEM images showed the smoothness of the nanofibers and indicated that the fiber diameter increased with crosslinking and drug loading. Atomic force microscopy (AFM) images confirmed the uniform production of the scaffolds, and elemental mapping via energy dispersive X-ray spectroscopy (EDS) showed the uniform distribution of the drug within the nanofibers. An attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy study demonstrated that naftifine has sufficient secondary interactions with the polymer blend. The crosslinking treatment decreased the burst drug release effectively and the release mechanism followed Korsmeyer-Peppas Super Case-II transport. Overall, these findings suggest the potential use of naftifine-loaded PVA/SA nanofibers as a topical antifungal drug delivery system.