Formulation, Evaluation, and Clinical Assessment of Novel Solid Lipid Microparticles of Tetracycline Hydrochloride for the Treatment of Periodontitis.

The novel solvent-free process to formulate long-acting microparticles of tetracycline hydrochloride (TH) using hot melt extrusion granulation process coupled with size reduction using comil for the treatment of periodontitis was investigated using hydrogenated castor oil (HCO) as hydrophobic matrix former. The microparticles were characterized for micromeritics, drug diffusion, SEM studies, and stability analysis by DSC, FTIR, and proton NMR. Xanthan gum gel was used as delivery vehicles to administer microparticles inside periodontal pockets. The microparticles were sterilized using gamma radiation; delivery vehicle was sterilized using gamma radiation and autoclave process. Microparticles were evaluated for microbial load as per compendial guidelines. Optimized composition was evaluated for clinical parameters such as plaque index, gingival index, probing pocket depth, and clinical attachment level. Based on the statistical analysis of the data, the micromeritic properties and drug diffusion profiles vary based on the concentration of HCO in the formulation. SEM images reflect the surface properties prior and post drug diffusion studies, which indicates that release takes place predominantly by diffusion of TH through HCO matrix. DSC studies indicate no change in the respective spectra of initial and stability samples. FTIR studies indicate possibility of hydrogen bonding. Proton NMR data suggests characteristic peaks of TH being retained in the stability samples, indicating stable composition. Gamma radiation has led to significant reduction in viscosity of xanthan gum solution over autoclave. Clinical studies indicated statistical improvements in the formulation compared to baseline results, indicating the efficacy of the formulation in the treatment of periodontitis.

Design and Evaluation of Topical Diclofenac Sodium Gel Using Hot Melt Extrusion Technology as a Continuous Manufacturing Process with Kolliphor® P407.

The aim of the present context was to develop and evaluate a Kolliphor® P407-based transdermal gel formulation of diclofenac sodium by hot melt extrusion (HME) technology; central composite design was used to optimize the formulation process. In this study, we have explored first time ever HME as an industrially feasible and continuous manufacturing technology for the manufacturing of gel formulation using Kolliphor® P407 and Kollisolv® PEG400 as a gel base. Diclofenac sodium was used as a model drug. The HME parameters such as feeding rate, screw speed, and barrel temperature were crucial for the semisolid product development, and were optimized after preliminary trials. For the processing of the gel formulation by HME, a modified screw design was used to obtain a uniform product. The obtained product was evaluated for physicochemical characterization such as differential scanning calorimetry (DSC), X-ray diffraction (XRD), pH measurement, rheology, surface tension, and texture profile analysis. Moreover, it was analyzed for general appearance, spreadibility, surface morphology, and drug content. The optimized gel formulation showed homogeneity and transparent film when applied on a glass slide under microscope, pH was 7.02 and uniform drug content of 100.04 ± 2.74 (SD = 3). The DSC and XRD analysis of the HME gel formulation showed complete melting of crystalline API into an amorphous form. The Kolliphor® P407 and Kollisolv® PEG400 formed excellent gel formulation using HME with consistent viscoelastic properties of the product. An improved drug release was found for the HME gel, which showed a 100% drug release than that of a marketed product which showed only 88% of drug release at the end of 12 h. The Flux value of the HME gel was 106 than that of a marketed formulation, which showed only about 60 value, inferring a significant difference (P < 0.05) at the end of 1 h. This study demonstrates a novel application of the hot melt extrusion process for manufacturing of topical semisolid products.

Development of novel floating delivery system based on psyllium: application on metformin hydrochloride.

psyllium, a medicinally active gel forming natural polysaccharide and a dietary fiber has been used as a medicine in myriad of conditions such as constipation and inflammatory bowel syndrome. One of its more recent uses that have received attention has been its ability to reduce blood sugar levels in diabetics. Therefore present work is an attempt to formulate anti diabetic drug Metformin as a controlled release floating delivery making use of pysllium as release retardant and to assist the drug in stabilizing blood sugar level in type II diabetics. Drug and excipients compatibility studies were monitored by thermal analysis using differential scanning calorimeter (DSC) and Fourier transform infra red (FTIR). The DSC thermogram and FTIR of drug and drug-polymer mixture did not reveal any incompatibility. psyllium was tried in different concentrations along with other polymers like HPMC K15M and carbopol 940 to achieve the desired release profile. The total drug: polymer ratio was kept between 1:0.4 to 1:0.5, and different polymer combinations were tried to achieve desired drug release for 12 hours. The prepared tablets were evaluated for in vitro release studies and floating behavior. Our conclusion from the present study indicated that pysllium could potentially be used in conjunction with other polymers to formulate controlled release formulations of anti-diabetic drugs to provide better control over blood glucose levels.