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Controlled-release microparticles offer a promising avenue for enhancing patient compliance and minimizing dosage frequency. In this study, we aimed to design controlled-release microparticles of Glipizide utilizing Eudragit S100 and Methocel K 100 M polymers as controlling agents. The microparticles were fabricated through a simple solvent evaporation method, employing various drug-to-polymer ratios to formulate different controlled-release batches labeled as F1 to F5. Evaluation of the microparticles encompassed a range of parameters including flow properties, particle size, morphology, percentage yield, entrapment efficiencies, percent drug loading, and dissolution studies. Additionally, various kinetic models were employed to elucidate the drug release mechanism. Furthermore, difference and similarity factors were utilized to compare the dissolution profiles of the tested formulations with a reference formulation. The compressibility index and angle of repose indicated favorable flow properties of the prepared microparticles, with values falling within the range of 8 to 10 and 25 to 29, respectively. The particle size distribution of the microparticles ranged from 95.3 to 126 μm. Encouragingly, the microparticles exhibited high percent yield (ranging from 66 to 77%), entrapment efficiency (80 to 96%), and percent drug loading (46 to 54%). All formulated batches demonstrated controlled drug release profiles extending up to 12 hours, with glipizide release following an anomalous non-Fickian diffusion pattern. However, the drug release profiles of the reference formulation and various polymeric microparticles did not meet the acceptable limits of difference and similarity factors. In-vivo studies revealed sustained hypoglycemic effects over a 12-hour period, indicating the efficacy of the controlled-release microparticles. Overall, our findings suggest the successful utilization of polymeric materials in designing controlled-release microparticles, thereby reducing dosage frequency and potentially improving patient compliance. [ABSTRACT FROM AUTHOR]

The current study is aimed to formulate pH responsive polymeric hydrogels. Potassium per sulphate and Methylene bis acrylamide were employed as initiator and cross linker respectively. To determine the effect of substrate on degree of cross linking different ratios of the acrylic acid (AA), potassium per sulphate (KPS) and methylenebisacrylamide (MBA) were used. Swelling experiments were conducted in both basic and acidic media. Phosphate buffer of pH 7.4 and 0.1N HCl solution were used for swelling experiment of hydrogels. The hydrogels were more responsive towards basic medium as compared to acidic environment. Formulations were also evaluated for In vitro evaluation. Diacerein was selected model drug for hydrogel. Release pattern of the diacerein was studied both in acidic (0.1N HCl solution) and basic medium. Percentage drug release from M3 formulation showed as crosslinker concentration increase (0.03 %) drug release decrease Hydrogel samples were characterized by FTIR to confirm the functional groups of the hydrogels and their components and scanning electron spectroscopy (SEM) was performed to characterize the structure or morphology of the hydrogels. Finally, the dissolution studies were performed to evaluate the sustain release property of the hydrogel samples. Results show that all formulations of hydrogels are pH-sensitive and follow zero-order kinetics for drug release. Hence, optimized nexus (M3) serves as excellent carrier for target drug delivery. [ABSTRACT FROM AUTHOR]

Grewia asiatica L. is a potential medicinal plant used for various diseases in traditional medicine. Current study was aimed to evaluate the cardio protective, anti-inflammatory, analgesic and CNS depressant activities of Grewia asiatica L. fruit extract. In cardio protective activity myocardial injury was produced by injection of Isoproterenol (200 mg/kg, s.c), G. asiatica 250 and 500mg/kg treated groups significantly (p<0.05) decreased the level of serum AST, ALT, LDH and CKMB, hence produced cardio protective effect. In analgesic activities G. asiatica produced significant (p<0.05) analgesic effects in acetic acid induced writhing, formalin, paw pressure and tail immersion test. G. asiatica at 250 and 500mg/kg oral dose, significantly (p<0.05) reduced the rat paw edema in carrageen an induced rat paw edema test. G. asiatica extract also produced significant CNS depressant effects in open field, hole board and thiopental sodium induced sleeping time. Findings of the current study suggest that G. asiatica fruit extract showed potential pharmacological effects and can be utilized in alternative medicine. [ABSTRACT FROM AUTHOR]

Controlled release" in drug release kinetics denotes reproducibility and predictability, implying that drug release from delivery devices follows a kinetically predictable and repeatable rate profile from dose to dose. In the current study controlled release tablets of famotidine were prepared by direct compression technique using Eudragit RL 100 polymer. Four different formulations of controlled release tablets of famotidine as (F1, F2, F3 and F4) were prepared by adding different drug to polymer ratio. The pre compression and the post compression of the formulation, characteristics were compared. All results obtained were within the specified standard limits. FTIR studies showed that both the drug and the polymer were compatible. In vitro dissolution study were conducted by Method II (Paddle Method) in phosphate buffer (pH 7.4), at 100rpm. Power law kinetic model was applied for drug release mechanism. The difference similarity of the dissolution profile was determined. The formulation F1 and F2 were released 97 and 96 % in 24 hours and other formulations F3 and F4 were released subsequently 93% and 90% in 24 hours. The results showed that incorporation of Eudragit RL 100 in the formulation of controlled release tablets prolong the drug release rates for 24 hours. The release mechanism was Non-Fickian diffusion mechanism. It was deducted from the current study that the Eudragit RL 100 can be efficiently incorporated in the formulation of controlled release dosage forms with predictable kinetics. [ABSTRACT FROM AUTHOR]

The purpose of this study was to purify the phytoconstituents and to explore the antibacterial, antifungal, phytotoxic and cytotoxic potential of dichloromethane and methanol extracts of aerial and root parts of Trigonella polycerata. The phytochemical study on methanol extract of aerial parts of the plant led to the isolation and purification of seven compounds that were identified as 3,4-dimethoxycinnamaldehyde, Trigocoumarin, 6,7,8-trimethoxycoumarin, Penduletin, 5-hydroxy-3,6,7,4´-tetramethoxyflavone, 3,5,7-trihydroxy-6,4-dimethoxyflavone and 5-hydroxy-4,7-dimethoxyflavone. These structures were elucidated by interpretation of EI-MS and NMR spectral data. The plant aerial parts methanol extract (TPAM) demonstrated higher antibacterial (78.99%), phytotoxic (85% growth regulation at 1000μg/mL) and cytotoxic activities (LD 50 : 45.643μg/mL). While the methanol root extract (TPRM) was highly active against bacteria's; Salmonella typhi (71.56%), Staphylococcus aureus (70.15%), Escherichia coli (69%), fungi like Candida albicans (70.21%) and moderately active against Brine shrimp larvae (LD 50 : 125.663μg/mL). The dichloromethane aerial (TPAD) and root (TPRD) extracts exhibited significant antibacterial (78.03% and 50.21% inhibitions respectively) and phytotoxic (55% growth regulation at 1000μg/mL) potential. Only TPAD indicated the best inhibition against fungi; Aspergillus flavus (75.31%) and moderate inhibition against Microsporum canis (42.21%). This phytochemical and biological work is the first time reported in Trigonella polycerata.

Meloxicam (MEL) is an oxicam derivative with low water solubility that is useful in the treatment of colorectal cancer (CRC) as a COX-2 inhibitor. MEL-loaded HPMC micro particles were fabricated using an oil-in-oil (o/o) emulsion solvent evaporation (ESE) method. FTIR, XRD, particle size analysis, DSC, SEM and in vitro dissolution investigation were utilized to evaluate the produced micro particles physiochemically. Finally, rabbits were used as animal models in an in vivo pharmacokinetic study to assess the MEL concentration in the plasma of rabbits. Pure MEL, F1 and F2 were given to rabbits by a single dose for in vivo pharmacokinetic investigations. The XRD and DSC results confirmed the transformation of MEL from its crystalline nature to the amorphous state in micro particles. The formulations F1 and F2 particle sizes were determined 92.43μm and 163.26μm, respectively. The prepared micro particles had a smooth, non-porous and spherical surface. In comparison to the pure drug (22.4%), the F1 and F2 cumulative drug release (%) was 86.19% and 79.57%, respectively. Pure MEL, F1 and F2 have estimated C max values of 7.21, 25.41 and 22.38μg/mL, respectively. MEL had a half-life of 19.98 hours, which rose to 22.19 hours and 24.75 hours for F1 and F2, respectively. MEL, F1 and F2 had AUC0-α values of 116.034, 445.95 and 462.72μg/mL*h, respectively. Considering these aspects, MEL-loaded HPMC micro particles may have the potential to better the delivery and control the release of drug that is not easily dissolved in water which could lead to improved therapeutic efficacy and limited side effects.