In vitro drug release and antibacterial activity evaluation of silk fibroin coated vancomycin hydrochloride loaded poly (lactic-co-glycolic acid) (PLGA) sustained release microspheres

Currently, the treatment of osteomyelitis poses a great challenge to clinical orthopedics. The use of biodegradable materials combined with antibiotics provides a completely new option for the treatment of osteomyelitis. In this study, vancomycin hydrochloride (VANCO) loaded poly (lactic-co-glycolic acid) (PLGA) microspheres were prepared by a double emulsion solvent evaporation method, and the in vitro drug release behaviors of the drug loaded microspheres were explored after coating with different concentrations of silk fibroin (SF). Drug loading, encapsulation efficiency, Scanning electron microscopy, particle size analysis, Fourier transform infrared spectroscopy, hydrophilicity, in vitro drug release, and in vitro antibacterial activity were evaluated. The results showed that the drug loading of vancomycin loaded PLGA microspheres was (24.11 ±1.72)%, and the encapsulation efficiency was (48.21 ±3.44)%. The in vitro drug release indicated that the drug loaded microspheres showed an obvious initial burst release, and the drug loaded microspheres coated with SF could alleviate the initial burst release in varying degrees. It also can reduce the amount of cumulative drug release, and the effect of microspheres coated with 0.1% concentration of SF is the best. The time of in vitro drug release in different groups of drug loaded microspheres can be up to 28 days. The microspheres coated with (0.1%SF) or without (0%SF) SF showed a cumulative release of (82.50±3.51)% and (67.70±3.81)%,respectively. Therefore, the surface coating with SF of vancomycin loaded microspheres can alleviate the initial burst release, reduce the cumulative drug release, potentially prolong the drug action time, and improve the anti-infection effect.

FORMULATION AND EVALUATION OF THYROID HORMONE (T4) IMMEDIATE RELEASE TABLETS

The aim of this research work is to formulate and evaluate Levothroxine sodium immediate release tablets prepared by direct compression method . Five formulations were evaluated for different pre and post compression parameter and in vitro drug release studies.The results of pre compression parameters of formluation 1 to 5 were compared with prescribed limits. It showed that formulation 1 to 5 powder blend exhibit good flow property and compressibility property. The disintegration time of all formulation was found to be in the range 2mins 09 secsto 4mins 03 secs.Thus, based on evaluation of different parameters it was concluded that formulation of immediate release tablet Levothyroxine sodium was successfully done and F-5 showed almost 93% drug release at 45 mins in Alkaline borate buffer( pH 10). Keywords: Thyroid hormone (T4), Immediate release tablets, Direct compression, Dissolution.

Development and Evaluation of Clove and Cinnamon Supercritical Fluid Extracts-Loaded Emulgel for Antifungal Activity in Denture Stomatitis

Denture stomatitis (DS), usually caused by Candida infection, is one of the common denture-related complications in patients wearing dentures. Clove and cinnamon oils have been acknowledged for their anti-inflammatory, antimicrobial activity, and antifungal effects in the oral cavity. The aim of this study, therefore, was to prepare clove/cinnamon oils-loaded emulgel and to assess its efficacy in treating Candida albicans-associated denture stomatitis. Central composite design was adopted to formulate and optimize clove/cinnamon extracts-loaded emulgel. The formulated preparations were assessed for their physical appearance, particle size, viscosity, spreadability, and in-vitro drug release. In addition, in-vivo therapeutic experiments were conducted on 42 patients with denture stomatitis. The prepared emulgel formulations showed good physical characteristics with efficient drug release within 3 h. In addition, in-vivo antifungal studies revealed that the optimized formula significantly (p < 0.001) reduced Candida colony counts from the denture surface, compared to commercially available gel (240.38 ± 27.20 vs. 398.19 ± 66.73 CFU/mL, respectively). Furthermore, the optimized formula and succeeded in alleviating denture stomatitis-related inflammation with a better clinical cure rate compared to commercially available gel Collectively, herbal extracts-loaded emulgel might be considered an evolution of polyherbal formulations and might represent a promising alternative to the existing allopathic drugs for the treatment of denture stomatitis, with better taste acceptability and no side effects.

FORMULATION AND DEVELOPMENT OF PRONIOSOMAL GEL FOR TOPICAL DELIVERY OF AMPHOTERICIN B

Objective: The present research work of Amphotericin B Proniosomal gel focuses on improving patient compliance by reducing the side effects of conventional intravenous injections and minimizing the problem of physical stability and to localize drug at site of action. Methods: Proniosomal gels are prepared by coacervation phase separation technique using different concentration of non-ionic surfactants (Span and Tween) for uniform vesicle formation, lecithin as permeation enhancer/membrane stabilizer and cholesterol as a vesicle cement providing prolonged release. Prepared gels were evaluated for their viscosity, pH, spreadability, entrapment efficiency, drug content uniformity, extrudability, in vitro drug release, permeability and stability studies. Results: Among the nine formulations, F2 (containing 10 mg drug, 250 mg Span 60, 50 mg Soya lecithin) was found to be promising. Fourier Transform infra-red (FT-IR) spectra studies represented no interaction and physicochemical characteristics were found within the limits. The percentages of drug content and entrapment efficiency were determined to be 95.16%±0.40 and 94.20%±0.20, respectively. In vitro drug release was about 95.72%±0.30. Conclusion: Proniosomal gel could constitute a promising approach for topical delivery of Amphotericin B by encapsulating it in non-ionic surfactant to provide patient compliance with cutaneous fungal infection, which was found to be safe, tolerable and efficacious.

Preparation of Tablet from Naagdon Plant by Wet Granulation Method for Treatment of Excessive Bleeding in Piles

The objective of present study was to formulate and evaluate the tablets for piles with different combination of herbal drugs. Material and Method: The tablet for piles containing lactose and mannitol as diluent and containing natural drugs like naagdon which was prepared by wet granulation method. The wet and compressed formulations were subject to several evaluation parameters like appearance, thickness, weight variation, hardness and friability. Results: The results of all evaluation parameters of piles tablet were within the acceptable limit. Pre-compression studies of piles tablet show satisfactory results. The thickness, hardness, weight variation, and friability of pilestablet were found to in acceptable range. The in-vitro drug release of eugenol from optimised for treatment piles formulation was found to be 90.23%. Significant results were obtained from present study. Discussion: The finding of current investigation clearly found that the health promotion of the body could be done by piles

Formulation and Evaluation of Nutraceutical Tablet Using Clove Drugs by Wet Granulation Method

The objective of present study was to formulate and evaluate the nutraceutical tablets with different combination of herbal drugs. Material and Method: The nutraceutical tablet containing lactose and mannitol as diluent and containing natural drugs like clove and cinnamon which was prepared by direct compression method. The compressed formulations were subject to several evaluation parameters like appearance, thickness, weight variation, hardness and friability. Results: The results of all evaluation parameters of nutraceutical tablet were within the acceptable limit. Pre-compression studies of nutraceutical tablet show satisfactory results. The thickness, hardness, weight variation, and friability of nutraceutical tablet were found to in acceptable range. The in-vitro drug release of eugenol from optimised nutraceutical formulation was found to be 90.23%. Significant results were obtained from present study. Discussion: The finding of current investigation clearly found that the health promotion of the body could be done by nutraceuticals. Keywords: Direct compression, Nutraceutical, Eugenol, In-vitro drug release

Sustained ophthalmic delivery of pH triggered Cromolyn sodium in situ gel

The research study intends to formulate pH triggered in situ gel of Cromolyn sodium composed of Polyacrylic acid (carbopol 934) polymer in combination with Hydroxypropyl Methylcellulose (HPMC K4M) polymer at 1:1, 1.5:1, 2:1 molar ratio by utilizing pH trigger method. Formulations were evaluated for pH, viscosity, gelling capacity, drug content and in vitro drug release. Results of Carbopol 934 and HPMC K4M based in situ gelling systems at 1:1, 1.5:1, 2:1 shown that the formulations were fluid state at room temperature in a formulated pH (pH 4.5) and went through fast progress into the viscous gel phase at the pH of the tear fluid 7.4. The viscosity of formulated pH triggered in situ gel at 2:1 molar ratio shown excellent result compares to 1:1, 1.5:1 molar ratio. The in vitro drug release of the developed in situ gelling formulations at 1:1, 1.5:1, 2:1 molar ratios increases the contact time and showed a non – fickian diffusion type of release behavior with 94.45%, 83.26%, 70.48% respectively over 8 hours periods compared with that of marketed formulation that shows 99.4% over 4 hours. Thus, the developed system at 2:1 molar ratio acts as a viable alternative to conventional eye drops and also prevent the rapid drainage.

Enhancement of Aqueous Solubility, Dissolution Profile, and Oral Bioavailability of Pentoxifylline by Microsponges

Microsponge, a novel drug delivery system, is designed to deliver a pharmaceutically active ingredient efficiently at the minimum dose. Microsponge plays an important role in enhancing drug stability, reducing side effects, and modifying drug release profiles. It is mostly used for transdermal delivery. Recent studies also explored their use for oral administration. This study aimed to explore the potential use of the microsponge technique in improving the aqueous solubility and dissolution profile of pentoxifylline (PTX). In this study, microsponges were prepared by a quasi-emulsion solvent diffusion method by varying concentrations of carriers. Nine different ratios of the PTX:Eudragit E-100 with varying amounts of dichloromethane were used. All formulated microsponges were evaluated for %production yield, compatibility of drug excipient, encapsulation efficiency, in vitro drug release, and in vivo bioavailability, as well as recorded by scanning electron microscopy (SEM) and differential scanning calorimetry(DSC). Our data suggested that the aqueous solubility of PTX microsponges was four times greater than that of pure drug. The in vitro drug release of selected microsponges (M8) was found to be 70%; furthermore, the in vivo study suggested that the selected formulation significantly enhanced drug concentration in the plasma (9,219 ng/mL in 12 hours) in comparison to pure drug PTX (2,476 ng/mL in 12 hours). SEM showed that the prepared microsponges were spherical with porous nature. Fourier-transform infrared spectroscopy and DSC studies confirmed an absence of incompatibility among drugs and selected excipients. The pH of the selected gel was found to be 6.8, which was compatible with those of skin and oral formulations also. All above data suggested a highly successful and beneficial use of the microsponge technique in enhancing aqueous solubility, dissolution profile, and oral bioavailability of PTX. Microsponge-based delivery of PTX may represent an alternative strategy to improve the bioavailability of the drug.

Studies on Preparation and Evaluation of Soluble 1:1 Stoichiometric Curcumin Complex for Colorectal Cancer Treatment

This study investigates the complex of curcumin (CMN), which has enhanced solubility and hence, higher cytotoxicity compared to free CMN. Insilco molecular modelling and phase solubility (PS) studies were performed with the drug and carriers for interaction. The complex was characterized by in vitro drug release, FT-IR, PXRD, TGA, DSC, SEM, DLS, and functionalized dyeing test. The result showed that the CMN-PEG6000 complex produced significant properties of solubility (≈ 190 folds) and dissolution (80.68 % at 30 min), with stability constants equivalent to 309 and 377 M-1 at 25 and 37 °C, respectively. It exhibited AL type of isotherm indicating 1:1 stoichiometry. The result from the in vitro cytotoxicity showed that 50 % inhibition (IC50) was achieved on the SW480 and Caco-2 cells at an amount of complex that was considerably lesser than free CMN. Apoptosis study showed that the cells underwent cell death mainly by apoptosis with a small number by necrosis. HIGHLIGHTS Enhanced curcumin solubility up to 190 fold higher than pure curcumin was investigated The phase solubility results of curcumin range from 5.7×10-4 M-1 and 7.8×10-4 M-1 at 25 and 37 °C, respectively First time of novel dyeing test was performed with complex of curcumin, signified its solubility This study provides useful approach for obtaining curcumin products with maximum aqueous solubility GRAPHICAL ABSTRACT

Frovatriptan Succinate Loaded Lipid Nanoparticles: Formulation, Evaluation, Stability Study and Shelf Life Determination

Aims: The aim of the research work was to prepare and optimize the Frovatriptan Succinate (FVN) loaded solid lipid nanoparticles. Methods: SLNs were developed by solvent emulsification diffusion technique and evaluated for particle size, PDI, zeta potential, in-vitro drug release, and finally stability study was conducted for the detection of shelf life. Results: The optimized formulation exhibited particle size, PDI, and zeta potential 122.85±9.24 nm, 0.129 and -25.85 mV, respectively. In-vitro drug release study exhibited biphasic drug release pattern. Initially (in first two hrs) the drug was release in fast manor i.e. burst release (32.36±7.28 %). It might be due to the presence of drug on the surface of SLNs. After 2 hrs of study, the release pattern became sustained up to 24 hrs. The total amount of drug release in 24 h was found to be 91.29 ± 8.26%. Various kinetic models were applied to evaluate the release pattern of the drug form the formulation. Higuchi model was found to be the best fitted with the R2 value of 0.9482. The release mechanism was found to be the Fickian type with the release exponent (n) value of 0.4386. Finally, stability study was conducted. The formulation was found to be the stable under the studied conditions. The shelf life of the formulation was found to be 1.77 years. Conclusion: Finally, it could be concluded that, the SLNs are the suitable carrier for the delivery of FVN .