CURCUMIN MICROENCAPSULATION USING CHITOSAN–ETHYL CELLULOSE–GMS MIXTURE FOR PRESERVATION OF MUCOADHESIVE PROPERTIES AND CONTROLLED RELEASE KINETIC

Objective: This research aimed to prepare curcumin microcapsules by the spray drying method and to evaluate their characteristics. Methods: The microcapsules were prepared by the spray drying method. The generated microcapsules were evaluated for organoleptic, morphology, particle size, the percentage of curcumin and water content. Furthermore, the release of curcumin from the microcapsules was tested in vitro and compared to uncoated curcumin powder. In addition, the mucoadhesive properties of uncoated curcumin powder and curcumin microcapsules were also evaluated. Results: The results showed that the microcapsules had spherical shape with particle size in the range of 100–1009 µm and water content of 9.34% (w/w) (FIII) and 8.09% (w/w) (FVI). The release of curcumin from its uncoated powder and the microcapsules FVI within 8 h were 8.87% and 26.32% (w/w), respectively. It was found that the mucoadhesive properties of microcapsules FVI were better than those of FIII and uncoated curcumin powder. Microcapsules FVI rendered the cumulative amount of curcumin remaining on the intestinal mucosa of 55% (w/w) within 3 h. Conclusion: Accordingly, curcumin microcapsules generated by spray drying could be further formulated into various solid dosage forms for a better therapeutic effect.

DESIGN, OPTIMIZATION, AND EVALUATION OF RAFT FORMING GASTRO RETENTIVE DRUG DELIVERY SYSTEM OF LAFUTIDINE USINGBOX–BEHNKEN DESIGN

Objective: The current research was aimed to formulate and evaluate raft forming gastro retentive floating drug delivery systems of Lafutidine for improving gastric residence time and sustained drug release for an extended time. Methods: Using Box–Behnken experimental design 17 formulations of lafutidine GRDDS were designed and evaluated for various parameters like physical appearance, pH, In vitro gelling study, in vitro buoyancy study, measurement of viscosity, density measurement, gel strength, drug content, acid neutralization capacity, the profile of neutralization, in vitro dissolution, release kinetic and stability studies. Results: All the evaluations were performed and observed that the values were within range, and the buoyancy lag time ranged within 14.76 to 25.84 sec and the formulations remained buoyant for more than 8h with the gelling time of 12h, the drug content was ranging from 98.96 to 99.55 %, and in vitro release was 86.86 to 99.34% by the end of 12h. The release kinetics followed zero-order with Higuchi’s model that indicating that drug release was found to be followed by the matrix diffusion process. Conclusion: Out of all formulations F3 was the optimized formulation and it was further characterized for FTIR, DSC, and stability studies, which exposed that there were no interactions amongst drug and excipients and no major change in the formulation and found to be stable.

Formulation and Evaluation of Cefaclor Extended-Release Tablet

Over past 30 years as the expanse and complication involved in marketing new drug entities have increased, with concomitant recognition of the therapeutic advantages of controlled drug delivery, greater attention has been focused on development of extended or controlled release drug delivery systems. In the present research work an attempt has been made to optimize, formulate and characterize extended-release tablet of Cefaclor. The preformulation studies were performed for the drug (e.g., physico-chemical properties, melting point, solubility etc.). The drug had shown the results under standard specifications. UV spectroscopic analytical method was also performed for quantitative determinations by plotting standard curve. Before this the pure drug was also scanned for the ƛ max value at different concentrations. The pre-compressions parameters and the post compression parameters for the nine formulated tablets were performed. The drug release study of the selected formulations EF3, EF6 and EF9 was performed as those formulations has shown the results within pharmacopoeia limits. The Formulation EF9 was then taken for release kinetic study as it has shown best results among the other three formulations. So, it confirms the drug release by Higuchi diffusion mechanism. From the results, conclusion can be drawn that the formulation consisting 10-12% concentration of hydroxypropyl methyl cellulose K4-M with 1% microcrystalline cellulose and 25% of lactose are considered as ideal for the optimized extended-release tablet formulation for Cefaclor. Keywords: Extended release, Cefaclor, Higuchi diffusion mechanism, PBP, bacterial cell wall synthesis.

Activation of Cadmium Under Simulated Solar Illumination and Its Impact on the Mobility of Cd in Flooded Soils

In waterlogged paddy soils, cadmium (Cd) can be precipitated as cadmium sulfide (CdS) under reductive environment, thereby limiting the absorption of Cd by plants. Multiple environmental factors (such as water, pH, Eh, etc.) played a role in the control of Cd mobility and bioavailability. In this study, we investigated the influence of the solar irradiation on the photo-dissolution of synthetic CdS-montmorillonite composites (CdS-M) in solution and the stability of Cdin natural soil. The release kinetic of Cd2+ showed that after the irradiation of simulated sunlight, CdS-M composites became less stable compared to the dark control. The solar irradiation seemed to enhance the release of Cd2+ from CdS significantly and continuously. Electron paramagnetic resonance (EPR) and quenching experiments confirmed that the photogenerated holes, O2·- and •OH were possibly involved in the photo-induced release of Cd2+, while the holes was primarily responsible for the reaction.Irradiation under alkaline solution or the presence of DOM, PO43-, CO32- and urea markedly inhibited the photodissolution process of CdS. The photo-mediated activation of Cd was further confirmed in paddy soil under natural sunlight, with a nearly 3-fold increase in concentration of extractable Cd during the 15 days irradiation. This study highlights the importance of photochemical transformation of Cd in the environmental water and soil.

β-Cyclodextrin-Modified Mesoporous Silica Nanoparticles with Photo-Responsive Gatekeepers for Controlled Release of Hexaconazole

In the present research, photo-responsive controlled-release hexaconazole (Hex) nanoparticles (Nps) were successfully prepared with azobenzene (Azo)-modified bimodal mesoporous silica (BMMs), in which β-cyclodextrin (β-CD) was capped onto the BMMs-Azo surface via host–guest interactions (Hex@BMMs/Azo/β-CD). Scanning electron microscopy (SEM) confirmed that the nanoparticles had a spherical structure, and their average diameter determined by dynamic light scattering (DLS) was found to be 387.2 ± 3.8 nm. X-ray powder-diffraction analysis and N2-adsorption measurements indicated that Hex was loaded into the pores of the mesoporous structure, but the structure of the mesoporous composite was not destroyed. The loading capacity of Hex@BMMs/Azo/β-CD nanoparticles for Hex was approximately 27.3%. Elemental components of the nanoparticles were characterized by X-ray photoelectron spectroscopy (XPS) and electron dispersive spectroscopy (EDS). Ultraviolet–visible-light (UV–Vis) absorption spectroscopy tests showed that the azophenyl group in BMMs-Azo undergoes effective and reversible cis-trans isomerization under UV–Vis irradiation. Hex@BMMs/Azo/β-CD Nps exhibited excellent light-sensitive controlled-release performance. The release of Hex was much higher under UV irradiation than that in the dark, which could be demonstrated by the bioactivity test. The nanoparticles also displayed excellent pH-responsive properties, and the sustained-release curves were described by the Ritger–Peppas release kinetic model. BMMs nanocarriers had good biological safety and provided a basis for the development of sustainable agriculture in the future.

Synthesis, Controlled Release, and Stability on Storage of Chitosan-Thyme Essential Oil Nanocapsules for Food Applications

The nanoencapsulation of thyme essential oil has been greatly important in food science, given its remarkable antioxidant and antimicrobial capacity. However, its analysis in storage has not been established in terms of physical stability, antioxidant capacity, and release studies. In this paper, chitosan-thyme oil nanocapsules were prepared by the ionic gelation method. These were characterized for differential calorimetry, release kinetic, and infrared spectroscopy. The chitosan-thyme oil nanocapsules were stored at 4 and 25 °C for 5 weeks, the changes in particle size, zeta potential, stability (diffuse reflectance), and antioxidant capacity were analyzed and associated with nanocapsules’ functionality. The results show that the storage time and temperature significantly modify the particle size (keeping the nano-size throughout the storage), the release of the bioactive was Fickian with t0.193 according to Korsmery & Peppas and best described by Higuchi model associated with changes in the zeta potential from 8 mV to −11 mV at 4 °C. The differential scanning calorimetry and infrared spectroscopy results confirm the good integration of the components. The antioxidant capacity revealed a direct relationship with residual oil concentration with a decrease in the ABTS test of 15% at 4 °C and 37% at 25 °C. The residual bioactive content was 77% at 4 °C and 62% at 25 °C, confirming nanoencapsulation effectiveness. The present investigation provides helpful information so that these systems can be applied in food conservation.

Design and Optimization of a Novel-Herbosomal Loaded PEG-Poloxamer Topical Formulation For the Treatment of Cold Injuries: A Quality By Design Approach

Cold injury/injuries can range from minor chilblain to extreme form of frostbite. Cold injuries are pathologically a combination of ice crystal formation in tissue with inflammation, thrombosis and ischemia to extremities, necessitating limb amputation in extreme cases due to tissue necrosis. Less severe forms of cold injuries can be managed by gentle rewarming of limb and avoiding exposure to cold leading to favorable outcomes, however severe forms of frostbite are a cause of major concern to patients as well as the treating physician. Due to lack of effective pre-treatment modalities and paucity of research in prophylaxis and therapeutics of cold injuries, we have developed a novel-herbosomal loaded PEG-Poloxamer topical formulation (n-HPTF) by Quality by Designed approach, incorporating natural ingredients which are having potential therapeutic effect for the treatment of cold injury in a form of a novel-lipid vesicles (herbosomes) loaded in polymers (PEG-3350 and Poloxamer-188) resulting excellent occlusive barrier and thus promote rapid healing. Optimized novel-herbosomes showed entrapment efficiency > 90% and < 300 nm mean particle size and in-vitro drug permeation of about 2 µg/cm2 followed by Higuchi’s release kinetic. Skin irritancy study on female Sprague Dawley rats showed no edema or erythema. In-vivo bio-efficacy study was performed and found significantly good at p-value < 0.05 when compared to the standard treatment groups.

FORMULATION AND IN VITRO–IN VIVO PHARMACOKINETIC EVALUATION OF CARDIOVASCULAR DRUG-LOADED PULSATILE DRUG DELIVERY SYSTEMS

Objective: This study is to formulate Nebivolol into a Pulsatile liquid, solid composite compression coated tablet, which will delay the release of the drug in early morning hypertension conditions. Methods: The liquid, solid composite tablet was formulated and compressed with the ethylcellulose coating polymer. The percent in vitro drug release of the liquid solid composite compressed tablet was tested. Based on disintegration time and wetting time, the LCS2, LCS3, LSC6, LCS7 and LCS12 formulations were found to be the optimized solid-liquid compacts fast-dissolving core tablet formulations, which may be excellent candidates for further coating with polymer to transfer into press coated pulsatile tablet formulations. Coating the core tablet with varying ethyl cellulose concentrations resulted in five different formulations of the pulsatile press-coated tablet (CT1, CT2, CT3, CT4, CT5). In vitro drug release, in vitro release, kinetic studies, in vivo pharmacokinetic and stability tests were all performed for the prepared pulsatile press coated tablet. Results: CT3 tablets are coated with ethyl cellulose polymer, which shows maximum controlled drug release from the core tablet i.e. 96.34±1.2% at 8th h. It shows there was an efficient delay in drug release form core tablet i.e. up to 3 h, followed by the maximum amount of drug release of 96.34±2.4 at 8h. Which shows the core drug will be more efficiently protected from the gastric acid environment 1.2 pH, duodenal environment 4.0 pH and release drug only in the small intestine. Conclusion: According to the findings, CT3 Pulsatile press-coated tablet increased the bioavailability of Nebivolol by 3.11 percent.

DEVELOPMENT, CHARACTERIZATION AND IN VITRO RELEASE KINETIC STUDIES OF IBANDRONATE LOADED CHITOSAN NANOPARTICLES FOR EFFECTIVE MANAGEMENT OF OSTEOPOROSIS

Objective: The objective of the present study was to develop, optimize, and evaluate Ibandronate-sodium loaded chitosan nanoparticles (Ib-CS NPs) to treat osteoporosis. Methods: NPs were prepared by the Ionic gelation method and optimized for various parameters such as the effect of concentration of chitosan, sodium tripolyphosphate (TPP), and pH effect on particle size polydispersity index (PDI), zeta potential, and entrapment efficiency. The prepared nanoparticles were characterized using particle size analyzer (DLS), transmission electron microscopy (TEM), scanning electron microscopy (SEM), and Fourier-Transform Infrared spectroscopy (FTIR). Results: Formulated NPs were obtained in the average nano size in the range below 200 nm in TEM, SEM, and DLS studies. The particle size and encapsulation efficiency of the optimized formulation were 176.1 nm and 63.28%, respectively. The release profile of NPs was depended on the dissolution medium and followed the First-order release kinetics. Conclusion: Bisphosphonates are the most commonly prescribed drugs for treating osteoporosis in the US and many other countries, including India. Ibandronate is a widely used anti-osteoporosis drug, exhibits a strong inhibitory effect on bone resorption performed by osteoclast cells. Our results indicated that Ibandronate sodium-loaded chitosan nanoparticles provide an effective medication for the treatment of osteoporosis.

Formulation and Development of Metoprolol Succinate Sustained Release Matrix tablet using Remusatia vivipara tubers mucilage

The purpose of this research was to formulate and evaluate sustained release tablet by using novel polymer Remusatia vivipara tubers mucilage. Currently natural gums and mucilages are being used extensively comparable to synthetic drug release modifiers. Natural plant materials possess various advantages. These are very cheap, biocompatible, biodegradable and free from side effects. In present research Metoprolol succinate matrix tablets were prepared by using Remusatia vivipara tubers mucilage. For the formulation of sustained release matrix tablets, direct compression method was used. The formulated matrix tablets were then evaluated for thickness, diameter, hardness, weight variation, friability, drug content, swelling index, in-vitro drug release and stability studies. The formulated sustained release tablet passed all tests required. The dissolution profile of prepared tablets showed sustained release of drug up to 11 hours compared to the reference tablet formulation PROLOMET XI 100. Drug release data were then fitted in to release kinetic models such as zero order kinetic, first order kinetic, Higuchi model and Korsmeyer-Peppas model to study the release pattern of drug from each formulation. The prepared sustained release tablet formulation was compared with marketed formulation (reference formulation) for drug release study and factor f1 (difference factor) and f2 (similarity factor) were determined. From this study it can be concluded that as the concentration of Remusatia vivipara mucilage increases, there is decrease in the rate of drug release from the formulation. The best formulation was found to be F3 which consists of 20% Remusatia vivipara mucilage but did not give comparable drug release profile to the reference formulation with factor f1 69.4 % and f2 34.8%. But it can be said that Remusatia vivipara gum mucilage can be used in tablet formulation to give sustained release effect up to 10 hours or in combination with other natural gum mucilage it may enhance the release retardant effect of drug up to or more than 20 hrs. The release kinetic study showed that the prepared sustained release tablet formulation shows anomalous (non-fickian) diffusion pattern and follows both diffusion controlled and swelling controlled mechanisms for drug release.