Ionotropic Gelation Technique Research Articles

Synthesis of agro-industrial wastes/sodium alginate/bovine gelatin-based polysaccharide hydrogel beads: Characterization and application as controlled-release microencapsulated fertilizers

Synthesis of novel agro-industrial wastes/sodium alginate/bovine gelatin-based polysaccharide hydrogel beads, micromeritic/morphometric characteristics of the prepared formulations, greenhouse trials using controlled-release microencapsulated fertilizers, and acute fish toxicity testing were conducted simultaneously for the first time within the scope of an integrated research. In the present analysis, for the first time, 16 different morphometric features, and 32 disinct plant growth traits of the prepared composite beads were explored in detail within the framework of a comprehensive digital image analysis. The hydrogel beads composed of 19 different agro-industrial wastes/materials were successfully synthesized using the ionotropic external gelation technique and CaCl2 as cross-linker. According to micromeritic characteristics, the ionotropically cross-linked beads exhibited 77.86 ± 3.55 % yield percentage and 2.679 ± 0.397 mm average particle size. The dried microbeads showed a good swelling ratio (270.02 ± 80.53 %) and had acceptable flow properties according to Hausner's ratio (1.136 ± 0.028), Carr's index (11.94 ± 2.17 %), and angle of repose (25.03° ± 5.33°) values. The settling process of the prepared microbeads was observed in the intermediate flow regime, as indicated by the average particle Reynolds numbers (169.17 ± 82.81). Experimental findings and non-parametric statistical tests reveal that dried fertilizer matrices demonstrated noteworthy performance on the cultivation of red hot chili pepper plant (Capsicum annuum var. fasciculatum) according to the results of greenhouse trials. Surface morphologies of the best-performing fertilizer matrices were also characterized by Scanning Electron Microscopy. Moreover, the static fish bioassay experiment confirmed that no abnormalities and acute toxic reactions occurred in shortfin molly fish (Poecilia sphenops) fed with dried leaves of red hot chili pepper plants grown with formulated fertilizers. This study showcased a pioneering investigation into the synthesis of microcapsules using synthesized hydrogel beads along with digital image processing for bio-waste management and sustainable agro-application.

Innovative bile acid-cationic polymer nanoparticles in gene delivery: Cellular transfection relevant to eye, ear, and kidney cells

Gene therapy is an emerging treatment approach rapidly gaining broad interest across various pathologies. One common pitfall with gene therapy is the challenge of effective delivery, as current modalities suffer from poor safety and efficacious profiles. Polymer nanoparticles represent a novel method for the delivery of genes. Accordingly, this study developed novel polymer nanoparticles for the effective delivery of a reporter plasmid. Polymer nanoparticles were prepared by an ionotropic gelation technique with sodium alginate and cationic polymers; poly-L-lysine and chitosan. Bile acid excipients were incorporated for their therapeutic and permeation-enhancing properties. The nanoparticles were analyzed for physical properties including size, and charge as well as their safety and efficacy profiles. Eight nanoparticle formulations were prepared in the present study. Generated particles had a negative charge and particle size of between 100 and 400 nm. Particles also showed good biocompatibility against the cell lines tested, with acceptable survival at 0.5 mg/ml treatment concentration. Transfection efficiency however remained challenging. The addition of bile acid did improve transfection efficiency in some of the cell lines evaluated. Although suitable safety and physical characteristics were demonstrated in the investigated nanoparticles, further work involving formulation optimisation is required to improve transfection efficiency.

Calendula Oil Associated Dexibuprofen Nanoformulation Transdermal Patches: Formulation and Characterization

Objectives: To prepare and characterize the nanoparticle-based topical formulations of dexibuprofen in combination with calendula oil to enhance the topical anti-inflammatory effect. Methods: Chitosan and tri poly phosphate (TPP) were used to prepare nanoparticles developed utilizing the ionotropic gelation technique and analyzed by scanning electron microscope (SEM) and the ZS. Solvent casting was used to prepare the transdermal medication delivery system for the chitosan nanoparticle formulation. Results: Results revealed that nanoparticles were between the sizes of 267.3 nm. This particle size may enhance the drug’s solubility and penetration through the skin. These patches containing chitosan nanoparticles were produced utilizing polymer combinations - HPMC, chitosan, and PEG400 with tween80 as plasticizers. Accompanying the rise in hydrophilic polymer content came an increase in the rate of medication release via the patch. Conclusion: Transdermal patch - F3 released the drug reasonably well.

Formulation Development and Evaluation of Floating Beads of Propranolol Hydrochloride

Purpose: The purpose of present research work was to prepare sodium alginate and pectin antihypertensive floating beads of propranolol hydrochloride. Methods: Floating beads were prepared by using Ionotropic gelation technique using various natural and synthetic polymers in different proportion like sodium alginate, pectin, hydroxy propyl methyl cellulose k4m and calcium carbonate. Result: The floating beads were formulated and evaluated to physiochemical studies, Entrapment efficiency, swelling index, Invitro drug release, drug content, buoyancy studies (Floating time, floating lag time, total floating time) on the basis of evaluation of all floating beads were show good results. Conclusion: It Concluded that floating drug delivery system are float immediately upon contact with gastric fluid for increasing the bioavailability of drug and patient compliance.

EFFECT OF POLYMER CONCENTRATION AND SURFACTANTS ON PHYSICAL CHARACTERISTICS, DRUG RELEASE AND ANTIOXIDANT ACTIVITY OF GLUTATHIONE-KAPPA CARRAGEENAN NANOSPHERES

Objective: Glutathione is one of the antioxidants widely used as an antiaging and skin lightener. Glutathione at a dose of 250 mg/d orally proved useful as an antiaging. At the same time, glutathione topical night cream is effective at a dose of 0.1% for the skin of Indonesian women. Glutathione is one of the antioxidants that has easily oxidized properties in storage. Research purpose to optimize the concentration of kappa carrageenan polymer and surfactan to obtain the optimal physical characteristics of nanosphere system analyzed based on size, PDI, yield, drug loading, entrapment efficiency, dissolution and antioxidant activity. Methods: The most commonly used method of making nanospheres is ionotropic gelation because it has proven effective, easy, and easy to apply. Ionotropic gelation is depend on the tendency of polyelectrolytes to cross connect to develop hydrogel beads often called gelispheres in the existence of counter ions. Nanospheres were prepared by aerosolization ionotropic gelation technique followed by freeze-drying. This method uses carrageenan polymers of 0.5% and 1.0% with the addition of surfactant as a stabilizer. Evaluation parameters are particle size, entrapment efficiency, drug loading, drug release and antioxidant activity. Results: The results of the nanospheres obtained were tested physically and drug activity. Nanospheres successfully formed, with size 382.67±52.24 nm, F2 325.20±4.62 nm, F3 495.39±30.61 nm, and F4 409.80±4.11 nm. The greater the polymer concentration, the greater the value of entrapment efficiency and drug content in the nanosphere. The morphology of the nanosphere is quite good, spherical, with a smooth surface. The release profile shows that glutathione release is quite good but takes a long time, namely F1 73.91±2.17%, F2 75.91±2.76%, F3 78.56±2.82%, and F4 79.56±1.34% in 480 min or 8 h. Antioxidant activity of glutathione-Kappa carrageenan nanospheres with the DPPH method showed that nanospheres have medium or medium category antioxidant activity. Conclusion: The most optimal formula is F4 with 1% kappa-carrageenan concentration and 0.6% KCl.

Developing and Evaluating a Novel Drug Delivery System, Calcium-Alginate Beads loaded with Valsartan

Valsartan is one of the most common drugs used by chronic patients in the management of hypertension, heart failure, and diabetic nephropathy. This present study was conducted with the aim of formulating a long-acting pharmaceutical form by preparing millimeter dimensions’ solid polymeric beads using the Ionotropic Gelation technique by using the polymer “Alginate Sodium” (SA), and Calcium Chloride CaCl2 as a cross-linking agent. Prepared valsartan beads succeeded in the possibility of decreasing dose administration and therefore, reduced immediate release side effects of conventional forms of Valsartan. Valsartan beads were studied using different concentrations of Sodium Alginate and Calcium Chloride to select the optimal formula and then were compared with locally marketed film-coated tables containing Valsartan. The formula (SA 3%, CaCl2 10%) was chosen after conducting several physiochemical tests such as shape and dimensions, swelling index, entrapment efficiency, in vitro drug release, and FTIR. FTIR test showed no chemical bonding between Valsartan and other excipients. Selected beads achieved a high percentage of swelling in phosphate buffer solution pH=6.8. Entrapment efficiency was also high at about 80%. Prepared beads followed the Korsmeyer-Peppas release mechanism, and eventually obtained extended-release beads which slowed drug release for 24h, Compared with the film-coated tablets, the in vitro release of valsartan expired after only one hour.

PREPARATION AND EVALUATION OF COLON-SPECIFIC PROBIOTIC DELIVERY SYSTEM: SACCHAROMYCES BOULARDII

Probiotics are beneficial microbes that have a beneficial effect on humans as well as animals. Despite their advantages, probiotics face viability challenges during storage and while passing through the upper gastrointestinal tract. This study was designed to develop an encapsulated system of Saccharomyces boulardii (SB) probiotics to overcome challenges with oral administration and develop a colon-targeted delivery system. Pectin and sodium carboxy methyl cellulose encapsulated microbeads of probiotics: polymer ratio (1:1, 1:2, and 1:3) were prepared using the ionotropic gelation technique and then coated with Eudragit® S 100 and cellulose acetate phthalate. They were then evaluated for efficacy and compared for bead size, flow properties, entrapment efficiency, percent yield, swelling index, mucoadhesive ness, in vitro release and viability of probiotics. The microencapsulated probiotics showed higher viability in the colon as compared to gastric and intestinal environments. Hence, microencapsulation is a potential delivery system for the administration of viable probiotics

Chitosan and Anionic Solubility Enhancer Sulfobutylether-β-Cyclodextrin-Based Nanoparticles as Dexamethasone Ophthalmic Delivery System for Anti-Inflammatory Therapy.

Cataract surgery interventions are constantly increasing, particularly among adult and elderly patients. This type of surgery can lead to inflammatory states of the ocular anterior segment (AS), usually healed via postoperative treatment with dexamethasone (DEX)-containing eye drops. The application of eye drops is challenging due to the high number of daily administrations. In this study, mucoadhesive nanoparticles (NPs) were formulated to improve the residence time of DEX on the corneal mucosa, enhancing the drug's solubility and bioavailability. The NPs were generated using an ionotropic gelation technique, exploiting the interaction between the cationic group of chitosan (CS) and the anionic group of sulfobutylether-β-cyclodextrin (SBE-β-CD). The formation of the inclusion complex and its stoichiometry were studied through phase solubility studies, Job's plot method, and Bi-directional transport studies on MDCKII-MDR1. The obtained NPs showed good chemical and physical characteristics suitable for drug loading and subsequent testing on animal mucosa. The DEX-loaded CS/SBE-β-CD NPs exhibited a prolonged residence time on animal mucosa and demonstrated enhanced drug permeability through the corneal membrane, showing a sustained release profile. The developed NPs posed no irritation or toxicity concerns upon local administration, making them an optimal and innovative drug delivery system for inflammatory AS diseases treatment.

Development of Anthocyanin-Rich Gel Beads from Colored Rice for Encapsulation and In Vitro Gastrointestinal Digestion.

Colored rice anthocyanins are water-soluble natural pigments that can be used as an active ingredient in healthy food and pharmaceutical products. However, anthocyanin utilization is limited because of its instability. This work produced anthocyanin-rich gel beads from colored rice using a modified ionotropic gelation technique for encapsulation, and their efficacy was studied in vitro in the gastrointestinal tract. In total, 15 colored rice samples of three types (whole grain rice, ground rice, and ground germinated rice) were screened to identify the highest anthocyanin content. The anthocyanin content of the whole grain rice was significantly (p < 0.05) higher than it was in the ground and ground germinated rice. The sample with the highest anthocyanin content (1062.7 µg/g) was the black glutinous rice grain from Phrae, chosen based on its anthocyanin-rich crude extract. A new formula using a modified ionotropic gelation technique was prepared for the inclusion of the extract in gel beads. The results indicated that the incorporation of oil and wax significantly increased the encapsulation efficiency of the gel beads (% EE value of 85.43%) and improved the bioavailability of the active ingredient. Moreover, after simulated digestion, the release of anthocyanin and total phenolic content occurred more than five times. Scanning electron microscopy revealed that the surface of the gel beads was smooth. Furthermore, the presence of polyphenols and polysaccharides in the gel beads was confirmed using FTIR. The oil-wax-incorporated, anthocyanin-rich gel beads could be implemented for antioxidant delivery into the gastrointestinal tract to further improve healthy food and nutraceutical products.

Pharmacokinetics evaluation of newly formulated beads alginate/gum acacia loaded ketoconazole in rabbit plasma by oral administration.

The combination of alginate and gum acacia in previous studies showed good results in inhibiting ketoconazole precipitation due to the supersaturation phenomenon. Ketoconazole-loaded alginate and gum acacia can produce hydrogel beads through cross-linking with Ca2+ using ionotropic gelation techniques. However, the pharmacokinetic study of the ketoconazole beads loaded to alginate and gum acacia needs further investigation. This study aimed to evaluate pharmacokinetic parameters using rabbits via oral administration. The drug was administered orally to 2 groups of rabbits: pure ketoconazole (KTZ) and formulation of ketoconazole (AG75) groups. Blood samples were obtained from the ear marginal vein at various time points: 0 (before administration), 15, 30, 45, 60, 90, 120, 150, 180, 240, 300, 360, and 420 minutes after oral dosage. The pharmacokinetic study employed a non-compartment analysis to calculate the area under the curve (AUC), the volume of distribution (Vd F-1), clearance (Cl F-1), maximum concentration (Cmax), and time to reach maximum concentration (tmax). The data obtained from the parameter result was analyzed using the independent-sample T-test. The results of the KTZ group include AUC of 15.83±0.62 h μg mL-1, VdF-1 of 8.95±1.17 mL, ClF-1 of 3.45±0.3 mL h-1, Cmax of 4.7±0.69 μg mL-1, and tmax of 1.67±0.17 h. The results of the AG75 group include AUC of 27.8±1.01 h μg mL-1, VdF-1 of 11.5±2.4 mL, ClF-1 of 2.15±0.11 mL h-1, Cmax of 4.49±0.52 μg mL-1, and tmax of 2.5±0.5 h. The formulation incorporating ketoconazole beads resulted in a higher AUC0-∞ than the pure ketoconazole. This finding suggests that the created formulation has enhanced the bioavailability of ketoconazole.

Formulation of Glutathione-Alginate Microspheres for Diabetes Mellitus Dietary Supplementation

The microsphere is a multi-molecule drug conveyance framework made to accomplish controlled drug conveyance to further develop bioavailability and dependability and target medications to explicit destinations at a given rate. Glutathione as a model for microspheres as dietary supplementation can restore GSH synthesis and lower oxidative stress and oxidant damage in the face of persistent hyperglycemia. The biomedical utilization of glutathione stays restricted because of its moderately short half-life, shaky properties, fast digestion, discharge, and high hydrophilicity. Hence, the motivation behind this study was to get ready GSH utilizing a microsphere with polysorbate 80 and sorbitan monooleate 80, beat skin obstruction capability, and research the properties and delivery profile of GSH-stacked alginate microspheres. It was to do. GSH microspheres were ready by ionotropic gelation technique. The produced microspheres were broken down in vitro for the proficiency of ensnarement (EE%), drug stacking (DL%), molecule size, yield, and medication discharge profile to acquire a streamlined plan. The pre-arranged GSH Microspheres had a high EE% going from (41.50 ± 1.12%) for F1 to (50.36 ± 0.86%) for F2, with little molecule sizes running (2.02 ± 0.09 µm) for F1 to (2.19 ± 0.16 µm) for F2, and drug stacking going from (5.81 ± 0.13%) for F1 to (6.15 ± 0.09%) for F2. The transition profile was tracked down in the scope of 0.018 ± 0.001 µg/cm2/h to 0.030 ± 0.002µg/cm2/h. GSH microspheres were ready by aerosolization utilizing the ionotropic gelation strategy. The GSH microspheres were assessed in vitro for the effectiveness of entanglement (EE%), drug stacking (DL%), molecule size, yield, and medication discharge profile to acquire a streamlined plan

Development and Comparative Analysis of Metronidazole Microspheres Prepared with Different Combinations of Polymers Using Ionotropic Gelation Technique

Development and Comparative Analysis of Metronidazole Microspheres Prepared with Different Combinations of Polymers Using Ionotropic Gelation Technique

Optimization and In Vitro Evaluation of Curcumin-loaded Calcium Alginate Microbeads using Box-Behnken Design for Colorectal Cancer

Background and Objective:: After lung cancer and breast cancer, colorectal cancer (CRC) is the third most common type of cancer and has the second-highest fatality rate. Curcumin is one such naturally occurring dietary compound that demonstrated promise to treat colon cancer. For that, the goal of the current study was to coat curcumin with Eudragit S100 to treat colorectal cancer in the distal intestine release. The multiparticulate dosage form can increase the solubility of curcumin in the colon environment, sustain the drug release, and protect the drug from abrupt degradation in the colon environment. All of these alterations can enhance the colon tissue levels, especially in the colon cancer cells in the patients, and thereby can enhance the utility of the therapy. Methods:: By using the ionotropic gelation technique, the formulations were made. Moreover, Design Expert 13 used a three-factor, three-level Box-Behnken design (BBD) in this work to optimize the formulation for colon-targeted drug delivery. The concentration of potassium alginate, the concentration of calcium chloride, and the curing duration were considered independent variables, and prepared microbeads were refined to study their impacts on entrapment effectiveness and particle size. Eudragit S100 was enteric coated on Calcium alginate beads with an improved core. Results:: Regarding particle size and entrapment effectiveness, respectively, the polymer concentration and curing duration had a substantial impact. The ideal concentrations of calcium chloride and potassium alginate were 15% w/v and 6% w/v, respectively, with a 20-minute curing time. With a drug entrapment efficiency of 88.4%, the improved formulation had particles with a size of 708 μm. After 12 hours, 79.23±0.32% of the drug was released following an enteric coating of Eudragit S100 of optimized calcium alginate microbeads (10% weight gain). Conclusion:: The present study conclusively demonstrates the usefulness of a Box-Behnken design in the optimization of colon-targeted formulations. To effectively treat colorectal cancer, enteric-coated calcium alginate microbeads can be administered orally to deliver curcumin precisely to the colon.

Development and optimization of in-situ gel containing chitosan nanoparticles for possible nose-to-brain delivery of vinpocetine

Vinpocetine (VIN), a derivative of vincamine found in the vinca plant, widens blood vessels in the brain and has been shown to improve cognitive function, memory, and cerebrovascular disorders. Nevertheless, the clinical utility of VIN is constrained by factors such as low oral bioavailability owing to the first-pass metabolism that often demands frequent dosing of 3–4 tablets/day. In this regard, the present work aimed to develop VIN-loaded chitosan nanoparticles (VIN-CH-NPs) to surmount these limitations and in view to enhance delivery to the brain of VIN by minimizing systemic exposure. The chitosan (CH) nanoparticles (NP) were developed by ionotropic gelation technique employing tripolyphosphate (TPP) as a cross-linking agent. Employing Design of Experiments (DoE), the effect of CH and TPP concentrations and stirring speed were systematically optimized using Box Behnken design (BBD). The optimized batch of nanoparticles displayed a particle size, zeta potential, entrapment efficiency, and drug loading of 130.6 ± 8.38 nm, +40.81 ± 0.11 mV, 97.56 ± 0.04 %, and 61 ± 0.89 %, respectively. Fourier Transform Infrared Spectroscopy indicated the chemical integrity of the drug ruling out the interaction between the VIN and excipients used. DSC and PXRD data indicated that reduction of the crystallinity of VIN in the chitosan matrix. These VIN-CH-NPs manifested good stability, exhibiting an almost spherical morphology. To mitigate rapid mucociliary clearance upon intranasal administration, the optimized VIN-CH-NPs were incorporated into thermosensitive in situ gel (VIN-CHN-ISG). It was observed that the in-situ gel loaded with nanoparticles was opalescent with a pH level of 5.3 ± 0.38. It was also noted that the gelation temperature was 32 ± 0.89 °C, and the gelation time was approximately 15 s. The drug delivery to the brain through the nasal application of optimized VIN-NPs in situ gel was assessed in rats. The results indicated significant nasal application of the in-situ gel nearly doubled the Cmax (P < 0.05) and AUC0-t (P < 0.05) in the brain compared to oral administration. Nasal administration improved drug delivery to the brain by reducing systemic exposure to VIN. A histopathological study of the nasal mucosa revealed no irritation or toxicity, making it safe for nasal administration. These findings suggest that the developed NPs in-situ gel effectively targeted vinpocetine to the brain through the nasal pathway, providing a potential therapeutic strategy for managing Alzheimer's disease.

Fabrication, Characterization and in vitro Evaluation of Prednisolone Sustained Release Multiparticulate System for Colonic Targeting

Background: Prednisolone (PRD) is orally prescribed for inflammatory bowel syndrome (IBS) as the upper GIT is the main site of absorption; therefore, long-term PRD dosing decreases therapeutic effectiveness through systemic side effects. Objective: This work focused on formulating sustained-release alginate beads as a multiparticulate system for colon targeting using prednisolone (PRD) to be filled in an HPMC capsule. Methods: PRD beads were prepared by the ionotropic gelation technique using sodium alginate as the primary polymer and inulin, guar gum, and pectin as secondary polymers. In addition to the impact of polymer type and quantity, other factors were investigated: The CaCl2 concentration and tween 80 addition Thirteen formulations were successfully prepared, and their properties, such as bead size, morphology, percentage of encapsulation efficiency, yield, DL, in vitro release study in GIT buffer media, IBS media, SEM, and FTIR, were assessed. Results: The study showed that the beads were close in size, and the size was not an obstacle for loading the beads in HPMC capsules. Further, yield%, EE%, and DL% increased according to the bead’s content increase. Conclusions: The optimum formula was F3 that coated HPMC capsules with Eudragit S-100, which gave sustained release profiles in GIT and IBS simulating media, and F13 that could last the release in different pH media, pH 1.2, 6.8, and 7.4.

Synergistic Effect of Linezolid Incorporated Chitosan Nanoparticles in Restorative Dental Cements – A Promising Dental Formulation.

Chitosan is considered one of the best materials for use as a drug delivery vehicle. Chitosan is incorporated into dental cement to enhance its properties. Previous investigators have found its antibacterial activity near dental restorations, which was insufficient to produce a clinically significant effect. Hence, the incorporation of various antibacterial agents was proposed. Linezolid is one of the oldest drugs in the oxazolidinone antibiotics category, approved by the US FDA in 2000. It is used to treat various antibiotic-resistant bacterial infections. However, there needs to be more literature regarding using linezolid with chitosan. Current research aims to prepare and characterize chitosan nanoparticles with linezolid for use in dental cement. Chitosan nanoparticles were prepared using the ionotropic gelation technique. They were incorporated with Linezolid, and samples were analyzedby FTIR spectroscopy, Particle size analysis, Transmission Electron Microscopy, High-performance liquid chromatography analysis, antibacterial activity, and biocompatibility. Linezolid was successfully incorporated into chitosan. Chitosan's FTIR spectrum reflected the functional groups present in chitosan, and their peaks were superimposed in the presence of linezolid. Both chitosan and chitosan with linezolid had similar particlesizes (142nm). Linezolid was released from chitosan effectively on the 1st and 7th days (19.78 and 144.14μg/ml). The formulation showed antibacterial activity and was not cytotoxic to cells. Thus prepared linezolid incorporated chitosan is a promising material to be used as an antimicrobial agent in dental cement. Its bio-physico-chemical properties are promising for use in dental cement. In the future, these linezolid-loaded chitosan nanoparticles may be added to various restorative materials.

Bioactivity of Nanohybrid: Comprising of Metallosalen Incorporated into Lacunary Polyoxometalate and Encapsulated with Chitosan Biopolymer

Biocompatible polymer chitosan has note-worthy applications in biomedical science. Nanohybrids synthesized by using chitosan as an encapsulating unit for polyoxometalates (POMs) and study of its biomedical applications is a fast-emerging field. In this research work, a lacunary polyoxometalate (α-K8SiW11O39) has been synthesized and then alkylsilane has been inserted into its lacunary position. It has been then reacted with 2-hydroxy-1-naphtaldehyde followed by copper metalation and finally encapsulated into chitosan by using the ionotropic gelation technique, in which the chitosan and the POM served as cation and anion, respectively. The bands in UV-Vis spectra at characteristic wavelength indicate that the organosilane is successfully inserted into α-K8SiW11O39 and metalled with Cu. Then its encapsulation into chitosan to synthesize final nanohybrid has been confirmed by UV-Vis spectra. Further, chitosan, POM inserted with organosilane and nanohybrid have been characterized by FT-IR. EDX analysis reveals the presence of all the expected elements in their desired ratios. EDX study was further supported by Inductively Coupled Plasma (ICP) technique. Morphology of nanohybrid has been studied by Scanning Electron Microscope (SEM) imaging. The loading and entrapment efficiency of the prepared nanohybrid was exceptionally excellent and was calculated to be 81.2% and 59.1%, respectively. In vitro drug release study suggested sustainable and pH-modulated release behaviour of the nanohybrid. Further, it is the first time that an organosilane attached to lacunary POM, then metalated with Cu and finally encapsulated into CS has been investigated for drug delivery. The antibacterial activity of POM inserted with organosilane and nanohybrid have been tested against bacterial strains of B. subtilis gram (+)ve and E. coli gram (-)ve. The antibacterial activity of nanohybrid has been improved as compared to bare POM inserted with metallated organosilane and chitosan.

Preparation and Evaluation of Aceclofenac microsphere containing Natural gum

Aceclofenac is an oxyacetic and non-steroidal anti-inflammatory drug which has a half-life of 4 h. Aceclofenac is used to reduce fever, inflammation of rheumatoid arthritis, traumatic pain etc. Aceclofenac has higher anti-inflammatory action than conventional NSAIDs. Development of aceclofenac microsphere is carried out to achieve sustained release of the drug after administration. The objective of this study was to find out the role of natural gum (Guar gum) for the preparation of microspheres. So, the amounts of natural gum were increased in various formulation at a successive rate. Aceclofenac microsphere is microencapsulated with guar gum and sodium alginate by Ionotropic gelation technique. There are various formulations of microspheres are developed. The prepared microspheres were spherical in shape, white in color and free flowing. Formulated microspheres were characterized for particle size, entrapment efficiency and in vitro drug release study. The aceclofenac microsphere showed particle size ranging from 330±10µm to 210±11µm 86.5% drug entrapment efficiency. The in vitro drug release is carried out up to 9 h in pH 6.8 phosphate buffer solution. F5 formulation showed maximum drug release of about 95.40% after 9 hour.

Production of chitosan complexes with 3ʹ,5ʹ-сyclic diadenosine monophosphate

To solve the problem of delivering pharmacologically promising 3ʹ,5ʹ-cyclic diadenosine monophosphate (cyclo-diAMP) to target cells in humans and animals, the complexes of the above-mentioned dinucleotide with natural polymer – chitosan were originally synthesized by ionotropic gelation technique. It was found that the binding degree of cyclo-diAMP to this biopolymeric carrier reaches 60 %; wherein the capacity of the obtained complexes with respect to the dinucleotide is 800–860 µg/mg of the produced complex. Cyclo-diAMP has also been shown to elute from the chitosan complex to the citrate-phosphate buffer (pH 7.4) up to 36 % by 21 hours. The obtained results testify in favor of potential application of cyclodiAMP complex with chitosan for prolonged delivery of the studied cyclic dinucleotide to target cells.

Alginate-bentonite composite decorated by chitosan-folate conjugate for the oral delivery of 5-Fluorouracil

In this work, a novel alginate-modified Na-Bentonite clay composite (APTSB-AL) was synthesized via an ionotropic gelation technique for the controlled delivery of 5-Flurouracil. Characterization of the composite was performed using Fourier transform infrared spectroscopy (FTIR): X-ray diffraction (XRD): scanning electron microscopy (SEM) etc. In order to acquire the targeted drug delivery, the composite was covered by chitosan-folate conjugate (APTSB-AL-CSFA). The freeze-drying method was adopted to avoid the leakage of water-soluble drug molecules during the drying process. The maximum swelling of the composite was found to be at pH 6.8 and the maximum drug release was at pH 7.4. The release kinetics mechanism was explained by the Korsmeyer-Peppas kinetic model. In order to find out the material toxicity, the biocompatibility assay in a normal cell line of mouse fibroblast (L929) was carried out. At the concentration of 2.5 μg/ml, the cell toxicity was negligible. At the high concentration level of 40.0 μg/ml, the cell viability was not less than 70.0 %. The in vitro cytotoxicity of the drug-loaded composite was studied in Human Colorectal Adenocarcinoma cells and the findings indicated good biocompatibility of the composite. At the concentration of 2.5 μg/ml of the drug-loaded composite (FU-L-APTSB-AL-CSFA): the cell toxicity was found to be less than 50%. And at the high concentration level of 40.0 μg/ml, the cell viability was found to be less than 10%, indicating the targeting action of the loaded composite.