Gelation Technique Research Articles

Characterization, Bioactivity and Application of Chitosan-Based Nanoparticles in a Food Emulsion Model

In this study, chitosan nanoparticles (CNPs) were prepared by the ionic gelation technique with tripolyphosphate (TPP), and the effect of CNP composition and physicochemical characteristics were evaluated. After the synthesis optimization, CNPs were used as carriers for a fish protein hydrolysate (FPH) with bioactive properties (CNPH). The physicochemical characteristics, antioxidant capacity and antimicrobial, antihypertensive and emulsifier properties of unloaded and loaded CNPs in a food system model were studied. CNPH showed a uniform particle distribution, size ~200 nm, high stability (zeta potential around 30 mV), radical scavenging activity and increased antimicrobial activity against Staphylococcus aureus, Shigella sonnei and Aeromonas hydrophila. Additionally, CNPH showed an angiotensin I-converting enzyme (ACE)-inhibitory activity of 63.6% and, when added to a food emulsion model, this system containing CNPs, with or without FHP, exhibited improved food emulsion stability. Thus, CNPs were able to carry the FPH while maintaining their bioactive properties and can be an alternative to the delivery of bioactive peptides with potential as an emulsion stabilizer for food applications.

Investigation on Potential of Chitosan Nanoparticles for Oral Bioavailability Enhancement of Risedronate Sodium.

Risedronate sodium (RS) is used in osteoporosis for bone reabsorption. It is a BCS class III drug having poor oral bioavailability (<0.63%) due to low permeability. In the present study, RS-loaded chitosan nanoparticles were developed to increase oral bioavailability and evaluated for various parameters. The DSC study indicated compatibility of RS with excipients in their physical mixture. The nanoparticles were prepared by ionotropic gelation technique and lyophilized. The optimized batch (RS-CNs) was found to have particles of size 268.7 nm and zeta potential of 24.9 mV. The TEM image of RS-CNs revealed discrete spherical particles. Angle of repose of 27.02 indicates good flow property of nanoparticles. FT-IR spectra of RS-CNs showed characteristic peaks of RS indicating compatibility of RS with the excipients. The mucin binding efficiency of RS-CNs was obtained as 63.42%. The in vitro release study of RS indicated controlled delivery from RS-CNs over 22 h. The release mechanism was found to be diffusion- and erosion-controlled release. Ex vivo study using rat intestine revealed faster permeation of 32.78% in 6 h from RS-CNs compared to plain drug solution. In vivo pharmacokinetic study in rats showed increased Cmax (1.8 fold) from RS-CNs compared to marketed formulation. The relative bioavailability of 193% from RS-CNs indicated significant enhancement in bioavailability upon nanoparticle formulation. The RS-CNs were found to be stable at room and refrigerated conditions. In conclusion, developed RS-loaded chitosan nanoparticles seem to be a promising approach to increase oral bioavailability and can avoid upper GI tract side effects.

Zingiber officinale essential oil-loaded chitosan-tripolyphosphate nanoparticles: Fabrication, characterization and in-vitro antioxidant and antibacterial activities.

Zingiber officinale essential oil (ZEO) was encapsulated in chitosan nanoparticles at different concentrations using the emulsion-ionic gelation technique and its antioxidant and antibacterial effects were investigated. The results indicated that ZEO level had a significant effect on encapsulation efficiency (EE), loading capacity (LC), particle size and zeta potential. The value obtained for EE, LC, mean particle size and zeta potential were 49.11%-68.32%, 21.16%-27.54%, 198.13-318.26 nm and +21.31-43.57 mV, respectively. According to scanning electron micrographs, the nanoparticles had a spherical shape with some invaginations due to the drying process. The presence of essential oil within the chitosan nanoparticles was confirmed by Fourier transform infrared (FTIR) spectroscopy. In vitro release studies in simulated gastrointestinal fluid (SGF) and simulated intestinal fluid (SIF) indicated an initial burst effect followed by slow release with higher release rate in acidic medium of SGF. ZEO-loaded nanoparticles showed DPPH radical scavenging activity of 20%-61% which increased by raising the ZEO level. Moreover, results of antibacterial activity revealed that Staphylococcus aureus (with inhibition zones of 19-35.19 mm2) and Salmonella typhimurium (with inhibition zones of 9.78-17.48 mm2) were the most sensitive and resistant bacteria to ZEO, respectively. Overall, chitosan nanoparticles can be considered as suitable vehicles for ZEO and improve its stability and solubility.

Production of polylactic acid aerogels via phase separation and supercritical CO2 drying: thermodynamic analysis of the gelation and drying process

The application range of aerogels, especially in the life-science sector, can be extended by utilizing biocompatible polymers such as polylactic acid (PLA). However, the low glass transition temperature (Tg) of PLA and the challenging gelation techniques limit the application of supercritical CO2 (scCO2) drying and thus the PLA-aerogel production. The aim of this work is to overcome this challenge and to provide a better understanding of the thermodynamics of the process. Therefore, the gelation of amorphous PLA (PDLLA) and semicrystalline PLA (PLLA) via thermal-induced phase separation (TIPS) was studied. To identify polymer/solvent/antisolvent ratios suitable for gelation, thermodynamic modeling (PC-SAFT) was used to describe the corresponding ternary phase diagrams. scCO2 drying was used to preserve the mesoporous gel structure formed during the gelation. Due to the decrease in the Tg of PLA in the presence of CO2, this could not be applied to all gels. It was found that the critical parameter to enable the scCO2 drying of low Tg polymers is the crystallinity degree (Xc) of the polymer. Based on these results, some guidelines for producing aerogels from polymers with low Tg are formulated.Graphical abstract

Synthesis, characterization, and antimicrobial activities of 3-HPAA-Alg-Chi nanoparticles

Encapsulation of bioactive compounds (e.g., phenolic acids) into nanoparticles is a well-received technique in the searching for new antimicrobial agents against multidrug-resistant pathogens. Encapsulation can be a good technique to maintain the stability of phenolic acids against environmental conditions. In this study, 3-hydroxyphenylacetic acid (3-HPAA) was encapsulated into alginate-chitosan nanoparticles with the ion gelation technique. The characterization of loaded and unloaded nanoparticles was performed via dynamic light scattering, Fourier transform infrared spectroscopy, and scanning electron microscopy. According to the results, 3-HPAA loaded nanoparticles have spherical shapes with a diameter range of 40-80 nm and an average hydrodynamic diameter of 361.0 +_ 69.8 nm. The loading of 3-HPAA was successfully achieved based on the Fourier transform infrared spectra and encapsulation percentage studies. The antimicrobial effect of the nanoparticles in solution forms was tested on P. aeruginosa, S. epidermidis, MRSA, and MSSA. The results demonstrated that the 3-HPAA loaded alginate chitosan nanoparticle solution showed elevated antimicrobial effect due to the pH change by treatment with 1% acetic acid, and it displayed bacteriocidal effects in a strain-specific and dose-dependent manner. Therefore, the 3-HPAA loaded alginate chitosan nanoparticle solution was produced successfully with the bacteriocidal effect against serious pathogenic bacteria.

Effect of Alginate-Microencapsulated Hydrogels on the Survival of Lactobacillus rhamnosus under Simulated Gastrointestinal Conditions.

Thanks to the beneficial properties of probiotic bacteria, there exists an immense demand for their consumption in probiotic foods worldwide. Nevertheless, it is difficult to retain a high number of viable cells in probiotic food products during their storage and gastrointestinal transit. Microencapsulation of probiotic bacteria is an effective way of enhancing probiotic viability by limiting cell exposure to extreme conditions via the gastrointestinal tract before releasing them into the colon. This research aims to develop a new coating material system of microencapsulation to protect probiotic cells from adverse environmental conditions and improve their recovery rates. Hence, Lactobacillus rhamnosus was encapsulated with emulsion/internal gelation techniques in a calcium chloride solution. Alginate–probiotic microbeads were coated with xanthan gum, gum acacia, sodium caseinate, chitosan, starch, and carrageenan to produce various types of microcapsules. The alginate+xanthan microcapsules exhibited the highest encapsulation efficiency (95.13 ± 0.44%); they were simulated in gastric and intestinal juices at pH 3 during 1, 2, and 3 h incubations at 37 °C. The research findings showed a remarkable improvement in the survival rate of microencapsulated probiotics under simulated gastric conditions of up to 83.6 ± 0.89%. The morphology, size, and shape of the microcapsules were analyzed using a scanning electron microscope. For the protection of probiotic bacteria under simulated intestinal conditions; alginate microbeads coated with xanthan gum played an important role, and exhibited a survival rate of 87.3 ± 0.79%, which was around 38% higher than that of the free cells (49.4 ± 06%). Our research findings indicated that alginate+xanthan gum microcapsules have a significant potential to deliver large numbers of probiotic cells to the intestines, where cells can be released and colonized for the consumer’s benefit.

Shape control and stability of multicore millimetre‐sized capsules using a combined monoaxial dispersion electrospraying–ionotropic gelation technique

AbstractMulticore millimetre‐sized fish oil‐loaded alginate capsules were developed using a combined monoaxial dispersion electrospraying–ionotropic gelation technique and their stability was explored. By adjusting the preparation parameters, the capsule shapes could be irregular, spherical with a short‐tail, spherical, fusiform, and fusiform with a long‐tail. The continuous phase of the millimetre‐sized capsules consisted of hydrophilic alginate calcium and water. Moreover, the water content increased from 17% to 69% with increased alginate concentration (2.5–30 mg mL−1). The capsules prepared with alginate concentration of 10 mg mL−1 or 20 mg mL−1 show a similar loading ratio (about 5–8%) of fish oil during storage. Headspace solid‐phase microextraction–gas chromatography mass spectroscopy (HS‐SPME‐GC‐MS) results confirmed the capsules masked the fishy odour of fish oil. Moreover, fish oil slowly migrated from the inside to the outside of the capsules. This work presented a simple method to prepare multicore millimetre‐sized capsules with controlled shapes and a basic understanding of the effect of encapsulation using alginate to mask the fish oil odour.

Development and Characterization of Calcium-Alginate Beads of Apigenin: In Vitro Antitumor, Antibacterial, and Antioxidant Activities

The objective of this work was to develop sustained-release Ca-alginate beads of apigenin using sodium alginate, a natural polysaccharide. Six batches were prepared by applying the ionotropic gelation technique, wherein calcium chloride was used as a crosslinking agent. The beads were evaluated for particle size, drug loading, percentage yield, and in vitro drug release. Particle size was found to decrease, and drug entrapment efficiency was enhanced with an increase in the polymer concentration. The dissolution study showed sustained drug release from the apigenin-loaded alginate beads with an increase in the polymer proportion. Based on the dissolution profiles, BD6 formulation was optimized and characterized for FTIR, DSC, XRD, and SEM, results of which indicated successful development of apigenin-loaded Ca alginate beads. MTT assay demonstrated a potential anticancer effect against the breast cancer MCF-7 cell lines. The antimicrobial activity exhibited effective inhibition in the bacterial and fungal growth rate. The DPPH measurement revealed that the formulation had substantial antioxidant activity, with EC50 value slightly lowered compared to pure apigenin. A stability study demonstrated that the BD6 was stable with similar (f2) drug release profiles in harsh condition. In conclusion, alginate-based beads could be used for sustaining the drug release of poorly water-soluble apigenin while also improving in vitro antitumor, antimicrobial, and antioxidant activity.

Hybrid Hosts Based on Sodium Alginate and Porous Clay Heterostructures for Drug Encapsulation.

In this study, some hybrid materials based on sodium alginate (NaAlg) and porous clay heterostructures (PCHs) were investigated as new hosts for 5-Fluorouracil (5-FU) encapsulation. The hybrid hosts were prepared by ionotropic gelation technique using different concentrations of PCHs (1, 3, and 10 wt%) in order to identify the optimal parameters for encapsulation and drug release. The obtained hybrid materials were characterized using FTIR Spectrometry, thermogravimetric analysis (TGA), scanning electron microscopy (SEM), and UV-Vis spectrometry to investigate the interactions of the raw materials involved in the preparation of hybrid hosts, the influence of PCHs concentrations on drug encapsulation efficiency and drug release profile. All the results show that the synthesized hybrid materials were able to load a high amount of 5-FU, the encapsulation efficiency and the release profile being influenced by the concentrations of PCHs.

Understanding the Effect of Conformational Rigidity on Rheological Behavior and Formation of Polysaccharide-Based Hybrid Hydrogels.

The importance of conformational rigidity on macroscopic rheological properties was revealed using two model polysaccharides, namely, xanthan gum and hyaluronic acid. Xanthan gum has a rigid tertiary conformation due to its ordered double-helical structure, and the interactions between the tertiary structures result in the formation of a network/quaternary structure. In comparison, hyaluronic acid possesses a relatively flexible tertiary conformation due to its secondary random coil structure. Xanthan gum exhibits a much stronger shear thinning and more solidlike behavior compared to hyaluronic acid, owing to its network/quaternary structure. The rigid tertiary structure and the presence of a network/quaternary structure also endow xanthan gum with better resistance against environmental changes (e.g., salt and/or urea addition, temperature change) compared to hyaluronic acid. The network/quaternary structure allows xanthan gum to form gels with chitosan via electrostatic interactions when using the vapor-induced gelation technique, which is not possible for hyaluronic acid due to its flexible tertiary conformation under similar conditions.

Formulation, characterization and in vitro digestion of polysaccharide reinforced Ca-alginate microbeads encapsulating Citrus medica L. phenolics

Using ionotropic gelation technique, Citrus medica L. phenolics was encapsulated in Ca-alginate microbeads to deliver associated health benefits. Microbeads were strengthened by polysaccharide fillers (starch, carrageenan, and pectin) at different concentrations (0.5–4 g/100 mL) for an effective phenolic encapsulation, controlled release, and swelling. All blended solutions were subjected to a similar set of instrumental conditions for controlled extrusion. Whereas, three polymeric combinations (ASE, ACE, and APE) with higher encapsulation efficiencies (EE%) were selected. Furthermore, the impact of polysaccharide fillers on physical properties of Ca-alginate microbeads, such as size, sphericity factor, viscosity, and water activity, was investigated. In contrast to AE, ASE, and ACE microbeads, APE (pectin; 2 g/100 mL) showed highest EE% (90.18) and antioxidant activity with a half maximal effective concentration (EC50) of 108.97 μg/mL. Under in vitro gastrointestinal conditions, APE outperformed in terms of controlled release and swelling. While, UHPLC-DAD-QTOF-IMS also showed the higher amount of hesperidin (264.11 mg/100 g) and polymethoxy-flavones (PMFs) encapsulated in APE microbeads. The chemical interaction was confirmed by FTIR, which showed similar C–H stretching of aromatic components in APE and CMEE. Overall, the study revealed that Ca-alginate microbeads with polysaccharide fillers improved entrapment and controlled delivery of citrus phenolics for therapeutic uses.

Synthesis and Properties of Chitosan Nanoparticles CrossLinked with Tripolyphosphate

Chitosan nanoparticles (ChNPs) have been extensively examined for various biomedical applications due to their advantages include large surface area, biodegradability, and biocompatibility. The purpose of this research was to synthesize ChNPs using a simple ionic gelation technique by the interaction of low molecular weight chitosan (LMWC) and sodium tripolyphosphate (TPP) as a cross-linking agent. ChNPs, TPP, and LMWC were analysed by X-ray diffraction (XRD) and Fourier transforms infrared (FTIR) spectra that indicated the formation of ChNPs, attributing to the rearrangement of the nanoparticles after adding the TPP cross-linker into the LMWC solution. XRD analysis exhibited that ChNPs were amorphous, due to the effect of TPP cross-linker. Dynamic light scattering showed the nano-dimension of ChNPs with a hydrodynamic size of 68.50 nm. Thus, the obtained results indicated that the properties of chitosan were improved through converting it into nanoparticles using TPP initiated ionic gelation procedure.

Flutamide Loaded Polymeric Nanoparticles for prostate Cancer: A Review

Flutamide is a potent nonsteroidal anti androgen used to treat advanced prostate cancer. It blocks the androgen receptors on the cancer cells and inhibits the androgen dependent cell growth. This work was planned to compile the research work available in the scientific publications in the formulation and evaluation of Flutamide loaded polymeric nanoparticles for the treating the prostate cancer including the study of influence of various formulation components such as polymer concentration, organic phase volume, drug content, stabilizer concentrations and the ratio between aqueous to organic phase in the characteristics of nanoparticles. Literature study revealed that, methods like Ionic Gelation Technique, Solvent Evaporation method and Nanoprecipitation have been utilized and polymers like Chitosan, casein, Methacrylic acid, PHEA-IB-p(BMA) graft copolymer, mPEG – PLGA and PVA have been utilized. The drug loaded polymeric nanoparticles were evaluated for their physiocochemical properties along with characterization with FTIR, in vitro release and in vitro and in vivo anticancer potential. From the literature it was understood that, nanoprecipitation method was the most commonly used method in various research perspectives. Based on the findings of the present review, Flutamide loaded polymeric nanoparticles may be used as an treatment adjunctive for prostate cancer.

Formulation and Evaluation of Ranitidine Hydrochloride Loaded Floating Microspheres for the Treatment of Gastric Ulcer

The study was aimed to prepare gastro retentive floating microsphere of Ranitidine Hydrochloride by Ionotropic Gelation technique and solvent evaporation technique by using the different carriers’ ratios (Carbopol 934, Chitosan, and sodium alginate). Both natural and synthetic polymers have been used to prepare floating microspheres and evaluated the relevant parameters. There was no drug and carrier interactions assessed from FTIR. Depending upon the ratio, the percentage yield was found between 58.33% to 90.38%. in all formulations. The surface morphology of microspheres was characterized by SEM and it was discrete, spherical in shape with rough outer surface and showed free flowing properties. The mean particle size of microspheres significantly increases with increasing polymer concentration and the range between 99.92±1.221 to 168.23±1.963 µm. Among all the formulations, RF3 showed high drug entrapment efficiency (87.52%). The percentage in-vitro buoyancy of the floating microspheres was in the range of 66.92% to 81.52%. The in-vitro drug release study revealed that RF3, RF6 and RF9 Formulations having 89.97%,92.91%,93.68% drug released at the end of dissolution studies respectively. It could be concluded that the developed floating microsphere of Ranitidine Hydrochloride can be used for prolonged release in stomach. Therefore improving the bioavailability and patient compliance.

New sustainable chemically modified chitosan derivatives for different applications: Synthesis and characterization

The functionalization of chitosan (CS) by terephthaloyl chloride (TPC), glutaraldehyde (GA), and 4(4-(ethyl carbamoyl) benzoyl chloride) benzene sulfonamide was performed under different reaction conditions to yield the new hydrogels (I, II, III) respectively. However, hydrogel (I-NPs) was prepared from reaction of chitosan with (TPC) via ionic gelation technique using sodium tripolyphosphate (TPP) as a cross-linker. Moreover, hydrogel (I) was loaded (Au, Ag and ZnO) nanoparticles to give the nanoformulations (I-Au NPs, I-Ag NPs and I-ZnO NPs) respectively. Structural and morphological analysis of the new chitosan derivatives hydrogels and NPs formulations were characterized by FTIR, elemental analysis, TGA, DSC, XRD, SEM and TEM. From swelling study, chitosan derivatives hydrogels revealed higher swelling degree compared to (CS) with increasing time, temperature and pH values which reached maximum at pH 7 then decreased at pH 10. In addition, the maximum sorption capacities of Congo Red (CR) in aqueous solution were in the range 81–88%. Moreover, adsorption equilibrium isotherm results displayed favorable Langmuir model than Freundlich model. Furthermore, chitosan derivatives hydrogels showed broad spectrum antimicrobial activities against Gram-negative bacteria, Gram-positive bacteria and fungi with the inhibition zone diameter ranged from 13 to 25 mm compared to (CS) hydrogel which revealed inhibition zone diameter ranged from 11 to 16 mm, especially the nano formulation hydrogel (I-Ag NPs) showed the highest antimicrobial activity. The results were promising suggesting that the new modified chitosan derivatives could be potential for dye removal and as antimicrobial agents.

5-Aminosalicylic Acid Loaded Chitosan-Carrageenan Hydrogel Beads with Potential Application for the Treatment of Inflammatory Bowel Disease.

The aim of our work is to prepare mucoadhesive particles with biopolymers and 5-Aminosalicylic acid (5ASA) using the ionotropic gelation technique to ensure a controlled drug release at the colon level with potential applications in the treatment of intestinal bowel disease (IBD). The preparation of particles through the crosslinking of Chitosan (CS) with sodium tripolyphosphate (TPP) using different mass ratios and the influence of the k-Carrageenan (kCG) layer were studied. UV–VIS spectrometry was employed to assess encapsulation efficiency and drug release profile of 5ASA. The particles were investigated using FT-IR spectrometry for chemical characterization and the DLS results highlighted a monodisperse particle size distribution. The morphology of the polymeric beads was investigated using micro-computer tomography (µCT) and Scanning Electron Microscopy (SEM). Particles based on Chitosan and k-Carrageenan were able to incorporate and preserve 5ASA in an acidic and alkaline medium. The 5ASA loaded polymeric particles obtained after immersion for 1 h in kCG solution exhibited the lowest release rate in pH = 1.2. Biocompatibility studies performed on all of the particles displayed a good viability for the CCD 841 CoN cells and low cytotoxicity. All of the results have shown that these new biomaterials could be a versatile platform of targeted carriers with potential applications in inflammatory bowel disease treatment.

Biomacromolecules of chitosan – Bacopa saponin based LipL32 gene delivery system for leptospirosis therapy

Leptospirosis is a severe bacterial infectious disease caused by the organisms belonging to the genus of Leptospira. The chitosan/Bacopa saponin/tripolyphosphate (CS/BS/TPP) nanoparticles conjugated with recombinant DNA vaccines were designed against Leptospirosis. Chitosan, a polysaccharide is suitable for delivery of drug, and gene due to its bio-compatible and biodegradable properties. Bacopa saponins are used for the induction of the immune response against microbial infections. The recombinant DNA vaccine construct was composed of the leptospiral outer membrane LipL32 gene tagged with EGFP and hGMCSF adjuvant in the pVAX1 mammalian expression vector along with the Cytomegalovirus (CMV) promoter. These recombinant DNA vaccine constructs was termed as pVAX1-EGFP-LipL32 and pVAX1-EGFP-hGMCSF-LipL32, and these constructs were conjugated with CS/BS/TPP nanoparticles by using the ionic gelation technique. Thus, CS/BS/TPP conjugated nanoparticle DNA vaccine was confirmed by functionality (FT-IR), crystalline nature (XRD) and surface charge (Zeta potential). The 90% encapsulation efficiency was observed in the conjugated nanoparticle DNA vaccine. In contrast, cell viability analysis validated that the synthesized DNA conjugated CS/BS/TPP nanoparticles showed low cytotoxicity up to 10 mg/mL. The results showed here are the initial establishment of DNA vaccine conjugated nanoparticles, which can be used as a potential anti-leptospiral vaccine.

Oregano and Thyme Essential Oils Encapsulated in Chitosan Nanoparticles as Effective Antimicrobial Agents against Foodborne Pathogens.

The use of natural compounds with biocidal activity to fight the growth of bacteria responsible for foodborne illness is one of the main research challenges in the food sector. This study reports the preparation and physicochemical characterization of chitosan nanoparticles loaded with Thymus capitatus (Th-CNPs) and Origanum vulgare (Or-CNPs) essential oils. The nanosystems were obtained by ionotropic gelation technique with high encapsulation efficiency (80–83%) and loading capacity (26–27%). Nanoparticles showed a spherical shape, bimodal particle size distribution, and good stability (zeta potential values > 40 mV). The treatment of the nanosuspensions at different temperatures (4 and 40 °C) and storage times (7, 15, 21, and 30 days) did not affect their physicochemical parameters and highlights their reservoir ability for essential oils also under stressful conditions. Both Or-CNPs and Th-CNPs exhibited an enhanced bactericidal activity against foodborne pathogens (S. aureus, E. coli, L. monocytogenes) than pure essential oils. These ecofriendly nanosystems could represent a valid alternative to synthetic preservatives and be of interest for health and food safety.

Encapsulation of 5‐Fluorouracil Treated Reduced Graphene Oxide in Sodium Alginate Matrix for Controlled and pH‐Responsive Drug Delivery

AbstractThe present work encompasses the fabrication of sodium alginate microbeads embedded with 5‐fluorouracil (5‐FU)/reduced graphene oxide (rGO) for pH‐responsive drug delivery. Initially, 5‐FU is treated with rGO and then encapsulated with an alginate matrix by a simple ionotropic gelation technique with different cross‐linking agents for the controlled release of 5‐FU. The resultant beads were characterized by Fourier transform infrared spectroscopy (FTIR), X‐ray diffraction (XRD) analysis, differential scanning calorimetry (DSC), thermogravimetric analysis (TGA) and scanning electron microscopy (SEM). Besides, swelling andin vitrodrug release studies were also carried out at pH 1.2, 5.4, and 6.8 at 37 °C. The presence of rGO in the alginate matrix could greatly enhance the 5‐FU loading and accomplish sustained release of 5‐FU. The presence of Mg2+ions in the alginate matrix could greatly affect the swelling and release rate. The anticancer activity of the alginate beads was assessed using an MTT assay against MCF‐7 cells. The results findings that the developed alginate beads are probably to be effective drug carriers for drug delivery applications.

Optimization and characterization of hepatoprotective andrographolide microspheres in the necrotic rat model

This study aimed to develop controlled release drug delivery of oral andrographolide encapsulated in microspheres, targeted against degenerative hepatic disorder. Ionotropic gelation technique was used to prepare andrographolide loaded Chitosan/Na-Alginate microspheres. The final drug formulation was optimized based on the statistical modeling used in the study. SEM, DSC, and XRD studies revealed a spherical formulation with a smooth surface morphology and increased thermal stability. Mean particle size, drug entrapment efficiency, and cumulative drug release from the optimized formulation were observed to be 37.46 ± 2.3 μm, 88.13 ± 3.6%, and 93.04 ± 5.1%, respectively, and manifesting steady-state release profile up to 12 h with zero-order kinetics and Non-Fickian diffusional release. In-vivo studies show a remarkable effect in elevated liver enzyme levels, and hepatocellular necrosis in CCl4 intoxicated Wistar Rats. Findings from this study suggest that andrographolide microspheres could be a potential delivery system with high oral bioavailability and sustained drug release profile against hepatic necrosis.