Novel Natrosol/Pectin-co-poly (acrylate) based pH-responsive polymeric carrier system for controlled delivery of Tapentadol Hydrochloride.

Background & Objectives: This study aimed to create a controlled delivery system for Tapentadol Hydrochloride by developing interpenetrating networks (IPNs) of Natrosol-Pectin copolymerized with Acrylic Acid and Methylene bisacrylamide, and to analyze the effects of various ingredients on the physical and chemical characteristics of the IPNs. Methods: Novel Tapentadol Hydrochloride-loaded Natrosol-Pectin based IPNs were formulated by using the free radical polymerization technique. Co-polymerization of Acrylic Acid (AA) with Natrosol and Pectin was performed by using Methylene bisacrylamide (MBA). Ammonium persulfate (APS) was used as the initiator of crosslinking process. The impact of ingredients i.e. Natrosol, Pectin, MBA, and Acrylic Acid on the gel fraction, porosity, swelling (%), drug loading, and drug release was investigated. FTIR, DSC, TGA, SEM and EDX studies were conducted to confirm the grafting of polymers and to evaluate the thermal stability and surface morphology of the developed IPNs. Results: Swelling studies exhibited an increase in swelling percentage from 84.27 to 91.17% upon increasing polymer (Natrosol and Pectin) contents. An increase in MBA contents resulted in a decrease in swelling from 85 to 67.63%. Moreover, the swelling was also observed to increase with higher AA contents. Significant drug release was noted at higher pH instead of gastric pH value. Oral toxicological studies revealed the nontoxic and biocompatible nature of Natrosol-Pectin IPNs. Interpretation & Conclusion: The developed IPNs were found to be an excellent system for the controlled delivery of Tapentadol Hydrochloride.

Phytochemical analysis and antihyperglycemic activity of Carissa grandiflora leaves extract on streptozotocin-induced diabetic mice.

Diabetes mellitus (DM), a prevalent metabolic condition that impairs glucose metabolism, causes morbidity and hospitalization. Thus, there is need to establish novel therapeutics against DM. The current study examined the phytochemical analysis and antidiabetic effects of Carissa grandiflora leave extracts (CGLE) on streptozotocin (STZ)-induced DM in mice. CGLE (n-hexane, chloroform, ethanol) was extracted and phytochemically examined for primary and secondary metabolites. Fourier transformed infrared spectroscopy (FTIR) detected functional groups, while 2,2-diphenyl-1-picrylhydrazyl (DPPH) test assessed antioxidant capacity. Later, antidiabetic potential of CGLE extract was investigated in vivo in STZ induced diabetic mice. Phytochemical investigation revealed sugars, ketones, alkaloids, triterpenoids, and glycosides. FTIR indicated phenol, aldehyde, ketone, alkene, alkyne, alcohol, benzene ring and amines, while DPPH assay demonstrated antioxidant potential of extract. Oral CGLE treatment significantly improved body weight (P<0.05), polyphagia and polydipsia (P<0.05) and FBG (P<0.001). Moreover, CGLE extract reversed histopathological alterations in the pancreas, liver, and kidney of diabetic mice. These outcomes highlighted that C. grandiflora extract could be effective therapeutic approach against DM.

Formulation, optimization and in vitro evaluation of sustained release oral hydrogels of diacerein to treat arthritis.

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

Gastroprotective effects of Caragana ambigua stocks on ethanol-induced gastric ulcer in rats supported by LC-MS/MS characterization of formononetin and biochanin A.

BACKGROUND: Caragana ambigua has been the part of the dietary routines of the regional people in south-west Pakistan and has traditionally been used for the treatment of diabetes there. There is an increased production of reactive oxygen species in diabetics, leading to gastrointestinal disorders. Natural antioxidants exhibit gastroprotective effects owing to their free-radical scavenging action. C. ambigua possesses appreciable phenolic and flavonoid content; thus, it has the potential to protect against gastrointestinal disorders (e.g. gastric ulcer). RESULTS: This study reports the anti-ulcer potential of C. ambigua. Four different fractions (chloroform, ethyl acetate, butanol, and aqueous) of plant were compared against omeprazole. Ulcer index, ulcer inhibition percentage, gastric pH and volume, total acidity, gastric protein, gastric wall mucus, and histopathology of gastric walls of rats were assessed. All fractions exhibited a reduction in ulcer index and promotion of percentage of ulcer inhibition compared with the ulcer control group. Furthermore, the fractions revealed a significant (P < 0.001) diminution in gastric volume and total acidity with an increase in pH. Among the fractions investigated, the chloroform fraction unveiled the most promising anti-ulcer activity, which is comparable to omeprazole. Liquid chromatography-tandem mass spectrometry screening of fractions revealed the presence of formononetin and biochanin A (isoflavones reported to have anti-ulcer properties) in the chloroform fraction. CONCLUSION: This study establishes that C. ambigua possesses significant potential in reducing gastric ulcer progression. Formononetin and biochanin A are chiefly responsible for the stated bioactivity due to the fact that these compounds were solely present in the chloroform fraction. © 2022 The Authors. Journal of The Science of Food and Agriculture published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.

Impact of various monomers on release of losartan potassium from guar gum based polymeric network.

Present study was carried out to analyze the impact of three different monomers on release of losartan potassium from graft polymeric network prepared through free radical polymerization. N, N-methylene bis acrylamide was used as crosslinker and potassium persulfate as initiator. Losartan potassium as used as model drug because, it has very small plasma half-life and wide range of applications as an effective and efficient ARB (Angiotensin II Receptor Blockers) causing lower incidence of side - effects. Influence of three different monomers on swelling and in vitro drug release of the delivery system was evaluated at pH 1.2 and 7.4. The polymeric networks were characterized by Fourier transform infrared spectroscopy, Thermogravimetric analysis and Scanning electron microscopy. Polymeric network prepared with acrylic acid and methacrylic acid showed pH responsive behavior and while acrylamide based nexus exhibited pH independent style in swelling and drug release. However, among all the formulations, maximum swelling ratio (25.86) and optimal prolonged drug release (82.92%) was observed for GG-co-AA (M2) polymeric network at intestinal pH 7.4. The results indicated that GG-co-AA polymeric network could be an impending pH-sensitive drug delivery system for Losartan potassium. (M2) designated as formulation code with varying acrylic acid contents.

Development and evaluation of Artemisia vulgaris mucilage based polymeric network for controlled drug delivery.

The present study was conducted to fabricate and compare pH-sensitive polymeric networks of Artemisia vulgaris- Methacrylic acid using free radical polymerization conventional method and microwave-assisted method. Potassium persulphate and N' N'- Methylene bisacrylamide were employed as an initiator-crosslinker system. Swelling studies were performed at pH 1.2, 4.5, 6.8 and 7.4. Concentrations of polymer and monomer along with radiation dose were optimized as a function of swelling. Porosity and gel fraction were calculated for all samples. FTIR study confirmed the formation of cross-linked networks. Results of SEM indicated that the microwave irradiated polymeric network had a more porous structure. DSC and XRD study indicated the entrapment of drug inside the polymeric networks in amorphous form. In comparison to the conventional method, the polymeric network prepared by the microwave-assisted method exhibited high swelling ratios, porosity, thermal stability and drug release. These results signify microwave radiations as an effective alternative to the conventional heating method.

Formulation and evaluation of interpenetrating polymeric network for controlled drug delivery.

Novel Cytarabine-loaded agarose and fenugreek-based hydrogel were formulated via the crosslinking process. Graft copolymerization of methacrylic acid (MAA) on agarose and fenugreek was carried out by using methylene bisacrylamide (MBA) as a crosslinker and potassium persulfate as an initiator. The influence of different formulation ingredients (fenugreek, agarose, MBA, MAA) on swelling index, percentage drug release, and percentage gel content were investigated. It was observed that an increase in the concentration of fenugreek and agarose resulted in an increase in the swelling index (72.45-97.17%). However, an increase in the amount of MBA led to a decrease in the swelling index from 74.23% to 57.74%. A similar result tendency was noted in the case of drug release. FTIR was employed to elucidate effective grafting. The thermal behavior of hydrogel was evaluated through TGA and DSC analysis whereas surface morphology was elucidated through SEM. Release studies were performed at both acidic and basic pH, that is, 1.2 and 7.4. Hence, formulated biocompatible hydrogels proved to be a promising system for the controlled delivery of Cytarabine.

GC-MS profiling and in vitro antioxidant, cytotoxic and antimicrobial activities of Trianthema triquetra Rottl. ex Willed.

Trianthema triquetra Rottl. ex Willed is being used as a herbal remedy for various diseases in India and Pakistan. Still, no scientific data is available about therapeutic potential and phytochemistry of the plant. The aim of the current investigation is to perform GC-MS analysis, antioxidant (total phenolic and flavonoid content, DPPH assay), antimicrobial (disc diffusion assay) and cytotoxic (XTT and RBC's cellular membrane protection assay) studies. Methanolic extract and its fractions (n-hexane, ethyl-acetate, chloroform, n-butanol and water) were investigated for in vitro studies. Results showed that n-butanol fraction exhibited a significant (p<0.05) antioxidant potential (IC50=63.35±0.13 µg/mL) and also possess highest phenolic content (177±4.36 mg/g GAE). Whereas, n-hexane fraction showed highest flavonoid content (14.67±1.53 mg/g QE). 2, 4-Ditert-butyl-6-nitrophenol (26.79%) and Squalene (25.64%) were detected as major components through GC-MS analysis of chloroform fraction, eluted from column chromatography. Moreover, chloroform fraction also exhibited antimicrobial potential. Significant (p<0.05) dose dependent inhibition response on cell growth against CCRF-CEM cell lines was exhibited by methanolic extract. Furthermore, hemolytic potential of methanolic extract was found to be in safe range (2.23%-6.37%). So, it can be inferred that Trianthema triquetra can be exploited as an alternative remedy for cancer, oxidative stress related disorders and various skin diseases.

GC-MS profiling and in vitro antioxidant, cytotoxic and antimicrobial activities of Trianthema triquetra Rottl. ex Willed.

Trianthema triquetra Rottl. ex Willed is being used as herbal remedy for chronic ulcer, wound healing, diabetes, skin and inflammatory diseases in India and Pakistan. Still, no scientific data is available about the therapeutic potential and phytochemistry of the plant. The aim of the current investigation is to perform GC-MS analysis, antioxidant (total phenolic and flavonoid content, DPPH assay), antimicrobial (disc diffusion assay) and cytotoxic (XTT and RBC's cellular membrane protection assay) studies. Whole plant material was dried and extracted with methanol to get crude methanolic extract and then it was fractionated with n-hexane, ethyl-acetate, chloroform, n-butanol and water. Results showed that n-butanol fraction exhibited a significant (p<0.05) antioxidant potential measured by DPPH assay (IC50=63.35±0.13µg/mL) and also possess highest phenolic content (177±4.36mg/g GAE). Whereas, n-hexane fraction showed highest flavonoid content (14.67±1.53mg/g QE). Two major components (2, 4-Ditert-butyl-6-nitrophenol (26.79%) and Squalene (25.64%) were detected in GC-MS analysis of chloroform fraction, eluted from column chromatography. Moreover, chloroform fraction also exhibited antibacterial activity towards all the tested strains of bacteria and fungi. Significant (p<0.05) dose dependent inhibition response on cell growth against CCRF-CEM cell lines was exhibited by methanolic extract. Furthermore, hemolytic potential of methanolic extract was found to be in safe range (2.23%-6.37%). So, it can be inferred that Trianthema triquetra can be exploited as an alternative remedy for cancer, oxidative stress related disorders and in various skin diseases.

Thiolation of arabinoxylan and its application in the fabrication of pH-sensitive thiolated arabinoxylan grafted acrylic acid copolymer.

Current research work was conducted to synthesize Thiol modified arabinoxylan and its application in fabrication of hydrogel. Thioglycolic acid was esterified with arabinoxylan to prepare Thiolatedarabinoxylan. Appearance of peak at 2533.34 cm-1 in FTIR and thiol content showed successful thiolation. The pH-dependent Thiolatedarabinoxylan/acrylic acid (TAX/AA) hydrogels of perindopril erbumine were prepared via free-radical co-polymerization. Perindopril erbumine (PE) was employed as model drug. Different batches with different feed ratio of TAX, AA, and MBA were prepared and their influence on swelling, solvent penetration, and consequent drug release was investigated. Swelling coefficients increased with increase in pH. TAX/AA hydrogels were characterized by Fourier-transform infrared spectroscopy (FT-IR), Thermal Analysis (TA), X-Ray diffraction (XRD), and scanning electron microscope (SEM). Dissolution studies were performed at pH 1.2 and 7.4 in which drug release showed direct correlation with TAX and AA ratio. In vivo studies showed that Cmax of TAX-co-AA based hydrogel was 81.57 ± 0.35 ng/ml which was maintained for a longer time after its administration. All the results of in vivo studies were significant and TAX-co-AA based hydrogel enhances the bioavailability of perindopril erbumine.

Mini Review: Chronic obstructive pulmonary disease, its new drug treatments and strategies: A review.

COPD is a complicated disease. Current available treatments are just for symptomatic relief and they cannot reverse the damages to lungs tissues due to alveolar destruction in COPD. Research is being conducted to evaluate new treatments and strategies to find specific treatments to minimize the symptoms of COPD. A new mixture of herbal medicine i.e AKL1 has emerged and thought to cure COPD symptoms especially cough related quality of life of COPD patients. Although, the results have showed no significant difference as compared to placebo but researchers recommend further evaluation in a large population (COPD Patients) group. Another medicine Roflumilast, a phosphodiesterase 4 inhibitor, was also found to be effective to treat COPD under specific recommendations with further research needed. Finally another medicine Indacaterol, a novel, once-daily (o.d) inhaled long-acting ß2-agonist proved to be effective clinically to treat COPD related broncho-constriction and also increasing the COPD patient's compliance by reducing the number of doses as compared to other conventional inhaled bronchodilators such as Albuterol.

Review - Lactic acid bacteria in traditional fermented Asian foods.

Lactic acid bacteria play vital roles in various fermented foods in Asia. This paper reviews many types of the world's lactic acid fermented foods and discusses the beneficial effects of lactic acid fermentation of food. The lactic acid bacteria associated with foods now include species of the genera Carnobacterium, Enterococcus, Lactobacillus, Lactococcus, Leuconostoc, Oenococcus, Pediococcus, Streptococcus, Tetragenococcus, Vagococcus and Weissella. Lactic acid bacteria (LAB) are involved in many fermentation processes of Asian traditional foods, demonstrating their profound effects on improving food quality and food safety. During the past few decades' interest has arisen in the use of the varied antagonistic activities of LAB to extent the shelf-life of protein-rich products such as meats and fish. This review article outlines the main types of LAB fermentation as well as their typical fermented foods such as idli, kishk, sauerkraut, koumiss, Suan-tsai, stinky tofu, Chinese sausage and kefir. The roles of LAB and the reasons for their common presence are also discussed.

Review: Nigella sativa (Prophetic Medicine): A Review.

The present report is a significant effort to explore detail description of N. Sativa, its pharmacognostic characteristics, morphological characteristics, and mechanism of actions, doses and medicinal uses. Nigella sativa (N. Sativa) is greatest form of healing medicine. It is also known as Prophetic Medicine as its use has been mentioned in Prophetic Hadit, as natural remedy for all the diseases except death. It is recommended on daily basis in Tibb-e-Nabwi (Prophetic Medicine). Hazrat Abu Hurairah States ''I have heard from Rasool Allah (PBUH) that there is cure for every disease in black seeds except death and black seeds are shooneeze''. Salim Bin Abdullah narrates with reference to his father Hazrat Abdullah Bin Omar that Rasool Allah (PBUH) said, 'Let all the black seed upon you, these contain cure of all diseases except death'. N. sativa claimed to have anti-inflammatory, analgesic, hepato-protective, neuro-protective, gastro-protective and other useful properties. Biological and pharmacological effects are attributed to its two important constituents Thymoquinone (TQ) and Nigella sativa oil (NSO). TQ has interaction with human serum albumin. Seeds containing volatile oils mainly Melanthin showed toxicity at larger doses. This report is a reference for all pharmaceutical researchers, physicians and biologists researching on N. sativa and will open a door towards novel agent.

Report: Antimicrobial activity of Kalanchoe laciniata.

This study was conducted to identify antimicrobial potential of Kalanchoe laciniata. The plants were extracted with 30-70% aqueous-methanol and n-hexane. The antimicrobial activities were examined using agar well diffusion method against bacteria (Staphylococcus aureus, Escherichia coli) and fungi (Candidaalbicans). Results showed that E. coli were more sensitive than Staphylococcus aureus and Candida albicans. The largest zone of inhibition (52 mm) was recorded against E. coli with the n-hexane extract of Kalanchoe laciniata.

Formulation and in-vitro evaluation of floating bilayer tablet of lisinopril maleate and metoprolol tartrate.

The purpose of this study was to introduce the technology for the development of rate-controlled oral drug delivery system to overcome various physiological problems. Several approaches are being used for the purpose of increasing the gastric retentive time, including floating drug delivery system. Gastric floating lisinopril maleate and metoprolol tartrate bilayer tablets were formulated by direct compression method using the sodium starch glycolate, crosscarmellose sodium for IR layer. Eudragit L100, pectin, acacia as sustained release polymers in different ratios for SR metoprolol tartrate layer and sodium bicarbonate, citric acid as gas generating agents for the floating extended release layer. The floating bilayer tablets of lisinopril maleate and metoprolol tartrate were designed to overcome the various problems associated with conventional oral dosage form. Floating tablets were evaluated for floating lag time, drug contents and in-vitro dissolution profile and different kinetic release models were applied. It was clear that the different ratios of polymers affected the drug release and floating time. L2 and M4 showed good drug release profile and floating behavior. The linear regression and model fitting showed that all formulation followed Higuchi model of drug release model except M4 that followed zero order kinetic. From the study it is evident that a promising controlled release by floating bilyer tablets of lisinopril maleate and metoprolol tartrate can be developed successfully.

Review-Epigenetic therapy for cancer.

Epigenetics means the study of alterations in the genetic material that affect the phenotype but does not affect the genotype. Epigenetics cause alterations in cell properties, which are inherited; but it does not cause alterations in DNA sequence. Epigenetic mediated silencing of gene is of four types, which are DNA methylation, histone deacetylation, RNA associated silencing and Genomic imprinting. Other factors (environmental and xenobiotics) can also cause gene silencing but DNA methytlation and changes in histones of chromatin are two important changes, which are responsible for malignant diseases. Two groups of drugs are under development, which corrects the epigenetic alterations. These are histone deacetylation (HDAC) inhibitors and DNA methytransferase (DNMT) inhibitors. These drugs may be used in cancer because in cancer, hypermethylation of cancer suppressor gene causes gene silencing. Epigenetic therapy scope is likely to increase in future.

Preparation, In Vitro Characterization, and Evaluation of Polymeric pH-Responsive Hydrogels for Controlled Drug Release.

The purpose of the current research is to formulate a smart drug delivery system for solubility enhancement and sustained release of hydrophobic drugs. Drug solubility-related challenges constitute a significant concern for formulation scientists. To address this issue, a recent study focused on developing PEG-g-poly(MAA) copolymeric nanogels to enhance the solubility of olmesartan, a poorly soluble drug. The researchers employed a free radical polymerization technique to formulate these nanogels. Nine formulations were formulated. The newly formulated nanogels underwent comprehensive tests, including physicochemical assessments, dissolution studies, solubility evaluations, toxicity investigations, and stability examinations. Fourier transform infrared (FTIR) investigations confirmed the successful encapsulation of olmesartan within the nanogels, while thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC) studies verified their thermal stability. Scanning electron microscopy (SEM) images revealed the presence of pores on the surface of the nanogels, facilitating water penetration and promoting rapid drug release. Moreover, powder X-ray diffraction (PXRD) studies indicated that the prepared nanogels exhibited an amorphous structure. The nanogel carrier system led to a significant enhancement in olmesartan's solubility, achieving a remarkable 12.3-fold increase at pH 1.2 and 13.29-fold rise in phosphate buffer of pH 6.8 (NGP3). Significant swelling was observed at pH 6.8 compared to pH 1.2. Moreover, the formulated nexus is nontoxic and biocompatible and depicts considerable potential for delivery of drugs and protein as well as heat-sensitive active moieties.

Mimosa/quince seed mucilage-co-poly (methacrylate) hydrogels for controlled delivery of capecitabine: Simulation studies, characterization and toxicological evaluation.

This research focused on developing pH-regulated intelligent networks using quince and mimosa seed mucilage through aqueous polymerization to sustain Capecitabine release while overcoming issues like short half-life, high dosing frequency, and low bioavailability. The resulting MSM/QSM-co-poly(MAA) hydrogel was evaluated for several parameters, including complex structure formation, stability, pH sensitivity, morphology, and elemental composition. FTIR, DSC, and TGA analyses confirmed the formation of a stable, complex cross-linked network, demonstrating excellent stability at elevated temperatures. SEM analysis revealed the hydrogels' smooth, fine texture with porous surfaces. PXRD and EDX results indicated the amorphous dispersion of Capecitabine within the network. The QMM9 formulation achieved an optimal Capecitabine loading of 87.17 %. The gel content of the developed formulations ranged from 65.21 % to 90.23 %. All formulations exhibited excellent swelling behavior, with ratios between 65.91 % and 91.93 % at alkaline pH. In vitro dissolution studies indicated that up to 98 % of Capecitabine was released after 24 h at pH 7.4, demonstrating the potential for sustained release. Furthermore, toxicological evaluation in healthy rabbits confirmed the system's safety, non-toxicity, and biocompatibility.

Development and evaluation of a pH-responsive Mimosa pudica seed mucilage/ß- cyclodextrin-co-poly(methacrylate) hydrogel for controlled drug delivery: In vitro and in vivo assessment.

In this comprehensive investigation, a novel pH-responsive hydrogel system comprising mimosa seed mucilage (MSM), ß-cyclodextrin (ß-CD), and methacrylic acid (MAA) was developed via free radical polymerization technique to promote controlled drug delivery. The hydrogel synthesis involved strategic variations in polymer, monomer, and crosslinker content in fine-tuning its drug-release properties. The resultant hydrogel exhibited remarkable pH sensitivity, selectively liberating the model drug (Capecitabine = CAP) under basic conditions while significantly reducing release in an acidic environment. Morphological, thermal, and structural analyses proved that CAP has a porous texture, high stability, and an amorphous nature. In vitro drug release experiments showcased a sustained and controlled release profile. Optimum release (85.33 %) results were recorded over 24 h at pH 7.4 in the case of MMB9. Pharmacokinetic evaluation in healthy male rabbits confirmed bioavailability enhancement and sustained release capabilities. Furthermore, rigorous toxicity evaluations and histopathological analyses ensured the safety and biocompatibility of the hydrogel. This pH-triggered drug delivery system can be a promising carrier system for drugs involving frequent administrations.

Development of Tofacitinib Loaded pH-Responsive Chitosan/Mucin Based Hydrogel Microparticles: In-Vitro Characterization and Toxicological Screening.

Tofacitinib is an antirheumatic drug characterized by a short half-life and poor permeability, which necessitates the development of sustained release formulation with enhanced permeability potential. To achieve this goal, the free radical polymerization technique was employed to develop mucin/chitosan copolymer methacrylic acid (MU-CHI-Co-Poly (MAA))-based hydrogel microparticles. The developed hydrogel microparticles were characterized for EDX, FTIR, DSC, TGA, X-ray diffraction, SEM, drug loading; equilibrium swelling (%), in vitro drug release, sol-gel (%) studies, size and zeta potential, permeation, anti-arthritic activities, and acute oral toxicity studies. FTIR studies revealed the incorporation of the ingredients into the polymeric network, while EDX studies depicted the successful loading of tofacitinib into the network. The thermal analysis confirmed the heat stability of the system. SEM analysis displayed the porous structure of the hydrogels. Gel fraction showed an increasing tendency (74-98%) upon increasing the concentrations of the formulation ingredients. Formulations coated with Eudragit (2% w/w) and sodium lauryl sulfate (1% w/v) showed increased permeability. The formulations equilibrium swelling (%) increased (78-93%) at pH 7.4. Maximum drug loading and release (%) of (55.62-80.52%) and (78.02-90.56%), respectively, were noticed at pH 7.4, where the developed microparticles followed zero-order kinetics with case II transport. Anti-inflammatory studies revealed a significant dose-dependent decrease in paw edema in the rats. Oral toxicity studies confirmed the biocompatibility and non-toxicity of the formulated network. Thus, the developed pH-responsive hydrogel microparticles seem to have the potential to enhance permeability and control the delivery of tofacitinib for the management of rheumatoid arthritis.