Validation of a Novel RP-HPLC Technique for Simultaneous Estimation of Lignocaine Hydrochloride and Tibezonium Iodide: Greenness Estimation Using AGREE Penalties.

Herein, we reported an HPLC method for the simultaneous determination of tibezonium iodide (TBN) and lignocaine hydrochloride (LGN). The method was developed according to the International Conference for Harmonization guidelines (ICH) Q2R1 using Agilent® 1260 with a mobile phase consisting of acetonitrile and phosphate buffer (pH 4.5) in a volumetric ratio of 70:30 and flowing through a C8 Agilent® column at 1 mL/min. The results revealed that TBN and LGN peaks were isolated at 4.20 and 2.33 min, respectively, with a resolution of 2.59. The accuracy of TBN and LGN was calculated to be 100.01 ± 1.72% and 99.05 ± 0.65% at 100% concentration, respectively. Similarly, the respective precision was 100.03 ± 1.61% and 99.05 ± 0.48%. The repeatability for TBN and LGN was found to be 99.05 ± 0.48% and 99.19 ± 1.72%, respectively, indicating that the method was precise. The respective regression co-efficient (r2) for TBN and LGN was found to be 0.9995 and 0.9992. Moreover, the LOD and LOQ values for TBN were 0.012 and 0.037 µg/mL, respectively, while for LGN, they were 0.115 and 0.384 µg/mL, respectively. The calculated greenness of the method for ecological safety was found to be 0.83, depicting a green contour on the AGREE scale. No interfering peaks were found when the analyte was estimated in dosage form and in volunteers' saliva, depicting the specificity of the method. Conclusively, a robust, fast, accurate, precise and specific method was successfully validated to estimate TBN and LGN.

Fast dissolving microneedle patch for pronounced systemic delivery of an antihyperlipidemic drug.

Fast dissolving microneedles (F-dMN) are quite a novel approach delivering specific drug molecules directly into the bloodstream, bypassing the first-pass effect. The present study reported an F-dMN patch to enhance systemic delivery of simvastatin in a patient-friendly manner. The F-dMN patch was developed using polyvinyl pyrrolidone and polyvinyl alcohol and characterized using light microscopy, SEM, XRD, FTIR, mechanical strength, drug content (%), an ex-vivo penetration study, an ex-vivo drug release study, a skin irritation test, and a pharmacokinetics study. The optimized F-dMN patch exhibited excellent elongation of 35.17%, good tensile strength of 9.68 MPa, an appropriate moisture content of 5.65%, and good penetrability up to 560 µm. Moreover, it showed 93.4% of the drug content within the needles and 81.75% in-vitro release. Histopathological findings and a skin irritation study proved that the F-dMN patch was biocompatible and did not cause any sort of irritation on animal skin. Pharmacokinetic parameters of F-dMN patches were improved (Cmax 6.974 µg/ml, tmax 1 hr and AUC 19. 518 µg.h/ml) as compared to tablet Simva 20 mg solution (Cmax 2.485 µg/ml, tmax 1.4 hr and AUC 11.199 µg.h/ml), thus confirming bioavailability enhancement. Moreover, stability studies confirmed the stability of the developed F-dMN patch, as investigated by axial needle fracture force and drug content.

Development and optimization of tibezonium iodide and lignocaine hydrochloride containing novel mucoadhesive buccal tablets: a pharmacokinetic investigation among healthy humans.

OBJECTIVE: It is clinically important to deliver a sustained-release mucoadhesive dosage of local anesthetic and antimicrobial agents for pain control. The current study aimed to develop and evaluate chitosan (CHI) based buccal mucoadhesive delivery for the local release of tibezonium iodide (TBN) and lignocaine hydrochloride (LGN). METHODS: Direct compression technique was employed, aided by other mucoadhesive polymers like hydroxypropylmethylcellulose (HPMC) and sodium alginate (SA) and evaluated for physicochemical and in vivo character. RESULTS: Fourier transform infrared spectral analysis (FTIR), powdered X-ray diffraction (XRPD), and differential scanning calorimetry (DSC) absence of physical interaction between ingredients. The physical parameters complied with USP specifications for all formulations. Optimum swellability (551.9%) was offered from formulation TL15, containing 30% SA. The highest ex vivo mucoadhesive strength (24.79 g) and time (18.39 h) was found with TL8. Formulation TL8 also exhibited maximum in vivo residence time (11.37 h). Almost complete drug release at 6 h was possessed by formulation TL5 (HPMC and CHI, 20% each) for TBN (99.98%) and LGN (99.06%). The optimized formulation TL5 exhibited dosage stability up to 6 months at 75% relative humidity and retained drug contents. TL5 was well tolerated by the volunteers with no inflammation, pain or irritation found. Almost 73% of volunteers reported an increase in salivary secretion. The first-order salivary Cmax of TBN and LGN were found as 16.02 and 7.80 µg/mL within 4 h, respectively. CONCLUSION: Therefore, the sustained release mucoadhesive dosage form of TBN and LGN can be an effective and alternative option to conventional delivery.

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.

Optimization of metronidazole SR buccal tablet for gingivitis using genetic algorithm.

Gingivitis is a condition that needs sustained concentration of antibiotic locally over extended period of time. The current study aimed to formulate and evaluate the sustained and localized release of metronidazole (MTZ) as mucoadhesive buccal tablet containing hydroxypropylmethyl cellulose (HPMC), Carbopol 940® (CP), carboxymethylcellulose (CMC) and ethyl cellulose (EC) as mucoadhesive polymers. Tablets were directly compressed with proportions of polymeric blends (F1-F16). The results indicated that weight variation (249±2.10mg) and friability (0.21%) were within USP compendial limits. Maximum mucoadhesive strength and time were depicted by F1 and F14 which were 28.47g and 12hr respectively. Formulations, except F4, were within physiological pH limit. Maximum swellability index (261.9%) was exhibited by F16, at 8 hr, containing highest concentration of CP, HPMC and additional CMC. For in vitro release, the pre-set 8 hr complete release were shown by formulations, F15 and F16 which were 100% and 97%, respectively. Genetic algorithm was applied on the attributes to optimize polymeric response in accordance with desirability. The software predicted composition (F17) was tested which revealed that physical characteristics were in accordance with the compendial standards. The release kinetics, evaluated through DDsolver⌖, suggested that release of MTZ followed non-Fickian diffusion type in Korsmeyer-Peppas model. Therefore, MTZ, if delivered as mucoadhesive buccal formulation (F17) containing amounts (mg) of CP (16.4), HPMC (78.7), CMC (8.3) and EC (10.5) will simulate satisfactory release i.e. 96% at 8 hr in simulated buccal fluid.

HEMA based pH-sensitive semi IPN microgels for oral delivery; a rationale approach for ketoprofen.

Objectives: The study aimed to develop safe, effective, and targeted drug delivery system for administration of nonsteroidal anti-inflammatory drugs (NSAIDs) in the form of microgels. We developed pH responsive microgels to overcome the mucosal damage caused by traditional immediate release dosage forms. Colon targeting and controlled release formulations have the potential to improve efficacy and reduce undesirable effects associated with NSAIDs.Methods: The pH sensitive oral hydrogel demonstrates the potential to target the colon. Cellulose acetate phthalate (CAP) and hydroxyethyl methacrylate (HEMA) based microgel particles were produced using a free radical polymerization technique using ammonium persulfate (APS) initiator and methylenebisacrylamide (MBA) as the crosslinking agent. Swelling and in-vitro drug release studies were performed at a range of pH conditions. The produced formulations were characterized using Fourier transform infrared spectroscopy, thermogravimetric analysis, differential scanning calorimetry, scanning electron microscopy (SEM), and X-ray diffraction. Biocompatibility of the microgels was analyzed in cytotoxicity studies.Key findings: The swelling and release rate were negligible at pH 1.2, which confirmed the pH-responsiveness of CAP-co-poly(HEMA). The co-polymeric system prevents the release of ketoprofen sodium in the stomach owing to limited swelling at gastric pH, whilst promoting release at the basic pH observed in the colon. SEM images confirmed porous nature of the microgels that facilitate effective drug diffusion through the polymeric matrix. Cytotoxicity studies revealed biocompatibility of hydrogels.Conclusion: These investigations showed that that the controlled drug release and gastro-protective drug delivery of NSAIDS was achieved using CAP-co-poly(HEMA) microgel particles.

Development of thiomer based buccal films for the enhancement of bioavailability: An in-vivo analysis.

Present work was conducted to improve the bioavailability of Tizanidine HCl (TZN) by formulating mucoadhesive buccal films (MBFs) using novel thiolated arabinoxylan (TAX) as film former. MBF's were prepared by solvent casting technique followed by their evaluation for surface morphology and folding endurance. Moreover, pharmacokinetic parameters including Cmax, tmax, t1/2 and AUC were determined after administering standard oral solution (SOS) and MBFs of TZN at a dose of 1mg/kg. Successful thiolation was confirmed by the presence of 4.98 to 7.04 mmol of thiol content per gram of the polymer. Results of in-vivo pharmacokinetics have signified (p=0.0089) the suitability of MBFs as a carrier of drug through buccal route. Results have explored that, t1/2 was increased from 2.51hrs (SOS) to 10 hrs, Cmax from 42.3 ng/ml (SOS) to 105ng/ml and tmax from 2hrs (SOS) to 6h. Conclusively, TAX has exhibited the potential to form MBFs thereby offering sustained release of TZN with improved pharmacokinetic profile.

Development and optimization of flurbiprofen loaded microsponges; an in-vitro evaluation.

Current study was designed with the aim to employ quasi emulsification, and double emulsification techniques for the development of Flurbiprofen (FLB) loaded micro sponges, followed by their physicochemical evaluation. FTIR interpretations exhibited compatibility of ingredients, while crystallographic analysis revealed crystalline nature of pure drug, which was masked upon incorporation into microsponges. Optical microscope and SEM have exposed spherical and spongy surfaces of prepared micro sponges. Micromeritics suggested that the flow properties are excellent and microsponges have remarkable drug entrapment efficiency (98.55±0.08%). In-vitro dissolution studies demonstrated good control over release of FLB until 8th h from the prepared microsponges. However, a difference in cumulated amount of released drug was noticed i.e. EC based formulation has released about 99.3±0.10%, while XG facilitated EC based formulations offered 92.7±2.1% release of the drug. Zeta potential indicated access of negative charge while zeta sizer has described the range of the particle size between 2.6 to 3.5µm. Conclusively the results have advocated the suitability of selected ingredients for incorporation of FLB into microsponges for its sustained delivery.

PLANTAGO OVATA: A COMPREHENSIVE REVIEW ON CULTIVATION, BIOCHEMICAL, PHARMACEUTICAL AND PHARMACOLOGICAL ASPECTS.

The basic aspire of current study was to review different aspects of Plantago ovata together with its cultivation, growth, biochemistry, pharmaceutical and pharmacological attributes. Plantago ovata belongs to family Plantaginaceae. It is an annual herb, indigenous to Mediterranean region especially Southern Europe, North Africa and West Asia. Different electronic databases (Medline, Science Direct, Springer link, Pubmed, Google and Google Scholar) were analyzed for the literature on medicinal properties of Plantago ovata. The literature analysis has revealed that Plantago ovata has been endowed with diverse pharmaceutical and pharmacological activities. It is widely used in numerous medicines owing to its both pharmaceutical properties such as mucilage, superdisintegrant, gelling agent, suspending agent as well as pharmacological actions like anti-diarrheal, anti-constipation, wound healer, hypocholestrolemic and hypoglycemic. Thus, Plantago ovata can be employed in the manufacture of a number of pharmaceutical products as well as a safe and efficacious ethnobotanical remedy in several health problems.

PREPARATION, IN VITRO AND IN VIVO CHARACTERIZATION OF HYDROPHOBIC PATCHES OF A HIGHLY WATER SOLUBLE DRUG FOR PROLONGED PLASMA HALF LIFE: EFFECT OF PERMEATION ENHANCERS.

Aim of present study was to develop metoprolol matrix patches using different enhancers. Combination of two hydrophobic polymers, ethyl cellulose and eudragit RL 100 (8 : 2) were used for preparation of unilaminated matrix patch. 10% w/w of isopropyl myristate (IPM), dimethyl sulfoxide (DMSO), span (20 (S20), Tween 20 (T20) and eucalyptus oil as enhancers and 40% of dibutyl phthalate as plasticizer were used. Prepared patches were evaluated for physical appearance, weight uniformity and thickness. FTIR studies were performed to assess compatibility among ingredients and developed formulation. Dissolution and permeation studies were performed to compare effects of enhancers. Surface morphology after release was examined by scanning electron microscopy. Selected formulation was subjected to in vivo studies by randomized crossover design in rabbits (n = 6) for pharmacokinetic comparison with oral solution administration. Physical evaluation revealed that translucent, flexible, non brittle patches of uniform weight and thickness were prepared. Release from patches followed Higuchi model. Mechanism of release was Fickian. Formulation containing IPM showed that release was by anomalous transport. Highest permeation flux was observed for formulation containing IPM with 2-fold enhancement in permeation. Permeation flux for patches was in order of formulation with no enhancer > IPM > T20 > S20 > DMSO = eucalyptus oil. Plasma concentration from in vivo studies exhibited sustained plasma levels of metoprolol after transdermal patch application in comparison to oral solution administration. Pharmacokinetic analysis of in vivo data elucidated that half life was increased 8 times when compared to oral administration, due to controlled release of drug for longer period of time. These findings suggested that hydrophobic transdermal patches of highly water soluble drug metoprolol were successfully prepared with 10% of IPM for sustained systemic delivery for prolonged half life.

FORMULATION AND IN VITRO EVALUATION OF ACYCLOVIR LOADED POLYMERIC MICROPARTICLES: A SOLUBILITY ENHANCEMENT STUDY.

Objective of present work was to formulate polymeric microparticles of acyclovir using 0-cyclodextrin by solvent evaporation method and kneading technique. Four different ratios were fabricated in each case. Sodium lauryl sulfate (4% was utilized as intestinal permeation enhancer in this study. Prepared microparticles were characterized for micromeritic properties i.e., angle of repose, Hausner's ratio, Carr's index, bulk density and tapped density, entrapment efficiency, zeta size and zeta potential, Fourier transform infrared spectroscopy, differential scanning calorimetry, powder x-ray diffraction, scanning electron microscopy, transmission electron microscopy, optical microscopy and permeability studies across chicken intestine. Kinetic models: zero order, first order, Higuchi and Korsmeyer Peppas were applied on release data. Based upon the results of entrapment efficiency (81.25% and 74.50%), product yield (92.50% and 85.50%), permeability (85.18% and 82.05%), x-ray diffraction (amorphous nature), and solubility etc., (1 : 2) drug-polymer ratio was declared the best. Moreover, solid dispersions (1 : 2) had shown promising results. A new potential approach for solubility, bioavailability and permeability enhancement of acyclovir and other BCS class IV drugs was successfully established.

IN VIVO EVALUATION OF SKIN IRRITATION POTENTIAL, MELASMA AND SEBUM CONTENT FOLLOWING LONG TERM APPLICATION OF SKIN CARE CREAM IN HEALTHY ADULTS, USING NON-INVASIVE BIOMETROLOGICAL TECHNIQUES.

The present investigation was conducted to evaluate non-invasively, various functional skin parameters i.e., irritation potential, melasma and sebum contents following long term application of topical cream (w/o) loaded with 2% methanolic extract of Ananas comosus L. versus placebo control (base) in healthy adults. Healthy human volunteers (n = 11, aged 20-30 years) were recruited for investigation and written informed consent was taken from each volunteer. In this single blinded study every volunteer applied formulation on one side of face and placebo on the other side of face twice daily for a period of 12 weeks (three months). Different skin parameters i.e., skin irritancy, melasma, and sebum contents were measured on both sides of face at baseline and after two weeks interval, using photometric device Mexameter and Sebumeter in a draught free room with modulated conditions of temperature (22-25°C) and humidity (55-60%). It was evident from the results that no primary skin irritancy was observed with patch test. Besides, statistical interpretation indicates that treatment with formulation is superior to placebo because it significantly (p ≤ 0.05) reduced the skin irritancy, melasma and sebum secretions throughout the study and reaching maximum -20.76 ± 0.89, -54.2 ± 0.37 and -40.71 ± 0.75%, respectively, at the end of study period. Antioxidant activity of extract was 92% compared to standard antioxidant. Conclusively, active cream loaded with fruit extract was well tolerated by all the volunteers and suitable to treat contact dermatitis, greasy skin, acne and seborrheic dermatitis and augmenting beauty and attraction by depigmentation of human skin. So, in the future, there is need to clinically evaluate these formulations in patients with compromised skin functions i.e., contact dermatitis, melasma, and acne vulgaris in order to explore the actual potential of this fruit.

PELLETS AND PELLETIZATION: EMERGING TRENDS IN THE PHARMA INDUSTRY.

The present time is considered as an era of advancements in drug delivery systems. Different novel approaches are under investigation that range from uniparticulate to multi particulate system, macro to micro and nano particulate systems. Pelletization is one of the novel drug delivery technique that provides an effective way to deliver the drug in modified pattern. It is advantageous in providing site specific delivery of the drug. Drugs with unpleasant taste, poor bioavailability and short biological half-life can be delivered efficiently through pellets. Their reduced size makes them more valuable as compared to the conventional drug deliv- ery system. Different techniques are used to fabricate the pellets such as extrusion and spheronization, hot melt extrusion, powder layering, suspension or solution layering, freeze pelletization and pelletization by direct compression method. Various natural polymers including xanthan gum, guar gum, tragacanth and gum acacia, semisynthetic polymers like cellulose derivatives, synthetic polymers like derivatives of acrylamides, can be used in pellets formulation. Information provided in this review is collected from various national and intemational research articles, review articles and literature available in the books. The purpose of the current review is to discuss pellets, their characterizations, different techniques of pelletization and the polymers with potential of being suitable for pellets formulation.

Development and characterization of pH-responsive Delonix regia/mucin co-poly (acrylate) hydrogel for controlled drug delivery of metformin HCl.

This study introduces a pH-responsive hydrogel developed from Delonix regia and mucin co-poly(acrylate) through free radical polymerization to enhance controlled drug delivery systems. Characterization using FTIR, DSC, TGA, SEM, PXRD, and EDX spectroscopy detailed the hydrogel's amorphous and crystalline structures, thermal stability, surface characteristics, and elemental composition. Tested at a pH of 7.4-mimicking intestinal conditions-the hydrogel demonstrated significant swelling, indicating its capability for targeted drug release. With Metformin HCl as a model drug, the hydrogel exhibited a promising sustained release profile, underscoring its potential for oral administration. Safety and biocompatibility were assessed through acute oral toxicity studies in albino rabbits, encompassing biochemical, hematological, and histopathological evaluations. X-ray imaging confirmed the hydrogel's navigability through the gastrointestinal tract, affirming its application in drug delivery. By potentially mitigating gastrointestinal side effects, enhancing patient compliance, and improving therapeutic efficacy, this Delonix regia/mucin co-poly(acrylate) hydrogel represents a step in pharmaceutical sciences, exploring innovative materials and methodologies for drug delivery.

Chitosan-based intelligent polymeric networks for site-specific colon medication delivery: A comprehensive study on controlled release of diloxanide furoate and network formation dynamics.

Oral medications are prone to gastric degradation and enzymatic inactivation, diminishing their efficacy. This study investigates a solution by developing intelligent polymeric networks, incorporating chitosan, methacrylic acid, N, N, methylene bisacrylamide, and montmorillonite clay, to enable the controlled release of Diloxanide Furoate (DF), an anti-protozoal drug. Employing a swelling-assisted diffusion technique, drug loading percentages varied from 63.96 % to 76.82 % among different formulations. Increased chitosan and methacrylic acid content enhanced drug loading, while N, N, methylene bisacrylamide and montmorillonite clay demonstrated an inverse relationship affecting diffusion and swelling. Equilibrium swelling studies unveiled formulation-dependent behaviors, with chitosan reducing swelling and methacrylic acid promoting it. Higher N, N, methylene bisacrylamide concentrations decreased swelling, indicating a denser cross-linked structure, while montmorillonite clay reduced hydrophilicity and swelling capacity. Further analyses confirmed successful gel formation, particularly in formulations with higher chitosan, methacrylic acid, and N, N, methylene bisacrylamide content, while montmorillonite clay limited gel fraction due to restricted polymer chain mobility. Techniques such as Fourier transform infrared spectroscopy, Differential scanning calorimetry, and thermal gravimetric analyses supported network development, enhancing thermal stability and cross-linking density. This research underscores the flexibility of polymeric networks for precise drug delivery, offering potential advancements in targeted therapies for various medical conditions.

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.

Sustained release delivery of favipiravir through statistically optimized, chemically cross-linked, pH-sensitive, swellable hydrogel.

In the current work, favipiravir (an antiviral drug) loaded pH-responsive polymeric hydrogels were developed by the free redical polymerization technique. Box-Behnken design method via Design Expert version 11 was employed to furnish the composition of all hydrogel formulations. Here, polyethylene glycol (PEG) has been utilized as a polymer, acrylic acid (AA) as a monomer, and potassium persulfate (KPS) and methylene-bisacrylamide (MBA) as initiator and cross-linker, respectively. All networks were evaluated for in-vitro drug release (%), sol-gel fraction (%), swelling studies (%), porosity (%), percentage entrapment efficiency, and chemical compatibilities. According to findings, the swelling was pH sensitive and was shown to be greatest at a pH of 6.8 (2500%). The optimum gel fraction offered was 97.8%. A sufficient porosity allows the hydrogel to load a substantial amount of favipiravir despite its hydrophobic behavior. Hydrogels exhibited maximum entrapment efficiency of favipiravir upto 98%. The in-vitro release studies of drug-formulated hydrogel revealed that the drug release from hydrogel was between 85 to 110% within 24 h. Drug-release kinetic results showed that the Korsmeyer Peppas model was followed by most of the developed formulations based on the R2 value. In conclusion, the hydrogel-based technology proved to be an excellent option for creating the sustained-release dosage form of the antiviral drug favipiravir.

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.

Correction: Shakir et al. Exorbitant Drug Loading of Metformin and Sitagliptin in Mucoadhesive Buccal Tablet: In Vitro and In Vivo Characterization in Healthy Volunteers. Pharmaceuticals 2022, 15, 686.

In the original publication, a mistake was observed in Figure 5 as published [...].

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.