Cumulative Percentage Drug Release Research Articles

Modified Release Interpenetrating Polymeric Network Hydrogel Beads of Montelukast Sodium Via Box Behnken Design

Background: Interpenetrating Polymeric Networks (IPN) are cross-linked polymeric alloys developed when two or more cross-linked polymers inter-penetratingly entangle. Interpenetrating polymeric networks possess several benefits including stability, biocompatibility, biodegradability, high swelling ability, and modified release efficiency. Aim: The aim of this study is to design stable, control-released montelukast sodium-loaded IPN hydrogel beads as a promising approach toward drug delivery. Objective: The goal of the present work was to develop Chitosan (swellable polymer) and glutaraldehyde (cross-linker) based modified (controlled) released montelukast sodium IPN hydrogel beads. Methods: The montelukast sodium IPN hydrogel beads were prepared via the precipitation method, and the final batch of IPN hydrogel beads was based on particle size, percent entrapment efficiency, area of swelling, and cumulative percent drug release using an overlay plot in Box-Behnken design. Compatibility studies (DSC, FT-IR) and microscopical observation (SEM) confirmed the compatibility and sphericity of the formulations. Results: The optimized (comprising 2.01% chitosan and 0.48% glutaraldehyde) IPN hydrogel beads having satisfactory particle size (817.76±54.49 μm), good entrapment efficiency (71.36±3.04%), and area of swelling (27.00±1.68 mm2) showed swelling and pH-dependent controlled montelukast release (92.96±1.05%) after 12 h with longer duration of action. Conclusion: The prepared montelukast sodium IPN hydrogel beads could be a potent control-released drug delivery vehicle.

Development and In vivo Evaluation of Nanogel Drug Delivery System for Promoting Wound Healing in Diabetic Induced Rats

Recently, researchers have looked at the use of nanotechnology as a drug-delivery system for topical and transdermal applications. The transport of medications and active ingredients to the skin via formulations, including nanoparticles, is a subject of substantial contemporary interest. The present work is proposed to prepare the atorvastatin nanogels to promote wound healing in a diabetic animalmodel.Atorvastatin nanogels were prepared by precipitation polymerization technique using hydroxy propyl methacrylate as polymer. The drug and polymer were selected in ratios of 1:1, 1:2, 1:3, 1:4, 1:5, 1:6, 1:7 and 1:8. Additionally, the produced nanogel was evaluated in vivo and examined for its particle size, trapping effectiveness, and drug release in vitro. The particle size of the prepared various formulations (F1-F8) showed a size range of 68 to 80nm, and entrapment efficiency was seen to be in the range of 58.36-86.75%. The cumulative percentage of drug release was reported to be 61.96 to 73.76 percent over a period of 12hours during the in vitro drug release investigation, which was conducted using phosphate buffer at pH 7.4.The drug release followeda non-fiction mechanism of release kinetics. On the other hand, in vivo comparative study showed a complete wound healing effect for nanogels on the 11th day, whereas for conventional gel on the 15th day.This study indicates that nanogels formulation heals the diabetic wound completely at a faster rate, and also the drug atorvastatin also can be used for diabetic wound healing.

Formulation and Characterization of Isoconazole Loaded Invasomal Gel for Effective Antifungal Activity

The characterization of isoconazole invasomal gel formulations (IG1–IG5) aimed to evaluate their physical attributes, drug content, and drug release kinetics for topical application. All formulations exhibited transparency and smooth texture, indicating uniform drug dispersion. While IG1 had an easily pourable consistency, IG4 displayed very good consistency, suggesting viscosity differences. Despite these variations, all formulations showed good homogeneity and high drug content, with IG4 leading in drug content percentage. Spreadability and viscosity varied among formulations, influencing ease of application and adherence to the skin. Cumulative drug release profiles revealed sustained release over 12 hours, with notable differences in release rates and extents among formulations. IG4 exhibited the most sustained release, aligning with pharmacokinetic requirements for antifungal therapy. Its release profile followed a diffusion-controlled mechanism, with a high cumulative drug release percentage of 98.95 ± 0.32% over 12 hours. Antifungal activity against Candida albicans was comparable to Isoconazole, suggesting IG4’s effectiveness in treating fungal infections. Stability studies confirmed the formulation’s stability under tested conditions, supporting its potential for further development and clinical use.

A Silver Nanoparticle‐Embedded Tamarind Kernel Gum/Poly (Sodium Acrylate) Nanocomposite for Sustainable Release of Doxycycline

AbstractThe current work describes an eco‐friendly novel synthesis of silver (Ag) nanoparticles (NPs)/Tamarind kernel gum (TKG)/Poly (sodium acrylate) (PSA) nanocomposite without the use of any toxic materials. It is a one‐step route synthesis of silver nanocomposite hydrogel in which TKG and PSA are cross‐linked using methylene bisacrylamide (MBA) cross‐linker. The developed hydrogels were characterized using XRD, FTIR, UV‐visible, FE‐SEM, and TEM techniques. Doxycycline (dox) was chosen as a model drug for release studies using TKG/PSA and Ag/TKG/PSA nanocomposite. The observation is that Ag NP/TKG/PSA nanocomposite showed a pH‐dependent swelling which is higher at pH 7.4 than at pH 1.2. Similarly, the cumulative drug release percentage (CDR %) using silver nanocomposite is higher at pH 7.4 than at pH 1.2. Also, the presence of Ag NPs decreased the swelling ratio (SR) of TKG/PSA hydrogel, which controls the rate of release of the dox drug. In addition, the dox release kinetics were studied using the Korsmeyer‐Peppas and Higuchi model. It has been found that drug release data was fitted in the Korsmeyer‐Peppas model with a higher value of regression coefficient (R2). Thus, Ag/TKG/PSA nanocomposite showed satisfactory results for sustainable release of doxycycline drug.

Mucoadhesive Buccal Tablet Formulation of Azithromycin dihydrate for treatment of Upper Respiratory Tract Infection

The buccal drug delivery system is a versatile delivery system which can be designed for local or systemic effect. The objective of the study was to developed patient complacent tablet which can give sustain release of antibacterial agent for relief of upper respiratory tract infection. Azithromycin dihydrate is a semi-synthetic macrolide antibiotic widely used to prevent bacterial infections in the upper respiratory tract. The mucoadhesive buccal tablets of azithromycin dihydrate were formulated by varying concentrations of polymers (natural and synthetic), glidant and other excipients. The drug-excipient compatibility studies were carried out through DSC and FTIR studies. The selected excipients were found to be compatible. Further the dry blend of drug-excipients was evaluated for pre-compression properties. The prepared tablets were evaluated as per the general monograph for tablets of IP. The studies were also carried out to evaluate sustained release of the drug and mucoadhesivity of the tablets. A 23 level (2 level and 3 factors) factorial design was navigated to study the effect of natural, synthetic polymers and the glidant on mucoadhesive strength and percentage cumulative drug release at 8 hours. The responsive variables were analysed using ANOVA by Design-Expert version 12.0. It was concluded that these excipients significantly affected the response variables. The optimized tablet formulation was found to have an adequate mucoadhesion and a cumulative percentage release. The final product was performed for accelerated stability studies, optimized formulation was found to be stable at room temperature and accelerated temperature for three months.

Study on the fabrication and performance of hierarchical porous 3D printed PCL-based artificial bone scaffold with anti-bacterial effect

Nonunion and large bone defects caused by trauma, tumor resection, and other bone diseases pose great challenges for clinical treatment. In this work, we fabricated a hierarchical porous scaffold mimicking the natural bone in structure and component. The inner MC/PCL/VCM (MCP-V) scaffold with pore sizes of 10–30 μm was prepared by vacuum freeze-drying, which has drug loading and mimics the bone component and structure. Then outer PT scaffold with pore sizes of 400–500 μm was prepared and a hole reserved for embedding the prepared MCP-V scaffold by 3D printing. The results showed that the compressive strength increased from 1.6 ± 0.01 MPa to 11.0 ± 0.38 MPa, and the compressive modulus increased from 1.1 ± 0.40 MPa to 12.4 ± 0.42 MPa, separately. As the variation of porosity for scaffolds, the cumulative drug release percentage decreased from (55.3 ± 1.43) % to (44.3 ± 2.47) % at 6 days. Furthermore, CCK-8 and the Live/Dead assay were utilized to assess the viability of MC3T3-E1 cells on scaffolds, which revealed no significant cytotoxicity. The hierarchical scaffold meets the mechanical requirement of cancellous bone, with slow drug release properties and excellent cytocompatibility, providing an effective repair strategy for clinical bone defects.

SYNERGISTIC DRUG COMPATIBILITY OF SUMATRIPTAN SUCCINATE AND METOCLOPRAMIDE HYDROCHLORIDE (IN SITU GEL FORMULATIONS) FOR NASAL DRUG RELEASE OPTIMIZATION

Objective: Migraine is a prevalent neurological condition that causes lifelong tenacious headaches and significantly impacts the daily lives of individuals. Despite being frequently underestimated or neglected, it affects the individual’s routine activities, performance, self-confidence, and identity. Treatment often involves the administration of painkillers, which can lead to various complications. This study aimed to develop and characterize an in situ nasal formulation of sumatriptan succinate and metoclopramide hydrochloride to enhance drug residence time in the nasal cavity and improve drug bioavailability. Methods: Eight formulations of intranasal in situ gels were prepared using the “Cold Method” and evaluated for various parameters, including appearance, texture, viscosity, pH, gel strength, gelation temperature, drug content, and in vitro/ex vivo drug diffusion. FT-IR studies confirmed no interactions between sumatriptan succinate, metoclopramide hydrochloride, and the excipients. Simultaneous estimation method was used to evaluate drug content, in vitro and ex vivo drug diffusion. Results: Among the formulations, “Sumatriptan Succinate Metoclopramide Hydrochloride Polymer (SMP8)” exhibited the most favorable characteristics. The percent cumulative drug release was determined to be 96.803±0.0015 for sumatriptan succinate and 92.569±0.0028 for metoclopramide hydrochloride, aligning with the Higuchi model kinetics. In vitro and ex vivo diffusion studies demonstrated that SMP8 provided sustained drug release for up to 9 h, making it the optimal dosage formulation for nasal drug delivery in the treatment of migraine. Conclusion: This study’s findings suggest that the developed intranasal in situ gel formulation, SMP8, effectively releases sumatriptan succinate and metoclopramide hydrochloride over an extended period. By improving drug residence time and bioavailability, this formulation has the potential to enhance the therapeutic efficacy and patient compliance in the management of migraine.

Fabrication and Evaluation of Luliconazole contains Cationic Guar Gum intended to use for Topical application

The novel imidazole topical drug luliconazole (LCZ) has potent antifungal efficacy against a wide variety of fungi. When applied to the skin, LCZ has tremendous promise as an antifungal agent, however, constrained by its poor skin permeability and limited solubility, requiring protracted therapy and repeated dosage to achieve full recovery. The current work explains the formulation and characterization of a cationic gel prepared by using Guar Gum (GG) and pH was adjusted by using NaOH solution. The created formulation was white in color. The FTIR spectroscopy analysis shows that the medication and polymer did not react with one another. The cumulative percentage drug release suggested that LCZ was released from the formulations. All the release kinetics show that drug release from the formulation was in Fickian transport nature. The correlation value was found to be more than 0.90 in all the fitted release models. The pH of each formulation fell within the predetermined range.The prepared LCZ gel shows a viscosity between 13000 to 28000 cps, which is a very good topical application.

Chemometrics Assisted Formulation of Glimepiride Nanosuspension for Solubility Enhancement in Diabetic Therapy—A Systematic Approach

AbstractGlimepiride (GLM), a third‐generation sulfonylurea oral hypoglycemic medication, is used to treat type II diabetes. Admittedly, it has a low bioavailability, a relatively short half‐life (t1/2), and high toxicity. To address the issue, a nanosuspension of poorly soluble GLM is designed using a Quality‐by‐Design (QbD) method, to enhance its solubility. Prospective risk factors are identified and assessed using Critical Material Attribute (CMAs) and Critical Processing Parameter (CPPs) to evaluate the targets by Taguchi orthogonal array (OA) design and to study the effects of formulation and process variables on dependent variables. The amount of Polyvinylpyrrolidone (PVP) (X2), agitation time (X5), and concentration of Poloxamer (X7) are found as significant parameters (p < 0.05), and are further optimized using the Box Behnken Design as response surface methodology model. The optimized GLM nanosuspension 1) has mean particle size (PS), zeta potential, viscosity (VS), and percentage cumulative drug release (CDR%) of 258.17 nm, −25.2 mV, 1.087cPs, and 98.52%, respectively. The pattern of drug release is fitted to Non‐Fickian kinetics. The study results in an economic and efficient nano formulation with enhanced solubility.

Formulation and Evaluation of Teneligliptin Nanosuspension

In this present study, the drug Teneligliptin is selected for the management of Type-2 Diabetes mellitus. The drug-excipient compatibility study results showed that there is no chemical change occur between the drug and the excipients and there was no functional group change observed. Teneligliptin is poorly water-soluble drug and it was fabricated as nanosuspension of Nine formulations by using nano precipitation technique. In this method, nano size particle size of Teneligliptin was obtained by using different type of various proportions of stabilizers along with other ingredient at different stirring speed. For the prepared formulation (F1-F9) the particle size, polydispersibility index and zeta potential were done. Among nine formulations, formulation 8(F8) results revealed that the values are desirable and stable. The total drug content of all the formulation ranges from 81% to 99%, The average particle size of F1 to F9 batches was found to be in the range of 0.211 nm to 0.486 nm The scanning electron microspore study stated that the nano size particles were spherical in shape. Among all the formulations (F8) was optimized which showed maximum highest percentage of drug release at 24 hours. The cumulative percentage of drug release of formulation 8 (F8) increase with the optimum concentration of stabilizers and tween 80. The release rate of optimized formulation 8(F8) was fitted with various release kinetic studies and the selected formulation followed zero order kinetics. The results of stability study was confirmed that the prepared Teneligliptin nanosuspension is stable during the stability study. Thus, it can be concluded that the nanosuspension method was commercially feasible and cost effective.

Evaluation of drug release, mucoadhesive and viscoelastic performances of Netildex gel versus an antibiotic‐steroid combination system

Purpose: The poor bioavailability and therapeutic response exhibited by conventional antibiotic‐steroid ophthalmic solutions due to rapid precorneal elimination of the drug may be overcome using a gel systems. Netildex gel is a preservative‐free product based on netilmicin and dexamethasone indicated for the treatment of inflammatory ocular conditions of the anterior segment and ocular adnexa including post‐cataract surgery. The current investigation evaluated the in vitro drug release, viscosity and mucoadhesion profile of Netildex gel in comparison to a gel matrix with regard to steroid and antibiotic delivery.Methods: In vitro drug release was assessed using Franz‐type diffusion cells, under sink condition, exploiting a simulated tear solution (STS) as dissolution medium and a regenerated cellulose membrane. Evaluation of mucoadhesive and viscoelastic properties were performed by texture analyzer TA‐XT2 and rheometer.Results: The dexamethasone and netilmicin release curves in Netildex gel exhibited a better sustained and controlled pattern over an extended time period (48 h) with respect to another gel system containing anti‐inflammatory and antibiotic drugs. The results were expressed as cumulative percentage of drug release and the antibiotics‐release kinetics from the polymeric matrix, evaluated by different mathematical models. The determination of detachment force demonstrated a significant mucoadhesive strength of Netildex gel compared to mucin. Moreover, rheological analysis of Netildex gel highlighted a strong pseudo‐plastic behaviour under shear strain due to its formulation features.Conclusions: Overall, Netildex gel exhibits a sustained and controlled drug release of both dexamethasone and netilmicin from polymeric matrix thanks to its viscoelastic and mucoadhesive properties allowing to prolong drug residence time on the ocular surface. These data support the reduced administration frequency while maintaining the same efficacy and simultaneously favouring patients' compliance [1].Reference1. Mencucci R. et al. Adv Ther (2022) 39: 5474–5486.

Design, Optimization and In vitro Evaluation of Mesalazine 400 mg Delayed Release Tablet for Colon Specific Delivery

Ulcerative colitis is a chronic inflammatory disease, and patients would get benefit more if the drug is given directly to the colon. Mesalazine is intended to deliver to the colon for treating ulcerative colitis. Here, we aimed to design and optimize mesalazine 400 mg delayed release tablet for colon-specific delivery using a quality by design (QbD) approach. The tablet was first formulated as an optimized core tablet and then coated with Eudragit S 12.5 for ensuring colonic delivery. The experimental design for the core tablet was constructed using a 32 full factorial design, where the percentages of sodium starch glycolate (SSG) and polyvinylpyrrolidone (PVP K-30) were independent variables and the tablet hardness (kg/cm2) and cumulative percentage of drug release at pH 7.2 phosphate buffer after 1.5 hours were treated as responses. Responses obtained from the initial exploratory formulations were evaluated to develop an optimized formulation to have a hardness value of 7-8 kg/cm2 and the maximum amount of drug release at pH 7.2 buffer. The optimized formulation involved the use of SSG and PVP K-30 at 3.05% and 1.69%, respectively. Hardness and cumulative percent of drug release obtained for the optimized core tablet were 7.8 kg/cm2 and 91.76%, respectively. The compatibility of drug and excipients was studied utilizing XRD, FTIR and TGA. The optimized core tablet was then coated with Eudragit S 12.5 to deliver the drug selectively to the colon and further assessed for its in vitro dissolution. Dissolution studies indicated that coated tablets with a weight gain of 7.4% exhibited the maximum cumulative percent of drug release (91.19 ± 0.11%), with a zero-order drug release profile (R2 = 0.943). A stability study performed according to ICH Q1A (R2) guidelines at accelerated storage conditions identified that there was no significant change in drug content over the storage period, indicating the stability of the formulated tablet batches. Together, these data suggest that the mesalazine tablet developed through the QbD approach offers excellent physical properties and drug release profile and, therefore, could be recommended for commercial manufacturing. Dhaka Univ. J. Pharm. Sci. 22(2): 189-201, 2023 (December)

Microemulgel Delivery of Ciprofloxacin Hydrochloride

Background: Ciprofloxacin hydrochloride is broad spectrum carboxyfluoroquinolone antibiotic from biopharmaceutics classification system (BCS) class IV. The oral dosage form exhibits gastric irritation whereas the topical cream has demonstrated poor penetration and low bioavailability. Objective: To optimize microemulsion-based gel of ciprofloxacin hydrochloride to increase its solubility and permeability through the cutaneous layer for targeting bacterial skin infections. Methods: To develop microemulsion, oil (soya oil, castor oil, oleic acid, isopropyl myristate and vegetable oil), surfactant (cremophore, span 80, tween 80) and cosurfactant (PEG 600 and PEG 400, propylene glycol) were evaluated. To depict the microemulsion formulation pseudo ternary phase diagram was employed. %Transmittance, zeta potential, dissolution study and size analysis were carried out for evaluation of microemulsion. 32 factorial design was used. Two variables i.e concentration of Sepineo P600 and Carbopol 934 effect on microemulgel was evaluated. Evaluation of gel was carried for physical parameters, antimicrobial, in-vitro and ex-vivo release study. Results: Solubility analysis suggested tween 80, oleic acid and propylene glycol for the formulation of microemulsion. Zeta potential for microemulsion batch F1 was -11.3 mV. This indicated good stability. In-vitro release study showed 91.98% percentage cumulative drug release for batch F1 at 8 hours. Microemulsion-based gel (F1) showed 22.96% inhibition against bacteria which proved its antibacterial activity. Conclusion: The obtained results exhibited that the permeability and bioavailability of the drug was increased when given through a topical route.

Olmesartan Medoxomil-Loaded Niosomal Gel for Buccal Delivery: Formulation, Optimization, and Ex Vivo Studies.

Olmesartan medoxomil (OLM) is a low bioavailability antihypertensive drug. This study aimed to prepare and optimize an OLM niosomal gel and investigate drug permeation via a chicken buccal pouch. OLM-loaded niosome were prepared using a film hydration technique. The vesicle size, zeta potential, entrapment efficiency, and percentage cumulative drug release of niosome were evaluated. The niosomes were incorporated into a Carbopol 974P (1.5% w/v) gel, and the drug permeability of the niosomal gel was evaluated. The formulations of the niosomal gel were optimized using the Box-Behnken design. The optimized formulation was further characterized by transmission electron microscopy (TEM) and Fourier transform infrared radiation analysis. The particle size and zeta potential of the optimized niosomal formulations were 296.4 nm and -38.4 mV, respectively. Based on TEM analysis, the niosomes were found to be spherical in shape. The permeability, flux, and permeability coefficient of the optimized niosomal gel were 0.507 mg/cm2, 0.083 mg/cm2 × hour, and 041 cm/hour, respectively. Histopathological evaluation revealed that the niosomal gel had better permeability than the OLM gel. Based on the results of the OLM niosomal gel, it can be concluded that the formulation can be beneficial in increasing bioavailability, resulting in better therapeutic efficacy.

Preparation and characterization of quetiapine fumarate loaded transfersome as a novel drug delivery system

Modern medicine delivery techniques like transdermal patches are vital for treating numerous disorders. With the aid of TDDS, first pass metabolism is prevented, which aids in achieving effective bioavailability. Drug molecules are also released into the systemic circulation at a controlled and predetermined rate. The objective of this study was creating matrix-type Quetiapine fumarate loaded transdermal patches with water bath method using different polymers like HPMC 5 cps, HPMC 15 cps, and Ethyl cellulose in different ratios. Polyethylene glycol-400, Dimethyl sulfoxide (DMSO) as a plasticizer and permeation enhancer, Solvents including methanol and chloroform in 1:1 ratio employed. FT-IR study indicated that pure drug and excipients are compatible with each other. The formulated patches are evaluated for thickness, weight variation, folding endurance, percentage moisture content, percentage moisture uptake, drug content and In vitro diffusion studies. A transfersomal formulation containing 25 mg of the drug and 10 mg of span 80 was concluded as the optimized formulation (F1) as it showed maximum drug entrapment (84.8%) and cumulative percent drug release (98.51%)

Development and optimization of mouth-dissolving strips of L-methyl folate: A modern approach for patient compliance

The goal of this study is to create a mouth-melting strip of L-methyl folate calcium, which will dissolve and disintegrate more quickly when given orally for the onset of action. : Solvent casting was used to create a calcium L-methyl folate film that dissolves in the mouth. Polymer, plasticizer, and flavouring agents were chosen after early experiments. Once the excipients were chosen, 3 complete factorial designs were used to improve the formulation. Folding endurance (Y1), tensile strength (Y2), and disintegration time (Y3) were chosen as dependent variables, whereas HPMC E5 concentration (X1) and glycerine concentration (X2) were chosen as independent variables. The film's physicochemical parameters, including SEM, thickness, percent elongation, percent cumulative drug release, and palatability, were measured for the optimized batch and compared to those of the commercial product. The formulation of the mouth-dissolving strip took into account outcomes from the trial batch, including transparency, stickiness, and brittleness. The optimal batch has 55% HPMC E5 and 14.9% glycerine, with a folding endurance of 59±0.23, a tensile strength of 4.18±0.07 N/m, and a disintegration time of 40±0.12 seconds. The optimized film has dimensions of 0.08±0.01 mm in thickness, 60±1.58 mg in mass, 15.33±0.25% in elongation, and 98.33±0.27% in content uniformity. The SEM results validate the uniform film with uniform drug distribution. After 3 minutes, the L-methyl folate calcium mouth-dissolving strip had a %CDR of 99.42%. Findings of f2=52.85 and f1=12.5 for the similarity factor suggest that the medication release is clinically and commercially equivalent. One month of stability at 30°C and 65%RH was observed for the improved batch. The results of the created mouth-dissolving strip test are satisfactory, indicating the intended medication release. When compared to pills that dissolve in the mouth, it is clear that it is more patient-friendly.

Formulation and Evaluation of Gastroretentive In Situ Gelling System of Ketoprofen

Abstract A revolutionary concept for achieving long-term medication release is the gastroretentive in situ gelling system. The goal of this research was to formulate and test a gastroretentive in situ gel for ketoprofen delivery to targeted site to increase the residence and delivery time. Ketoprofen gastroretentive in situ gels were synthesized using a cation-driven gelation approach using various combinations and concentrations of polymers such as gellan gum, sodium alginate, and hydroxypropyl methylcellulose (HPMC) K100M. Visual appearance, pH, viscosity, in vitro gelation, in vitro buoyancy, drug content, density measurement, gel strength measurement, water uptake, and in vitro drug release were all evaluated. The total floating time was more than 12 h, with a floating lag time of less than 2 min. The formulations showed pH ranging from 6.89 to 7.61 and drug content ranging from 82.01% to 95.53%. For 11 h, the percent cumulative drug release of formulations F5 and F14, which contained a greater concentration of polymer sodium alginate (1.5%) and a combination of gellan gum and HPMC K100M (0.175% and 0.2%), was 84.10% and 85.49%, respectively. In vitro dissolution experiments and stability investigations both revealed no significant changes in drug content. The findings revealed that the formulated in situ gels aided in extending gastric residence duration, allowing the drug to be released in the stomach.

Performance of Zr-Based Metal-Organic Framework Materials as In Vitro Systems for the Oral Delivery of Captopril and Ibuprofen.

Zr-based metal-organic framework materials (Zr-MOFs) with increased specific surface area and pore volume were obtained using chemical (two materials, Zr-MOF1 and Zr-MOF3) and solvothermal (Zr-MOF2) synthesis methods and investigated via FT-IR spectroscopy, TGA, SANS, PXRD, and SEM methods. The difference between Zr-MOF1 and Zr-MOF3 lies in the addition of reactants during synthesis. Nitrogen porosimetry data indicated the presence of pores with average dimensions of ~4 nm; using SANS, the average size of the Zr-MOF nanocrystals was suggested to be approximately 30 nm. The patterns obtained through PXRD were characterized by similar features that point to well-crystallized phases specific for the UIO-66 type materials; SEM also revealed that the materials were composed of small and agglomerate crystals. Thermogravimetric analysis revealed that both materials had approximately two linker deficiencies per Zr6 formula unit. Captopril and ibuprofen loading and release experiments in different buffered solutions were performed using the obtained Zr-based metal-organic frameworks as drug carriers envisaged for controlled drug release. The carriers demonstrated enhanced drug-loading capacity and showed relatively good results in drug delivery. The cumulative percentage of drug release in phosphate-buffered solution at pH 7.4 was higher than that in buffered solution at pH 1.2. The release rate could be controlled by changing the pH of the releasing solution. Different captopril release behaviors were observed when the experiments were performed using a permeable dialysis membrane.

Extraction, physicochemical characterization, functionality, and excipient ability of corn fiber gum-starch isolate from corn milling industry waste

Corn processing industries generate an extensive fibrous byproduct consisting of corn fiber gum (CFG) and residual starch (S). The present study hypothesized that CFG and S could be isolated as a single crosslinked conjugate. The isolated CFG-S conjugate was acidic, with a pKa value of 11.49, and a swelling index of 99.60%. Henderson–Hasselbalch equation predicted negligible ionization throughout the gastrointestinal pH range. The DSC thermogram highlights glass transition and temperature-specific structure stabilization through the exothermic crystallization domain. FTIR, SEM & XRD confirmed the structural conjugation and integrity of the conjugate. Tablets containing Venlafaxine hydrochloride as a model drug were prepared using CFG-S (14 and 57%) as excipient by wet granulation method. Percentage cumulative drug release with low concentration was up to 99.67175 ± 0.09 % in 5 h whereas with high concentration, it was extended to 12 h (P < 0.05). Korsemayer-Peppas release exponent indicates zero order (R2 = 0.9935) kinetics with super case-II anomalous transport showing diffusion and erosion as drug release mechanisms. The results confirmed that CFG-S isolate could act as a good binding agent at low concentrations and release extending cross-linked matrix former at a higher concentration for release retardant excipient.

PH sensitive in-situ gel for ophthalmic delivery of ofloxacin and dexamethasone sodium phosphate: Formulation, development, and evaluation

Ofloxacin and dexamethasone sodium phosphate will be used to create a gel-forming ocular medicine delivery system and examine its efficacy. Conventional dose forms have a number of drawbacks, including inadequate routes for drug transport to the posterior portion of ocular tissue, poor ocular drug bioavailability, and pulse-drug entry following topical administration and systemic exposure due to nasolacrimal duct outflow. Ofloxacin and Dexamethasone were obtained from Trimed Life Science Pvt. Ltd. Mumbai India. HPMC E50, Carbopol 930 was obtained from MET’s Institute of Pharmacy, Nashik. The developed formulation showed sustained drug release for 480 Minutes. While compared with marketed eye drop which shows drug release within 80 Minutes. The formulations were evaluated for different parameters like Clarity, pH of Sol, Gelling pH, Viscosity of Sol, Viscosity of gel, drug content, and Percentage Cumulative Drug Release. From these studies, formulation gives good clarity and satisfactory gelling pH along with good gelling capacity. The in situ gelling systems of Ofloxacin and Dexamethasone Sodium Phosphate were successfully developed. It also showed increased residence time with good gelling capacity at physiological pH and sustained drug release.