Drug Release Studies Research Articles

Posaconazole Loading and Release Behavior in Surface-Modified Mesoporous Silica Nanoparticular System

In conventional drug treatments, high toxic effects, low solubility, and low bioavailability of the active substance cause insufficient drug release in the target tissue and undesirable side effects in healthy tissue. Various drug delivery systems are utilized to eliminate these undesirable effects. Mesoporous silica nanoparticles (MSN) are biocompatible biomaterials that have a large surface area, high pore volume, and enhanced adsorption capacity. With MSN-mediated controlled drug release, the active substance concentration in the blood is kept within the desired therapeutic range. Posaconazole (PCZ) is an antifungal agent. Absorption of PCZ is difficult due to its low solubility in aqueous and acidic environments, low therapeutic effect and low bioavailability. The use of controlled drug release systems avoids these problems and facilitates the absorption and release of PCZ. In this study, it is aimed to enhance the PCZ adsorption and release by using a drug delivery system. MSNs were synthesized by sol-gel method, and surface modification of nanoparticles was achieved using (3-Aminopropyl) triethoxysilane (APTES). PCZ was loaded on APTES-modified MSN successfully. MSN, APTES-modified MSN and PCZ loaded APTES-modified MSN were characterized. Diffusion controlled release of PCZ was observed in drug release studies.

Generic selection criteria for safety and patient benefit [Ⅻ]: Comparing the physicochemical and pharmaceutical properties of brand-name and generic tulobuterol tape.

Physicochemical properties (drug release, peel strength, adhesion, and stiffness) of Hokunalin® Tape (Hokunalin) and 13 generic transdermal bronchodilator patches containing tulobuterol were characterized and evaluated for comparison. Drug-release studies evaluating sustained release behavior demonstrated better performance by the drug Hokunalin, than the generics MED, YP, Sawai, and Teikoku. Hokunalin yield a 16.2% release 1 hour after initiation, 30.1% at 3 hours, 50.0% at 8 hours. In comparison, the generics MED, YP, Sawai, and Teikoku showed an intermediate release behavior to that of Hokunalin, with more than 80% release after 8 hours. A 90-degree peel adhesion test for tape peel strength demonstrated that the generic MED (4.99 N), YP (3.26 N), Sawai (4.17 N), and Teikoku (4.37 N) tapes yielded significantly higher values compared to Hokunalin (2.66 N). Probe tack tests, evaluating adhesive strength, yielded significantly higher values for the generics HMT (4.89 N)and Towa (4.25 N) compared to Hokunalin (3.66 N). Furthermore, for the stiffness-softness test, a significantly higher value was obtained for each generic yielded compared to Hokunalin (3.7-degree). These factors are important components of product qualities that affect treatment efficacy, including "ease of application" and other usability factors.

Development of Polymeric Nanoparticles of Sunitinib malate in Eudragit S 100 for anti-colon cancer targeted drug delivery

Sunitinib malate (SM) is a multi-targeted tyrosine kinase (TK) inhibitor. It is proposed as a potent anticancer drug intended for colon cancer. The current work aimed at developing Sunitinib malate -loaded nanoparticles for colon- targeting. SM loaded ES100-nanoparticles were developed by nano-precipitation method using poly vinyl alcohol (PVA) as stabilizer. Different formulation of ESNP (F1-F3) were prepared and evaluated for particle size, poly-dispersity index, and drug entrapment, using Fourier transform infrared spectroscopy (FTIR), x-ray diffraction (XRD), and scanning electron microscopy (SEM). The optimized formulation was further studied by in-vitro drug release and anticancer cell line study. The mean particle size, PDI, %EE of optimized SM loaded ESNPF2 was found to be 384.8±5.53 nm, 0.58, and 60.31% respectively. In vitro release of the optimized ESNPF2 showed 10.2 % drug release till 2 h, at 4h 29.6% and 12 h and 24 h 66.45%, 82.2% respectively at pH 7.4. SEM images and surface morphology confirmed that nanoparticles were spherical and had smooth surfaces. An MTT assay was conducted in the colon cancer cell lines (CACO2) to evaluate anti-cancerous activity of SM. SM loaded ESNPF2 showed a high potential against colon cancer cells. The overall results suggest that SM loaded ES100-nanoparticels could be a potential option for colon targeting.

Formulation and Drug Release Study of Rivaroxaban Oral Disintegrating Tablets Using Various Super-Disintegrants

This study aims to improve Rivaroxaban's solubility, dissolution, and bioavailability. Orally disintegrating tablets (ODTs) made with super-disintegrants like crospovidone, sodium starch glycolate, and cross-carmellose sodium will do this. Tablet preparation used direct compression and formulation optimization with design expert software. After a thorough factorial design and evaluation of pre- and post-compression parameters, the F3 batch, which contained Rivaroxaban (7.97%), Crospovidone (3.59%), Croscarmellose sodium (5.18%), Sodium Starch Glycolate (5.18%), Lactose Anhydrous (31.08%), Mannitol (15.94%), MCC (27.89%), SSF (1.59%), and Talc (1.59%), was the best. The enhanced tablet formulation (F3) showed positive qualities, including 3.3 kg/cm² hardness, 23 seconds disintegration time, and 99% drug release after 30 minutes. The innovative Rivaroxaban orally disintegrating tablet (ODT) method disintegrated and dissolved faster than market forms. Rivaroxaban's physical and chemical properties were assessed before formulation. The medication was colorless, scentless, crystalline, and melted at 227°C-229°C, as described in published research. The pharmaceutical was found to be a BCS Class II drug with low water solubility and high solubility in acetate buffer pH 4.5 and 0.1 N Hydrochloric acid. Fourier-transform infrared spectroscopy (FTIR) confirmed no drug-polymer-excipient interactions. Every batch of tablets exhibited uniform thickness (3.5 mm to 3.8 mm) and diameter (10.31 mm to 10.36 mm), indicating good compression without adhering to shaping tools. All samples had a 3-5 kg cm-² hardness, indicating strong mechanical properties. The Roche friability method showed that all batches had good abrasion resistance, ranging from 0.1% to 0.5%. Variations in croscarmellose sodium and crospovidone on tablet disintegration time and hardness were examined using design expert software. The ANOVA showed important factors affecting these attributes. Data-driven polynomial equations predict tablet disintegration time and hardness. These models reveal formulation parameters that affect tablet performance. Thus, the improved F3 batch of rivaroxaban orally disintegrating tablets (ODTs) improves solubility, dissolving, and bioavailability. This may improve treatment outcomes.

Continuous preparation of sustained release vildagliptin nanoparticles using tubular microreactor approach

This investigation used a tubular microreactor to produce Vildagliptin (VLG) loaded ethyl cellulose (EC) nanoparticles (NPs) for sustained delivery of a drug. A central composite design was used to quantify the influence of independent variables on the desired responses. The independent factors selected to achieve the desired entrapment efficiency and sustained drug release were EC concentration and sodium lauryl sulfate concentration. On the other hand, the dependent variables chosen for assessment were particle size (Y1) and encapsulation efficiency (Y2). The nanoparticles produced were analyzed, which included particle size measurement, transmission electron microscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, encapsulation efficiency (EE) determination, and in vitro drug release study. The optimized samples TEM investigation verified the nanoparticles’ spherical shape and particle size distribution, ranging from 160 to 250 nm. The entrapment efficiency (EE) fell within the range of 63–87%. In the in-vitro drug release study, VLG-loaded EC nanoparticles exhibited sustained release over 12 h. Applying various kinetic equations to the in-vitro drug release data demonstrated that the drug release mechanism involved diffusion. This comprehensive study concluded that the VLG-EC-NPs achieved optimal particle size, EE, and desirable level of sustained drug release.

Development and Characterization of Novel Chitosan-Coated Curcumin Nanophytosomes for Treating Drug-Resistant Malaria.

This study aimed at enhancing the efficacy of curcumin (CR) by formulating and coating it with chitosan. In silico molecular docking studies revealed that CR exhibited almost similar and low binding energies when compared to artemisinin, indicating high stability at the target site. It can be confirmed that CR is effective in treating and reducing Plasmodium falciparum parasites. Fourier transform infrared studies confirmed that there was a shift and disappearance of some drug peaks in the formulation which revealed complexation with phospholipids. The F2EXT3-developed formulation exhibited greater solubility (24.31 ± 3.47 μg/mL) when compared to pure CR (7.99 ± 1.95 μg/mL). Proton nuclear magnetic resonance studies confirmed the formation of Curcumin-phospholipid hydrogen bonding in F2EXT3. The in vitro drug release studies revealed that the developed formulation F2EXT3 exhibited better drug release at 71.98% at 48 h; this might be due to the effective entrapment efficiency of the drug inside the phospholipid, presence of polyethylene glycol 4000 and chitosan further assisted in sustained release of the drug. Scanning electron microscopy studies revealed that optimized F2EXT3 CR nanophytosomes were nearly spherical with narrow size distribution and smooth surface. The zeta potential of the F2EXT3 showed -3.5 mV. Stability studies revealed that the formulation remained stable even after 6 months. It was observed from the hemin assay that CR and F2EXT3 exhibited (50 μg/mL curcumin) exhibited IC50 values of 47 ± 2.45 and 22 ± 1.58 μM, respectively. Further in vivo antimalarial activity on resistant and sensitive strains needs to be performed to evaluate the efficacy of the developed formulation.

Design, Development, and Characterization of Lyophilized Posaconazole-Loaded Mixed Micelles for Improved Fungal Treatment and Stability

Posaconazole, a BCS class II drug with poor solubility, hampers its absorption in the body, leading to suboptimal drug levels and reduced treatment effectiveness. To address this issue, this research aimed to develop a lyophilized powder of posaconazole-loaded mixed micelles (POS-MMs) using pluronic F68 and soluplus to enhance fungal treatment and stability. A 32 factorial design optimized the POS-MMs formulation by varying PF68 and soluplus concentrations. Various characterization techniques were employed, including particle size analysis, zeta potential measurement, FTIR, DSC, and XRPD. In vitro drug release studies indicated sustained release with 79.4% released within 24 hrs, while in vitro hemolysis studies confirmed biocompatibility. Lyophilization with lactose as a cryoprotectant was successful, yielding a stable formulation over three months. The optimized POS-MMs exhibited a particle size of 66.30 ± 2.10 nm, a high % entrapment efficiency of 94.88 ± 2.4%, and a desirable zeta potential of -25.3±2.8 mV. These findings highlight the potential of POS-MMs to enhance the therapeutic outcomes of posaconazole in the treatment of fungal infections. In addition, lyophilized powder is a promising technique for improving the stability of POS-MMs.

Improving astaxanthin-loaded chitosan/polyvinyl alcohol/graphene oxide nanofiber membranes and their application in periodontitis

Periodontitis is a chronic inflammatory disease primarily driven by host inflammation and plaque-induced immune responses. Controlling the host inflammatory response and improving the periodontal inflammatory microenvironment are crucial to promoting periodontal tissue regeneration. In this study, the blended nanofiber membranes previously prepared by our research group were improved, and we developed multifunctional chitosan/polyvinyl alcohol/graphene oxide/astaxanthin coaxial nanofiber membranes. Scanning electron microscopy showed that the prepared nanofibers had a smooth surface and a uniform diameter distribution. The mechanical property test results showed that the coaxial nanofiber membranes exhibited higher tensile strength compared to the blended nanofiber membranes, which increased from 4.50 ± 0.32 and 3.70 ± 0.45 MPa to 7.12 ± 0.22 and 5.62 ± 0.79 MPa respectively. Drug release studies indicated that the “shell-core” structure of coaxial nanofibers significantly reduced the initial burst release of astaxanthin (ASTA), with only 13.49 % and 10.71 % release in the first 24 h, and drug release lasted for over a week. Animal experiments confirmed that the coaxial nanofiber membranes loaded with ASTA promoted periodontal bone defect repair while inhibiting periodontal inflammation. In conclusion, the prepared coaxial nanofiber membranes are a promising sustained-release drug system for treating periodontitis.

Formulation, Optimization, and Evaluation of Gliclazide loaded Nanosuspension for Dissolution Rate Enhancement

Diabetes mellitus is a prolonged metabolic condition categorized through elevated blood glucose levels. To treat this condition, oral antihyperglycemic medications like gliclazide, a second-generation sulfonylurea insulin secretagogue, are commonly used. Gliclazide comes into the biopharmaceutical classification system (BCS) class-II types, known for its lower solubility. To enhance its solubility, gliclazide was integrated into nanosuspensions. This study focused on formulating these gliclazide nanosuspensions using Kollicoat IR and Soluplus through the anti-solvent-precipitation method, through optimization achieved using the Box Behnken Design. Key parameters assessed included particle size (224 ± 1.23 nm) and entrapment efficiency (95.65 ± 0.12%). The drug release studies conducted on pH 7.4 indicated that over 95% of the drug was released within 30 minutes for the nanosuspension, whereas the pure drug solution released less than 70% in the same time frame, indicating immediate release with the nanosuspension. The morphology was examined using scanning electron microscopy (SEM), while fourier transform infrared (FTIR), X-Ray diffractometers (XRD), and differential scanning calorimeter (DSC) analyses confirmed the presence of the drug within the nanosuspension. In summary, the incorporation of gliclazide into nanosuspensions proved successful, resulting in enhanced release characteristics and ameliorated solubility.

Formulation and Evaluation of Mouth Dissolving Tablet of Biperiden HCL for Treatments of Parkinson’s Disease

Seven formulations were developed using superdisintegrating substances like sodium starch glycolate, crospovidone, and cross-carmellose sodium at different concentrations. Three batches were created by employing varying concentrations of the super disintegration approach, utilizing sodium starch glycolate as the superdisintegrating agent. The batches underwent evaluation regarding sensory characteristics, firmness, breakability, weight consistency, disintegration time in a simulated environment, time is taken for wetting, laboratory tests on drug release within a controlled environment, and assessments of product stability. Fourier transform infrared spectroscopy (FTIR) studies confirmed the absence of drug-excipient interactions. In this examination, mouth-dissolve tablets of biperiden HCL were successfully ready with favorable parameters, including organoleptic properties, hardness (3.2 kg/cm3), friability (0.23%), weight variation (100 mg), disintegration time within a controlled laboratory environment (17 seconds), wetting time (11 seconds), and in-vitro drug release studies (99.80%). The study concluded that the biperiden hydrochloride mouth-dissolving tablet was effectively formulated using the direct compression method, demonstrating improved patient compliance.

Development and Evaluation of Eplerenone Microbeads as Floating Drug Delivery System using Design of Experiment

The present study was designed to formulate floating microbeads of eplerenone for decreasing dosing frequency and increasing gastric residence. The floating properties of the gastric juice were used to control the stomach stay time. Eplerenone was selected as a model bioactive which is used in lowering blood pressure by loading into floating microspheres was designed by using polymer ethyl cellulose and solvent ratio (Dichloromethane: methanol), keeping. The floating microbeads were studied for their drug entrapment efficiency, shape, percentage yield, and particle size, surface morphology, in-vitro drug release studies, percentage buoyancy, and formulation stability studies. Dichloromethane we used (DCM) as a constant and stirred them for hours. The study showed that fluid evaporation can be used to make floating microbeads that contain eplerenone. This method can be used to successfully make eplerenone-loaded floating microbeads. The study showed that making floating eplerenone microbeads with controlled release is a good way to cut down on how often you have to take your medicine.

In silico exploration of venlafaxine, a potential non-tricyclic antidepressant in a liposomal formulation for nose-to-brain drug delivery

Objective Non-tricyclic antidepressants (non-TCAs) work by preventing the intake of norepinephrine and serotonin. Therefore, the aim of this study was to identify a potent non-TCAs and to develop liposomal formulation, characterize and to determine the drug release study across model of dialysis membrane via in vitro and in silico techniques. Methods The in silico docking analysis identified venlafaxine (VLF) as the best non-TCAs with the depressant targets (PDB ID: 3PBL and 4BVN). VLF-loaded liposomal formulation was prepared by the thin-film hydration technique and characterized by physicochemical properties, including entrapment efficacy, in vitro drug release, particle size analysis, and FTIR. Moreover, this article also compares VLF and VLF-loaded with liposome carriers (LPs) based on nose-to-brain drug delivery approaches to treating depression. Results Drug release profiles of the optimal liposomal formulation of VLF-LPs were examined in the high entrapment efficiency 94.13 ± 1.20% was attained at 224 nm, composed of spherical particles having a mean particle size of 191 ± 2.0 nm, a polydispersity index of 0.281 ± 0.06 and zeta potential of −20.3 mV. The best formulation of VLF-LPs was more effective than oral VLF treatment, as shown by the in vitro drug release data. Conclusion The results show that the VLF-LPs formulation is a promising potential platform for application in nose-to-brain drug delivery. Thus, highlighting the robustness of the intranasal drug delivery system with enhanced pharmaceutical properties, efficacy, and bioavailability for the anti-depression effect.

Designing, Creating, and Assessing a Modified Pulsincap Delivery System for Intestine Targeting of Fluvastatin in Accordance with Circadian Rhythm

The current study’s objective remains to create the Pulscap delivery system using an insoluble capsule core that contains fluvastatin sodium microspheres. Eudragit RL 100 polymer fluvastatin sodium microspheres were made using the solvent evaporation method. To reduce the possibility of stomach upset, these microspheres were hand-filled into capsules, plugged with hydrogel plugs, then sealed with ethyl cellulose acetate and dipped in an eight: two (vol/vol) Acetone: ethanol solution by butyl pthalate of (0.75%) and 5% cellulose acetate phthalate solution. Formulated dosage form was assessed for in-vivo X-ray imaging studies, in-vitro drug release studies, and in-vivo imaging studies, pharmacokinetic study of the optimized formulation was conducted in a two-way cross-over design with 6 rabbits in each group and the pharmacokinetic parameters (Cmax, Ka, Ke, MRT and AUC0-α) are measured. A Pharmacodynamics study was also performed on lipid profiles in six groups of rabbits. Optimized formulation (F20) which is prepared with a drug and polymer ratio of 1:3, is selected based on a dissolution study which shows a percentage release of 99.98. ± 0.12% at 17th hour. In the in-vivo study, the plasma concentration at 12th hour 53.8 ± 0.02% and at 32nd hour 13.9 ± 0.05%. Pharmacokinetic parameter Cmax (ng/mL): 53.8 ± 0.41, MRT (h): 20.0 ± 0.14, t1/2 (h): 8.52 ± 0.014, Kel (h-1) :0.08 ± 0.014, Ka (h-1):0.25 ± 0.02, AUC0-a (ng h/mL): 944.9. ± 4.05. Serum lipid profile in high cholesterol rabbit after treatment with F20 formulation total cholesterol:240.83 ± 19.76, HDL-C:37.33 ± 2.16, triglycerides:318.67 ± 7.74, VLDL-C:63.73 ± 1.55, LDL-C:139.77 ± 18.74. Compared to lovastatin SR release, lovastatin pulsatile release, and fluvastatin SR release, the results imply that the F20 formulation’s pulsatile drug delivery has established good drug delivery for medications entering the gastrointestinal tract, and it displays superior pharmacokinetic and pharmacodynamic parameters.

Colon-targeted delivery of niclosamide from solid dispersion employing a pH-dependent polymer via hotmelt extrusion for the treatment of ulcerative colitis in mice

Niclosamide (NCL) is repurposed to treat inflammatory bowel disease due to its anti-inflammatory properties and potential to reduce oxidative stress. This therapeutic activity remains challenging if administered directly due to its low solubility and high recrystallization tendency in gastric pH. Solid dispersions using pH-dependent polymer will be a better idea to improve the solubility, dissolution and targeted delivery at the colon. Hot melt extrusion was used to formulate a solid dispersion with 30% NCL utilising hydroxypropyl methylcellulose acetate succinate as a pH-dependent polymer. In vitro drug release studies revealed formulation (F1) containing 10%w/w Tween 80 showed minimal release (2.06%) at the end of 2 h, followed by 47.87% and 82.15% drug release at 6 h and 14 h, respectively, indicating the maximum amount of drug release in the colon. The drug release from the formulations containing no plasticiser and 5%w/w plasticiser was comparable to the pure crystalline drug (approximately 25%). Solid-state analysis confirmed particle conversion of crystalline NCL to amorphous form, and the optimised formulation was stable for 6 months without significant changes in dissolution profile. In contrast to pure NCL, the F1 formulation substantially reduced the disease activity index, colonic inflammation, histological alterations and oxidative damage in colitis mice. These findings reveal that the prepared formulation can potentially deliver the drug locally at the colon, making it an effective tool in treating ulcerative colitis.

In vitro 5-fluorouracil release properties investigation from pH sensitive sodium alginate coated and uncoated methyl cellulose/chitosan microspheres

5-Fluorouracil (5-FU) has been in clinical practice for decades one of the oldest chemotherapy agents. However, intravenous administration of 5-FU requires the development of an oral controlled delivery system for improved patient compliances. For this purpose, 5-FU loaded and sodium alginate (NaAlg) coated and uncoated methyl cellulose (MC)/chitosan (CS) microspheres were prepared by emulsion crosslinking method using a mixture of water and oil. Firstly, MC/CS microspheres were prepared and then coated with NaAlg. The prepared microspheres were characterized by optical microscopy, Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC). Microspheres were also characterized by equilibrium swelling values and drug release profiles. The in vitro drug release studies were carried out with three pH values 1.2, 6.8, and 7.4, respectively, each for 2 h. It was determined that coating the microspheres with NaAlg provides more controlled drug release, especially at pH 1.2. The effects of the preparation conditions, such as coating time, MC/CS ratio, NaAlg concentration, and crosslinker concentration on the 5-FU release were investigated.

Fabrication of dual drug-loaded polycaprolactone-gelatin composite nanofibers for full thickness diabetic wound healing.

Aim: Design of moxifloxacin and ornidazole co-loaded polycaprolactone and gelatin nanofiber dressing for diabetic wounds. Materials & methods: The composite nanofibers were prepared using electrospinning technique and characterized for in vitro drug release, antibacterial activity, laser doppler and in vivo wound healing. Results: The optimized nanofiber demonstrated an interconnected bead free nanofiber with average diameter <200nm. The invitro drug release & antimicrobial studies revealed that optimized nanofiber provided drug release for >120h, thereby inhibiting growth of Escherichiacoli and Stapyhlococcusaureus. An in vivo wound closure study on diabetic rats found that optimized nanofiber group had a significantly higher wound closure rate than marketed formulation. Conclusion: The nanofiber provided prolonged drug release and accelerated wound healing, making it a promising candidate for diabetic wound care.

Towards a novel pullulan and pullulan-enteric hard capsules: Study of drug release and crucial capsule features

Pullulan, a natural polymer, is often used as a plant-based alternative polymer for gelatin to produce hard capsules. To the best of our knowledge, there have been negligible studies on the performance of enteric pullulan capsules. Hence, this paper describes a new formulation for enteric pullulan hard capsules that can resist the acidic environment of the stomach and release the drug in the small intestine without the need for an exterior coating. This formulation consists of three polymers, including pullulan, Eudragit L100, and κ-carrageenan, which are used to develop resistance against acid and facilitate gelation to form capsules. With regards to the humidity assessment of target hard capsules, it is estimated that the prepared capsules possess an appropriate potential for target utilizations. The capsules were tested using esomeprazole as a model drug for dissolution testing. The results demonstrated that the enteric hard-shell capsules remained stable for 2 h in 0.1 N HCl at a pH of 1.2 and then ruptured upon entering a phosphate buffer (simulated small intestine) medium at a pH of 6.8. The FESEM and cross-sectional analysis revealed that no drug was released due to the absence of pores on the surface. Rheological examinations also revealed that the prepared solution have a desirable property. It is certified that the NMR spectrum proposes the existence of crosslinking and polymerization of pullulan which signifies appropriate existing interactions polymeric binders and gelling agent. TGA and DSC evaluations are in well accordance with the strong cross-linked structure generated by comprising pullulan polymer with the Eudragit pH-sensitive Polymer. Overall. this new formulation has potential feature for utilization in drug delivery systems where controlled release is desired, especially for drugs that are sensitive to acidic environments in the stomach.

Development of microemulgel formulations with varied permeation enhancers for transungual delivery of luliconazole in onychomycosis management

Luliconazole-loaded microemulgels containing different permeation enhancers were formulated for transungual drug delivery for the management of onychomycosis, onychomycosis, which affects nails. The physicochemical properties like droplet size, zeta potential, pH, viscosity, spreadability, extrudability, oil binding capacity, drug content, and microscopic study were evaluated. The Pseudo-ternary phase diagram was constructed for the formulation of microemulsions (MEs) by keeping the Km ratio constant at 3:1 and characterized for clarity, mean droplet size, zeta potential, viscosity, pH, transmittance, refractive index, and stability. The ME mean droplet size and zeta potential were found in the range of 38.78 to 171.4 nm, and 0.00 to − 6.6 mV, respectively. Prepared MEs were converted into microemulgel by adding a 2.5% gelling agent (Carbapol 934) in the external phase, and a drug release study was conducted. Formulation E3 showed better drug release and was chosen as the control. Four different penetration enhancers were added separately within E3 and further evaluated for pH, viscosity, spreadability, extrudability, oil binding capacity, drug content, microscopic study, Compatibility study, XRD, and DSC. A favorable docking score was observed between luliconazole and Lanosterol 14-alpha-demethylase. In-vitro cumulative drug release at the end of 24 h from E3-SS, containing sodium sulfide as a penetration enhancer, was found to be 94.70% and was 2 times more than the control formulation. Ex-vivo transungual permeation studies through cutting nail clippings were found to be in the range of 28.18 - 36.52 µg/mm2. The microemulgels tagged as E3, E3-SS, and E3-SL showed a significant zone of inhibition against Candida albicans and Aspergillus fumigatus as compared to the marketed formulation.

Preparation of protein nanoparticles using diselenide functionalized gelatin for redox responsive release of doxorubicin

The present study demonstrates the fabrication of a nanocarrier system using diselenide conjugated gelatin (G-Se-Se-G) for the redox responsive delivery of a wide spectrum anticancer drug, doxorubicin (Dox). The method involves nanoprecipitation of the aqueous solution of G-Se-Se-G employing ethanol and F68 as the desolvating and stabilizing agents respectively. The drug, Dox is loaded within the nanocarrier by entrapment method during the nanoparticle synthesis. The physico-chemical characterizations confirm the formation of nanoparticles of regular spherical shape with hydrodynamic size, surface charge and loading efficiency of 181 ± 12.6 nm, -13.10 ± 0.83 mV and ∼9 % respectively. Notably, Dox loaded G-Se-Se-G carrier shows significantly higher drug release in response to acidic (pH = ∼5.5) and reducing (10 mM glutathione) sink conditions. Dox release kinetic data fitted to a universal Korsmeyer–Peppas model suggests that irrespective of the nature of stimuli, the release of Dox from G-Se-Se-G carrier follows non-Fickian mechanism which is attributed to the diffusion and erosion. The cytotoxicity studies employing human lung adenocarcinoma (A549) and human normal lung fibroblast (WI38) cells confirm the potency as well as selectively of Dox loaded G-Se-Se-G carrier towards cancer cells. The intracellular drug release studies through fluorescence imaging indeed corroborate the redox (reducing environment) mediated preferential release of Dox from G-Se-Se-G carrier in A549 cells as compared to WI38 cells. Finally, in vivo studies using A549 derived xenograft tumor model establishes that Dox loaded G-Se-Se-G nanocarrier is better tolerable than free Dox with almost similar efficacy.

Formulation and Evaluation of Herbal Transdermal patches for Rheumatoid arthritis

The allopathic healthcare system provides two conventional ways of treatment for rheumatoid arthritis, both of which have side effects. As a result, turning to Ayurvedic herbal treatment formulation that is safe, effective, and proven would be a better choice. Rheumatoid arthritis is an autoimmune disease that is chronic and progressive ,distinguished by chronic inflammation affecting the peripheral joints. Transdermal films containing herbal medicinal plants such as Cardiospermum helicacabum and Aloe barbadensis were designed in this study to treat rheumatoid arthritis . The solvent casting method was used to develop transdermal patches using plant extracts. The patches were evaluated based on physicochemical parameters such as thickness, folding endurance, physical appearance, weight uniformity, moisture content, drug content, flatness, moisture uptake, pH, and invitro drug release and stability study. The plots for average absorbance release vs time through transdermal film shows that drug release occurred at a steady rate. The skin irritation study on human volunteer's skin revealed that the formulation does not cause skin irritation. Overall, the present research provides a novel approach to the implementation of transdermal drug delivery techniques in the design of herbal remedies.