Drug Release Studies Research Articles

Synthesis and characterization of ZnO quantum dot-functionalized mesoporous nanocarriers for controlled drug delivery

In this study, ZnO quantum dots (ZnO@QDs) were synthesized and functionalized with 2nd generation poly amido amine (2GPD) using 3-amino-propyl tri-methoxy silane as the initiator core, facilitated by tetramethylammonium hydroxide (TMAH) to enhance stability against oleate coating. Concurrently, a mesoporous substrate with a unique morphology was developed as a drug reservoir for doxorubicin loading. ZnO quantum dots displayed photoluminescence radiation, with dimensions ranging from 5 to 7 nm and exhibiting spherical morphology. The cubic structure of the synthesized mesoporous nanocatalysts was also confirmed. Brunauer-Emmett-Teller analysis indicated a multidimensional porous structure of the nanocarriers, while zeta potential analysis showed a stable system (approximately −9.6 mV). Fourier transform infrared spectroscopy, X-ray diffraction, and energy dispersive spectroscopy corroborated these findings. Drug release studies demonstrated sustained release under acidic conditions (pH 5.5), with an efficiency of approximately 94 %. These results highlight the potential applications of this nanosystem for controlled drug delivery, underscoring its practical implications in the field of nanotechnology.

Enhancement of Cognitive Function by Andrographolide-Loaded Lactose β-Cyclodextrin Nanoparticles: Synthesis, Optimization, and Behavioural Assessment.

This study investigates whether Andrographolide-loaded Lactose β-Cyclodextrin (ALN-βCD) nanoparticles enhance cognitive function, particularly spatial learning and memory. The successful conjugation of lactose to β-cyclodextrin was confirmed via 1H NMR spectroscopy, facilitating neuronal cell entry. The solvent evaporation method was used to create the nanoparticles, which were characterised for particle size, PDI, zeta potential, and drug release. The nanoparticles exhibited a size of 247.9 ± 3.2 nm, a PDI of 0.5 ± 0.02, and a zeta potential of 26.8 ± 2.5 mV. FTIR and TEM analyses, along with in vitro drug release and BBB permeability studies, confirmed their stability and efficacy. Behavioural tests, including the Elevated Plus Maze, Y-Maze, Object Recognition, and Locomotor Activity tests, demonstrated significant improvements in memory, motor coordination, and exploration time in the nanoparticle-treated groups. The group treated with ALN-βCD at a dose of 100 mg/kg/p.o. showed superior cognitive performance compared to the group receiving free andrographolides (AG). Biochemical assays indicated a significant reduction in acetylcholinesterase activity and lipid peroxidation, suggesting increased acetylcholine levels and reduced oxidative stress. Histopathological examination showed improved neuronal function without toxicity. The results showed significant improvements (p < 0.001) in memory and cognitive abilities in experimental animals, highlighting the potential of ALN-βCD nanoparticles as a non-invasive treatment for memory loss. These promising findings warrant further exploration through clinical trials.

Evaluating the potential of ethyl cellulose/eudragit-based griseofulvin loaded nanosponge matrix for topical antifungal drug delivery in a sustained release pattern

Fungal infections are very alarming nowadays and are common throughout the world. Severe fungal infections may lead to a significant risk of mortality and morbidity worldwide. Sustained delivery of antifungal agents is needed to mitigate this problem. In the current study, an attempt has been made to formulate griseofulvin-loaded nanosponges using the quasi-emulsion solvent diffusion technique. For characterization, griseofulvin loaded nanosponges were tested by different instrumental techniques such as optical microscopy, scanning electron microscopy (SEM), powder X-ray diffractometer (PXRD), Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), and transmission electron microscopy (TEM). The antifungal activity of the nanosponges was assessed against Candida albican strain using the agar well-diffusion method. Finally, the drug-loaded nanosponges' in vitro sustained release activity was evaluated. FTIR spectra showed no chemical interference between the drug and polymers. Some of the peaks of the drug are not visible in the FTIR spectrum, which suggests drug entrapment. PXRD data showed that the drug lost its high crystallinity when entrapped in the nanosponge matrix. From the morphological studies via SEM and TEM, a brief idea of the surface morphology of the nanosponges was obtained. The small pores throughout the structure proved its high porosity. The antifungal sensitivity assay was successful, and a zone of inhibition was observed in all the formulations. The in-vitro drug release study showed sustained behaviour. The sustaining effect was due to the polymer and cross-linker used, which gave rise to a porous scaffold matrix. From the results, it can be concluded that griseofulvin-loaded nanosponges can be used for antifungal drug delivery against various topical skin infections.

Formulation Development and Evaluation of Polyherbal Emulgel for Anti Inflammatory Activity

This study focuses on the formulation development and evaluation of a polyherbal emulgel incorporating curcumin and coriander seed oil, aimed at enhancing anti-inflammatory activity. Preformulation studies were conducted to characterize the physical, chemical, and mechanical properties of the active substances, and to establish a robust basis for the formulation approach. Various parameters including solubility, melting point, partition coefficient, and drug-excipient interactions were assessed to ensure compatibility and efficacy. The emulgel was prepared through a systematic process involving the preparation of a gel base, oil phase, aqueous phase, and subsequent emulsification. The final product was evaluated for various properties such as physical appearance, homogeneity, pH, spreadability, extrudability, swelling index, viscosity, drug content, and in vitro drug diffusion. Stability studies were also conducted over three months to ensure the longevity and reliability of the formulation. Results indicated that the formulated emulgel exhibited desirable physical properties, optimal pH, high spreadability, good extrudability, and a significant swelling index. Viscosity measurements confirmed appropriate consistency, while drug content analysis ensured accurate dosing. In vitro drug release studies demonstrated sustained release profiles, fitting well with kinetic models. Additionally, in vivo anti-inflammatory activity was assessed using a carrageenan-induced paw edema model in rats, showing promising results with notable inhibition of inflammation. Overall, the polyherbal emulgel formulation developed in this study offers a promising alternative for anti-inflammatory therapy, combining the therapeutic benefits of curcumin and coriander seed oil in a stable and effective dosage form. Further studies are recommended to explore clinical efficacy and potential applications in broader therapeutic areas

Impact of PEG Content on Doxorubicin Release from PLGA-co-PEG Nanoparticles.

Nanoparticles (NPs) have become attractive vehicles for drug delivery in cancer therapy due to their ability to accumulate in tumours and mitigate side effects. This study focuses on the production of doxorubicin (DOX)-loaded NPs comprising Poly (lactic-co-glycolic acid)-Polyethylene glycol with varying PEG proportions and the examination of their impact on drug release kinetics. DOX-loaded NPs, composed of PLGA-co-PEG with PEG contents of 0%, 5%, 10%, and 15%, were synthesized by the solvent evaporation technique, exhibited spherical morphology, and had sizes ranging from 420 nm to 690 nm. In vitro drug release studies revealed biphasic profiles, with higher PEG contents leading to faster and more extensive drug release. The Baker-Lonsdale model demonstrated the best fit to the drug release data, indicating that the release process is diffusion-controlled. The diffusion coefficients for DOX determined ranged from 6.3 × 10-18 to 7.55 × 10-17 cm2s-1 and exhibited an upward trend with increasing PEG content in the polymer. In vitro cytotoxicity tests with CHO cells showed that unloaded NPs are non-toxic, while DOX-loaded PLGA-PEG 15% NPs induced a greater decrease in cellular viability compared to their PLGA counterparts. A mathematical relationship between the diffusion coefficient and PEG percentage was derived, providing a practical tool for optimizing DOX release profiles.

Cholic Acid-Grafted Thiolated Chitosan-Enveloped Nanoliposomes for Enhanced Oral Bioavailability of Azathioprine: In Vitro and In Vivo Evaluation.

The purpose of the present study was to develop a cholic acid-grafted thiolated chitosan (CA-CS-TGA) polymeric biomaterial for attaining improved permeation via attaching thiol groups and cholic acid moieties. For this purpose, a CA-CS-TGA graft was prepared, and modification was confirmed via FTIR analysis. The prepared CA-CS-TGA graft was used to coat the azathioprine-loaded nanoliposomes (ENLs), with subsequent characterization in terms of zeta size, zeta potential, and SEM analysis. Pharmaceutical evaluation was carried out in terms of drug release studies, and ex vivo permeation and in vivo oral bioavailability were studied. The particle size and zeta potential of CA-CS-TGA coated nanoliposomal formulation CA-CS-TGA-NLs were found to be 245 ± 15.6 and +22.4 ± 0.58, respectively, compared to that of nonenveloped nanoliposomal formulation 165.7 ± 12.3 and -21.8 ± 0.14, respectively, indicating successful coating. CA-CS-TGA-NLs indicated 64% of drug release in 24 h at pH 7.4. Ex vivo permeation enhancement and relative oral bioavailability studies indicated a 2.84-fold enhanced permeation and 6-fold enhanced oral bioavailability of CA-CS-TGA-NLs compared to Azathioprine suspension. Based on the results, it can be concluded that grafting the CA-CS-TGA polymer onto nanoliposomes seems to be a promising strategy to enhance the oral bioavailability of Azathioprine.

Light-activatable minimally invasive ethyl cellulose ethanol ablation: Biodistribution and potential applications.

While surgical resection is a mainstay of cancer treatment, many tumors are unresectable due to stage, location, or comorbidities. Ablative therapies, which cause local destruction of tumors, are effective alternatives to surgical excision in several settings. Ethanol ablation is one such ablative treatment modality in which ethanol is directly injected into tumor nodules. Ethanol, however, tends to leak out of the tumor and into adjacent tissue structures, and its biodistribution is difficult to monitor in vivo. To address these challenges, this study presents a cutting-edge technology known as Light-Activatable Sustained-Exposure Ethanol Injection Technology (LASEIT). LASEIT comprises a three-part formulation: (1) ethanol, (2) benzoporphyrin derivative, which enables fluorescence-based tracking of drug distribution and the potential application of photodynamic therapy, and (3) ethyl cellulose, which forms a gel upon injection into tissue to facilitate drug retention. In vitro drug release studies showed that ethyl cellulose slowed the rate of release in LASEIT by 7×. Injections in liver tissues demonstrated a 6× improvement in volume distribution when using LASEIT compared to controls. In vivo experiments in a mouse pancreatic cancer xenograft model showed LASEIT exhibited significantly stronger average radiant efficiency than controls and persisted in tumors for up to 7 days compared to controls, which only persisted for less than 24 h. In summary, this study introduced LASEIT as a novel technology that enabled real-time fluorescence monitoring of drug distribution both ex vivo and in vivo. Further research exploring the efficacy of LASEIT is strongly warranted.

Graphene oxide-loaded rapamycin coating on airway stents inhibits stent-related granulation tissue hyperplasia.

Our objective was to explore the safety and efficacy of a graphene oxide-loaded rapamycin-coated self-expandable metallic airway stent (GO@RAPA-SEMS) in a rabbit model. The dip coating method was used to develop a GO@RAPA-SEMS and a poly(lactic-co-glycolic)-acid loaded rapamycin-coated self-expandable metallic airway stent (PLGA@RAPA-SEMS). The surface structure was evaluated using a scanning electronic microscope. The in vitro drug-release profiles of the 2 stents were explored and compared. In the animal study, a total of 45 rabbits were randomly divided into 3 groups and underwent 3 kinds of stent placements. Computed tomography was performed to evaluate the degree of stenosis at 1, 2 and 3 months after the stent operation. Five rabbits in each group were sacrificed after the computed tomography scan. The stented trachea and blood were collected for further pathological analysis and laboratory testing. The in vitro drug-release study revealed that GO@RAPA-SEMS exhibited a sudden release on the first day and maintained a certain release rate on the 14th day. The PLGA@RAPA-SEMS exhibited a longer sustained release time. All 45 rabbits underwent successful stent placement. Pathological results indicated that the granulation tissue thickness in the GO@RAPA-SEMS group was less than that in the PLGA@RAPA-SEMS group. The TUNEL and hypoxia-inducible factor-1α staining results support the fact that the granulation inhibition effect in the GO@RAPA-SEMS group was greater than that in the PLGA@RAPA-SEMS group. GO@RAPA-SEMS effectively inhibited stent-related granulation tissue hyperplasia.

Formulation and characterization of antibiotic drug loaded aquasome for the topical application.

Aim: This study aimed to develop a topical antibiotic drug delivery system using aquasomes for enhanced treatment of skin and soft tissue infections (SSTIs). Materials & methods: Cephalothin was loaded into aquasomes using a multi-step process and optimized using design of experiment. The aquasomes were characterized for FT-IR, SEM and zeta potential analysis. Entrapment efficacy, In vitro drug release studies, antibacterial assays and stability study was performed to evaluate the efficacy of the formulated aquasomes. Results & conclusion: The formulated cephalothin-loaded aquasomes exhibited stable properties, controlled drug release and significant antibacterial activity against bacteria. This proves that the developed aquasome-based delivery system has the potential for sustained treatment of SSTIs.

An investigation of quantum dot theranostic probes for prostate and leukemia cancer cells using a CdZnSeS QD-based nanoformulation

Anticancer theranostic nanocarriers have the potential to enhance the efficacy of pharmaceutical evaluation of drugs. Semiconductor nanocrystals, also known as quantum dots (QDs), are particularly promising components of drug carrier systems due to their small sizes and robust photoluminescence properties. Herein, bright CdZnSeS quantum dots were synthesized in a single step via the hot injection method. The particles have a quasi-core/shell structure as evident from the high quantum yield (85 %), which decreased to 41 % after water solubilization. These water solubilized QDs were encapsulated into gallic acid / alginate (GA-Alg) matrices to fabricate imaging QDs@mod-PAA/GA-Alg particles with enhanced stability in aqueous media. Cell viability assessments demonstrated that these nanocarriers exhibited viability ranging from 63 % to 83 % across all tested cell lines. Furthermore, the QDs@mod-PAA/GA-Alg particles were loaded with betulinic acid (BA) and ceranib-2 (C2) for in vitro drug release studies against HL-60 leukemia and PC-3 prostate cancer cells. The BA loaded QDs@mod-PAA/GA-Alg had a half-maximal inhibitory concentration (IC50) of 8.76 μg/mL against HL-60 leukemia cells, which is 3-fold lower than that of free BA (IC50 = 26.55 μg/mL). Similar enhancements were observed with nanocarriers loaded with C2 and simultaneously with both BA and C2. Additionally, BA:C2 loaded QDs@mod-PAA/GA-Alg nanocarriers displayed a similar enhancement (IC50 = 3.37 μg/mL compared against IC50 = 11.68 μg/mL for free BA:C2). The C2 loaded QDs@mod-PAA/GA-Alg nanocarriers had an IC50 = 2.24 μg/mL against HL-60 cells. C2 and BA loaded QDs@mod-PAA/GA-Alg NCr had IC50 values of 7.37 μg/mL and 24.55 μg/mL against PC-3 cells, respectively.

Quality-by-Design-Driven Nanostructured Lipid Scaffold of Apixaban: Optimization, Characterization, and Pharmacokinetic Evaluation.

Apixaban, an anticoagulant, is limited in its efficacy due to poor solubility, low bioavailability, and extensive metabolism. This study investigates the application of nanostructured lipid carriers (NLCs) to enhance the bioavailability of Apixaban. NLCs were prepared using the high-pressure homogenization method. The influence of independent variables, viz., the amount of Tween 80, HPH pressure, and the number of HPH cycles, were studied using a 23 factorial design. The average particle size, PDI, zeta potential, and entrapment efficiency of the optimized NLCs were found to be 232 ± 23 nm, with 0.514 ± 0.13 PDI and zeta potential of about -21.9 ± 2.1 mV, respectively. Additionally, concerning the thermal and crystallographic properties of the drug, the NLCs showed drug entrapment without altering its potency. The in-vitro drug release studies revealed an immediate release pattern, followed by sustained release for up to 48 h. In-vivo pharmacokinetic experiments demonstrated that Apixaban-loaded NLCs exhibited higher values of t1/2 (27.76 ± 1.18 h), AUC0-∞ (19,568.7 ± 1067.6 ng·h/mL), and Cmax (585.3 ± 87.6 ng/mL) compared to free drugs, indicating improved bioavailability. Moreover, a decrease in the elimination rate constant (Kel) reflected the sustained effect of Apixaban with NLCs. NLCs offer improved oral absorption rates and enhanced therapeutic impact compared to free drugs, potentially reducing dose frequency and improving patient outcomes.

Preparation and Evaluation of Ranitidine Hydrochloride Floating Microspheres

&amp;lt;i&amp;gt;Introduction&amp;lt;/i&amp;gt;: Ranitidine hydrochloride, a member of the H2-receptor antagonist class, is widely employed in treating gastrointestinal conditions like ulcers, gastroesophageal reflux disease (GERD) and Zollinger-Ellison syndrome by reducing gastric acid production. Microspheres, designed for extended drug delivery and enhanced bioavailability, were formulated and evaluated in this study. &amp;lt;i&amp;gt;Aim&amp;lt;/i&amp;gt;: To develop ranitidine hydrochloride microspheres capable of prolonging drug delivery and improving bioavailability. Methods: The inotropic gelation method was utilized to prepare alginate microspheres incorporating polymers such as ethyl cellulose, sodium carboxymethyl cellulose, HPMC, and carbopol®. The resulting drug-loaded microspheres exhibited spherical rigidity after cross-linking with a 10% w/v calcium chloride solution. Evaluation parameters including Fourier transform infra-red (FTIR) analysis, precompression characteristics, percentage yield, swelling index, and drug content were determined. &amp;lt;i&amp;gt;Results&amp;lt;/i&amp;gt;: The FTIR results obtained, showed there was no incompatibility among the excipients and the active pharmaceutical ingredient. The Scanning electron microscopy (SEM) obtained, indicated the presence of spherical particles present in the formulation. The pre-compression evaluation showed that the angle of repose ranged from 4.85 ± 0.02 to 7.22 ± 0.06o for batched F4 and F1 respectively, while the Carr’s index ranged from 73.5 ± 2.47% to 87.00 ± 3.53% for batches F-7 and F-1 respectively. The percentage yield ranged from 73.5 ± 2.47% to 87.00 ± 3.53% for batches F-7 and F-1 respectively. &amp;lt;i&amp;gt;In vitro&amp;lt;/i&amp;gt; drug release studies revealed sustained drug release over 4 hours, with a maximum release of 69.50 ± 1.77% observed for batch F-1. &amp;lt;i&amp;gt;Conclusion&amp;lt;/i&amp;gt;: Overall, the formulated ranitidine hydrochloride microspheres demonstrated prolonged and controlled release characteristics, indicating their potential for use in controlled drug delivery applications.

Ketoconazole Nanocrystals Fortified Gel for Improved Transdermal Applications

Ketoconazole (KTZ) is a commonly prescribed antifungal drug used to treat several tropical and systemic fungus infections. The topical bioavailability of KTZ is limited due to extremely low water solubility and high molecular weight. The present investigation aimed to develop a ketoconazole nanocrystals formulation to improve the biomimetic attributes. The ketoconazole nanocrystals were prepared using a top-down media milling technique with a size of less than 800 nm and a narrow polydispersity index (PDI) of 0.434. The simplex lattice design was used to further investigate the effect of change in the proportion of different stabilizers on critical product attributes such as particle size and PDI. The result of the in vitro drug release and anti-fungal study proved the superiority of the optimized KTZ nanocrystal in inhibiting fungal infection and suspension of pure drug. The optimized nanocrystals entrapped within Carbopol-934P gel had higher permeability through cellulose membrane compared, to the marketed product (2 % ketoconazole % w/w Ketodoc Cream®) with sustained release for 24 h. Moreover, the release profile indicated diffusion-controlled release from gel following Korsmeyer-Peppas. The present investigation successfully demonstrated the application of simplex lattice design and desirability function in optimizing ketoconazole nanocrystals to improve its transdermal application.

A carboxymethyl-resistant starch/polyacrylic acid semi-IPN hydrogel with excellent adhesive and antibacterial properties for peri-implantitis prevention

Hydrogels possess inherent characteristics that render them promising for the prevention of peri-implantitis. Nonetheless, hydrogels with singular network structures are incapable of concurrently achieving the desired adhesion and mechanical properties. In this work, a carboxymethyl resistant starch/polyacrylic acid semi-interpenetrating (CMRS/PAA semi-IPN) hydrogel was successfully prepared in one step. Its morphology, structure, mechanical properties, and adhesion properties were systematically assessed, which revealed a homogeneously porous structure with a commendable mechanical strength of 67.317 kPa and an adhesion strength of 63 kPa. Ciprofloxacin (Cip) was loaded in the CMRS/PAA hydrogel via in situ compounding. The in vitro kinetic study of drug release shows that the slow drug release efficiency exceeds 90 % in the weakly acidic microenvironment at the infection site after 72 h, indicating enhanced antimicrobial properties. The Cip-loaded hydrogel also exhibits a remarkable bacterial inhibition rate exceeding 99 % against the pathogenic bacterium P. gingivalis and good cytocompatibility and hemocompatibility in vitro. In summary, the current work explored a novel solution and direction for the development of anti-infective medical materials applicable to dental implants.

Formulation, Optimization and Evaluation of Dabigartan Etexilate Encapsulated Solid Supersaturated Self-Nanoemulsifying Drug Delivery System

Objective: The present study proposed Dabigatran Etexilate loaded solid supersaturat-ed self-nanoemulsifying drug delivery system (solid S-SNEDDS) for enhancement of payload, drug solubility, dissolution rate as well as minimization of drug precipitation. Methods: The study involved formulation optimization using the Box-Behnken design. The op-timal SNEDDS consisting of Caprylic acid (32.9% w/w), Cremophor EL (50.2% w/w) and Transcutol HP (18.8% w/w) as Oil, Surfactant and Co-surfactant, respectively were formulated and evaluated for particle size, PDI, Zeta potential and saturation solubility. The SNEDDS was further incorporated with PPIs for the preparation of supersaturated SNEDDS (S-SNEDDS) to in-crease the drug payload in the formulation. S-SNEDDS was converted to solid S-SNEDDS by ad-sorption onto the porous carrier i.e., Aerosil®200. The in-vitro drug release study was also con-ducted for solid S-SNEDDS. Results: SNEDDS had size, PDI, and Zeta potential of 82 nm, 0.347, -10.50 mV, respectively. SNEDDS enhanced the saturation solubility of the drug by 93.65-fold. Among PPIs, HPMC K4M showed the most effective response for the formulation of S-SNEDDS. The S-SNEDDS had a more substantial drug payload, which further increased the solubility by 150 times of pure drugs and 16 times of SNEDDS. Solid S-SNEDDS exhibited free-flowing properties. Reconstituted sol-id S-SNEDDS had acceptable size, PDI, and Zeta potential of 131.3 nm, 0.457, and -11.3 mV, respectively. In-vitro drug release study revealed higher drug dissolution and minimized drug pre-cipitation by SNEDDS compared to marketed products and pure drugs. Conclusion: Proposed nano-formulation was found to efficiently improve the aqueous solubility of the drug and avoid the drug precipitation, thereby avoiding drug loss and improving drug bioa-vailability.

Formulation and Evaluation of Nanosuspension of Mebendazole for Solubility Enhancement by High Pressure Homogenization Technique

Background: Developing and evaluating a drug taken by mouth delivery method with mebendazole nanosuspension to treat intestinal worms infestations are the main objectives of the current research effort. This is because drug particles in the nano range help to reduce particle size and enhance dissolution. Methods: By using High pressure homogenization method, the mebendazole is converted into nanosuspension. Various amounts of HPMC K4M used as a stabilizer and Tween 80 and Poloxamer 188 used as a surfactant and compare its ratios. The results were investigated using effectiveness of drug entrapment, saturation solubility, zeta potential, particle size, drug release study and stability testing. Result: The drug purification results are shown by knowing the FT-IR spectrum. With a good entrapment efficiency and saturated solubility, optimized batches are found and the use of transmission electron microscopy confirms the nano size particle formed. The mebendazole nanosuspension showed higher release in the target site within 12 hours, according to an in-vitro dissolution experiment. Using the oral route for administration of the mebendazole nanosuspension, it increases the drugs absorption along with complete drug releasing. Conclusion: The study indicates that the prepared mebendazole nanosuspension has increased the rate of dissolution and solubility by converting nano range particles and encouraging the use of BCS class Ⅱ drugs with acceptable stability.

Microemulsion-Based Polymer Gels with Ketoprofen and Menthol: Physicochemical Properties and Drug Release Studies.

Ketoprofen is a non-steroidal, anti-inflammatory drug frequently incorporated in topical dosage forms which are an interesting alternatives for oral formulations. However, due to the physiological barrier function of skin, topical formulations may require some approaches to improve drug permeation across the skin. In this study, ketoprofen-loaded microemulsion-based gels with the addition of menthol, commonly known for absorption-enhancing activity in dermal products, were investigated. The main objective of this study was to analyze the physicochemical properties of the obtained gels in terms of topical application and to investigate the correlation between the gel composition and its mechanical properties and the drug release process. Microemulsion composition was selected with the use of a pseudoternary plot and the selected systems were tested for electrical conductivity, viscosity, pH, and particle diameter. The polymer gels obtained with Carbopol® EZ-3 were subjected to rheological and textural studies, as well as the drug release experiment. The obtained results indicate that the presence of ketoprofen slightly decreased yield stress values. A stronger effect was exerted by menthol presence, even though it was independent of menthol concentration. A similar tendency was seen for hardness and adhesiveness, as tested in texture profile analysis. Sample cohesiveness and the drug release rate were independent of the gel composition.

Influence of the Acceptor Fluid on the Bupivacaine Release from the Prospective Intra-Articular Methylcellulose Hydrogel.

Injections are one way of delivering drugs directly to the joint capsule. Employing this possibility, local anesthetic, such as bupivacaine (Bu), in the form of the suspension can be administered. The aim of this work was to propose a methylcellulose-based hydrogel-incorporated bupivacaine for intra-articular injections and to study the release kinetics of the drug from the hydrogel to different acceptor media, reflecting the synovial fluid of a healthy joint and the synovial fluid of an inflamed joint. The drug release studies were performed employing the flow apparatus. The drug was released to four different acceptor fluids: phosphate buffer pH = 7.4 (PBS7.4), phosphate buffer pH = 6.8 (PBS6.8), phosphate buffer pH = 7.4 with the high-molecular-weight sodium hyaluronate (PBS7.4H), and phosphate buffer pH = 6.8 with the low-molecular-weight sodium hyaluronate (PBS6.8L). The investigation was carried out at the temperature of 37 °C. The absorbance of the Bu released was measured at the wavelength of 262 nm every 2 min for 24 h. The release profiles of Bu to the acceptor media PBS7.4, PBS6.8, PBS7.4H, and PBS6.8L were described best by the first-order kinetics and the second-order equation. According to these models, the release rate constants were the highest when Bu was released to the fluid PBS7.4 and were k1 = (7.20 ± 0.01) × 10-5 min-1 and k2 = (3.00 ± 0.04) × 10-6 mg-1 × min-1, respectively. The relative viscosity of the acceptor medium, its pH, and the addition of high-molecular-weight or low-molecular-weight sodium hyaluronate (HAH or HAL) to the acceptor fluid influenced the drug dissolution. The release of Bu into the medium reflecting healthy synovial fluid takes a different pattern from its release into the fluid of an inflamed joint.

Green synthesis of chitosan gum acacia based biodegradable polymeric nanoparticles to enhance curcumin’s antioxidant property: an in vivo zebrafish (Danio rerio) study

Green-synthesis of biodegradable polymeric curcumin-nanoparticles using affordable biodegradable polymers to enhance curcumin’s solubility and anti-oxidative potential. The curcumin-nanoparticle was prepared based on the ionic-interaction method without using any chemical surfactants, and the particle-size, zeta-potential, surface-morphology, entrapmentefficiency, and in-vitro drug release study were used to optimise the formulation. The antioxidant activity was investigated using H2DCFDA staining in the zebrafish (Danio rerio) model. The mean-diameter of blank nanoparticles was 178.2 nm (±4.69), and that of curcuminnanoparticles was about 227.7 nm (±10.4), with a PDI value of 0.312 (±0.023) and 0.360 (±0.02). The encapsulation-efficacy was found to be 34% (±1.8), with significantly reduced oxidative-stress and toxicity (∼5 times) in the zebrafish model compared to standard curcumin. The results suggested that the current way of encapsulating curcumin using affordable, biodegradable, natural polymers could be a better approach to enhancing curcumin’s water solubility and bioactivity, which could further be translated into potential therapeutics.

Tyrosol-gold nanoparticle functionalized acacia gum-PVA nanofibers for mitigation of Candida biofilm

Increasing incidences of fungal infections and prevailing antifungal resistance in healthcare settings has given rise to an antifungal crisis on a global scale. The members of the genus Candida, owing to their ability to acquire sessile growth, are primarily associated with superficial to invasive fungal infections, including the implant-associated infections. The present study introduces a novel approach to combat the sessile/biofilm growth of Candida by fabricating nanofibers using a nanoencapsulation approach. This technique involves the synthesis of tyrosol (TYS) functionalized chitosan gold nanocomposite, which is then encapsulated into PVA/AG polymeric matrix using electrospinning. The FESEM, FTIR analysis of prepared TYS-AuNP@PVA/AG NF suggested the successful encapsulation of TYS into the nanofibers. Further, the sustained and long-term stability of TYS in the medium was confirmed by drug release and storage stability studies. The prepared nanomats can absorb the fluid, as evidenced by the swelling index of the nanofibers. The growth and biofilm inhibition, as well as the disintegration studies against Candida, showed 60–70 % biofilm disintegration when 10 mg of TYS-AuNP@PVA/AG NF was used, hence confirming its biological effectiveness. Subsequently, the nanofibers considerably reduced the hydrophobicity index and ergosterol content of the treated cells. Considering the challenges associated with the inhibition/disruption of fungal biofilm, the fabricated nanofibers prove their effectiveness against Candida biofilm. Therefore, nanocomposite-loaded nanofibers have emerged as potential materials that can control fungal colonization and could also promote healing.