Drug Release Test Research Articles

Investigation of Tannic Acid Crosslinked PVA/PEI-Based Hydrogels as Potential Wound Dressings with Self-Healing and High Antibacterial Properties

This study developed hydrogels containing different ratios of TA using polyvinyl alcohol (PVA) and polyethyleneimine (PEI) polymers crosslinked with tannic acid (TA) for the treatment of burn wounds. Various tests, such as scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), swelling, moisture retention, contact angle, tensile strength, the scratch test, antibacterial activity and the in vitro drug-release test, were applied to characterize the developed hydrogels. Additionally, the hydrogels were examined for cytotoxic properties and cell viability with the WST-1 test. TA improved both the self-healing properties of the hydrogels and showed antibacterial activity, while the added gentamicin (GEN) further increased the antibacterial activities of the hydrogels. The hydrogels exhibited good hydrophilic properties and high swelling capacity, moisture retention, and excellent antibacterial activity, especially to S. aureus. In addition, the swelling and drug-release kinetics of hydrogels were investigated, and while swelling of hydrogels obeyed the pseudo-second-order modeling, the drug release occurred in a diffusion-controlled manner according to the Higuchi and Korsmeyer–Peppas models. These results show that PVA/PEI-based hydrogels have promising potential for wound dressings with increased mechanical strength, swelling, moisture retention, self-healing, and antibacterial properties.

Co-biopolymer of zein/starch hydrogel incorporated montmorillonite for efficient quercetin delivery in lung cancer treatment

Today, cancer treatment is an important issue in the medical world due to the challenges and side effects of ongoing treatment procedures. Targeted nanodrug delivery systems can replace current methods to mitigate such side effects. In this study, a novel nanocomposite of starch, zein, and MMT with the drug quercetin (QC) was synthesised with the aim of effectively killing A549 cancer cells despite reducing any harmful effects on normal cells, and then the effect of the nanosystem to evaluate the damages on L929 cell lines (healthy) and A549 (cancerous) were investigated. For this purpose, the drug release test from the nanosystem was conducted at two pH levels of 5.4 and 7.4, and it was observed that the nanosystem successfully released 29 % of the QC drug in the first 12 h. The prepared nanocomposites were analysed by XRD, FT-IR, FESEM, DLS, Zeta potential, and MTT techniques. It was found that the nanoparticles exhibited a consistent and even morphology, with an average particle size ranging from 50 to 100 nm. The DLS study provided evidence of the precise range of size and outstanding durability of the nanoparticles. The nanosystem exhibited a notable enhancement in the rate of cell death in malignant tumours, as evidenced by the MTT tests. The synthesised nanosystem showed a precise and pH-dependent release of the drug, which indicates the biocompatibility of the nanocarrier for the QC drug. According to this, it has the capacity to function as an acceptable substitute for the therapeutic techniques that are now being used.

Effect of Fluid Paraffin on the Formulation Properties of Pressure Sensitive Adhesive Formulations Containing Diclofenac Sodium.

Understanding the relationship between the release characteristics of the active ingredient in the tape formulation and the pharmaceutical characteristics of the adhesive layer can optimize therapeutic efficacy and improve patient adherence. This study aimed to clarify the effect of liquid paraffine (LP)/styrene-isoprene-styrene (SIS) triblock copolymer ratio on pressure-sensitive adhesive (PSA) formulation properties, such as adhesive properties and drug release, with a certain amount of diclofenac sodium (DFS) and tackifier. The effects of changes in PSA composition in DFS-containing tape formulations on adhesive and drug release properties were evaluated. The viscoelasticity results showed rigid gel-like behavior at low angular frequencies regardless of the LP/SIS ratio, and deformable gel-like behavior at high angular frequencies, with a maximum plasticizing effect of LP up to an LP/SIS ratio of 3.7. The peel adhesion test results showed that peel adhesion was not affected, but indicated a decreasing trend by increasing the LP/SIS ratio in the presence of DFS. Drug release test results showed that DFS release increased up to 24h for LP/SIS ratios of up to 3.7, but decreased when the LP/SIS ratio was 6. The results of the drug permeation tests were similar to those of the drug release tests. In conclusion, it is possible to change the drug release properties by changing the amount of LP in the tape formulation; however, no definitive correlation was found between the adhesive and drug release properties.

Modeling Kinetics and Transport Mechanism Study of Poorly Soluble Drug Formulation in High Acidic Medium

Some medicinal particles are poorly soluble in highly acidic solutions, particularly those subjected to various production processes. Therefore, the present research investigated the kinetics and mechanisms of the drug release rate of newly formulated solid pills in a low pH medium. Three pills were prepared: one from a non-moisturized powder mixture (PILD) and the other two, PILC and PILM, from the dried powder mixtures, which were dried using hot-air heating and microwave radiation, respectively. These pills were subjected to drug release tests, and the outcomes were considered in the kinetics investigation using various models. Zero-order, Hixson–Crowell, First-order, Higuchi, Hopfenberg, Korsmeyer-Peppas, Logistic, and Peppas-Sahlin were the kinetic models used to inspect the release rate mechanism of these tablets. It was found that the Peppas-Sahlin and zero-order were the most reliable models to represent the drug release profile of all prepared pills with very high accuracy, estimated by R^2>0.99. The Hixon and first-order models were the weakest to characterize this work outcome. This work also applied these models to describe the controlling mechanism of the drug release for each prepared pill. It is detected that the non-Fickian diffusion and polymer chain relaxation control the PILC’s release behavior. However, case II transport and super case II transport with erosions is the dominant mechanism for PILD and PILM pills, respectively. Additionally, new semi-empirical models were modified to describe the kinetics of the solid release of those tablets with greater accuracy.

Formulation development, characterization, and evaluation of sorafenib-loaded PLGA-chitosan nanoparticles.

The basic purpose of this work was to develop environmentally friendly, biodegradable, and biocompatible polymeric nanoparticles of sorafenib that can effectively release the desired drug in a customized and controlled manner for targeting hepatocellular carcinoma. The solvent evaporation technique was employed for the synthesis of sorafenib-loaded PLGA-chitosan nanoparticles, followed by various experimental specifications and compatibility studies using poloxamer 407 as the stabilizer. The best nanoparticles thus synthesized were selected to be used for cytotoxicity investigations through in vitro and in vivo assessments. For the in vitro drug release tests, the dialysis bag diffusion technique was used. For both chitosan nanoparticles and PLGA loaded with sorafenib, a biphasic release pattern was found, exhibiting a protracted release lasting 10 days after a 24-h burst release. As experimental animals, rabbits were utilized to evaluate different in vivo pharmacokinetic properties of the selected formulations. Plasma samples were extracted with acetonitrile and analyzed through the developed HPLC method. Pharmacokinetic parameters such as AUC0-t, Cmax MRT, Vd, and half-life (t1/2) were enhanced significantly (p ≤ 0.001), while clearance was considerably decreased (p ≤ 0.001) for the chosen synthesized nanoparticles in contrast to the commercially accessible sorafenib formulation (Nexavar®). The cytotoxicity of the reference drug and sorafenib-loaded PLGA and chitosan nanoparticles was calculated by performing an MTT assay against HepG2 cell lines. The developed polymeric sorafenib nanoformulations possess the appropriate physicochemical properties, better targeting, surface morphology, and prolonged release kinetics. The pharmacokinetic parameters were improved significantly when the results were compared with commercially available sorafenib formulations.

An injectable self-lubricating supramolecular polymer hydrogel loaded with platelet lysate to boost osteoarthritis treatment

Globally, osteoarthritis (OA) is the most prevalent joint disease and is characterized by infiltration of M1 macrophages in the synovium, anabolic–catabolic imbalance of the extracellular matrix (ECM), increased articular shear force and overproduction of reactive oxygen species (ROS). Disease-modifying OA drugs are not yet available, and treatments for OA focus solely on reducing pain and inflammation and have limited therapeutic effect. Herein, we developed an injectable self-lubricating poly(N-acryloyl alaninamide) (PNAAA) hydrogel loaded with platelet lysate (PL) (termed “PNAAA@PL”) for treating OA. Tribological and drug release tests revealed suitable lubrication properties and sustained release of bioactive factors in PNAAA@PL. In vitro experiments showed that PNAAA@PL alleviated interleukin-1β (IL-1β)-induced anabolic–catabolic imbalance of chondrocytes and repolarized pro-inflammatory M1 macrophages to the anti-inflammatory M2 phenotype via intracellular ROS scavenging. Additionally, the PNAAA@PL hydrogel enhanced the migratory capacity and chemotaxis ability of stem cells, which are essential for chondrogenesis. In vivo, the functionalized PNAAA@PL hydrogel acted like synovial fluid following intra-articular injection into a rat OA model with anterior cruciate ligament transection, ultimately attenuating cartilage degeneration and synovitis. According to molecular mechanism studies, PNAAA@PL repairs cartilage in the OA model by inhibiting the NF-ĸB pathway. Overall, this self-lubricating PNAAA@PL hydrogel offers a comprehensive strategy for preventing OA progression by engineering a biophysiochemical microenvironment to generate high-quality hyaline cartilage.

Profile of a Composite Based on Bacterial Cellulose and Polyvinyl Alcohol as a Drug Release Matrix for Tetracycline Hydrochloride

Bacterial cellulose (BC) is a natural polymer with good mechanical properties and hydrophilicity. Polyvinyl alcohol (PVA) is a synthetic polymer widely used in medicine. Both have been researched for their potential in drug release and acceptance. This study aims to determine the role of BC and PVA as drug release matrices for tetracycline hydrochloride (TCH), with additional fillers such as graphite (G) and TiO2. The results showed that the composites with BC matrix had lower mechanical properties than those with PVA matrix, with tensile strength values of 6.4075 and 17.446 MPa, respectively. However, the BC matrix was superior in porosity and swelling ability. The drug release testing of TCH from the composites showed that the appropriate model to describe drug release in BC matrix composites was in zero order, while the PVA matrix was in first order. The antibacterial activity of the composites on both matrices was tested against Staphylococcus aureus. The results indicate that both composites have potential applications in promising biomedical fields.

Design, Development and Characterization of Nisoldipine Solid Lipid Nanoparticles: Statistical and Characterization Perspectives.

The objective of this study was to develop and characterize solid lipid nanoparticles (SLNs) loaded with Nisoldipine (NIS), aiming to enhance the drug’s bioavailability and provide a sustained release profile. SLNs were prepared using a solvent evaporation method and evaluated for several critical parameters. The superfluity test assessed the homogeneity of the SLN suspension, while particle size, drug entrapment efficiency, shapes, and surface morphology were analyzed using SEM/DLS/ TEM. Researchers studied the process of how drugs are released and performed in-vitro drug release tests to establish the substance’s release profile. HPLC and FT-IR were used to verify the drug’s chemical stability and encapsulation effectiveness. Stability studies assessed the formulation’s stability over time throughout different storage settings. The SLNs exhibited a high degree of homogeneity in the superfluity test, with no phase separation. The drug entrapment effectiveness was over 80%, and the typical particle size was 150-250 nm. Microscopy and transmission electron microscopy revealed that the SLNs had a flat, spherical top. NIS exhibited a regulated sequence of kinematics and prolonged release during dissolution investigations. FTIR and HPLC confirmed the stability and integrity of the drug within the SLNs. Stability studies indicated that the formulation remained stable over time. NIS-loaded SLNs show significant potential as an effective drug delivery system, offering enhanced bioavailability, sustained release, and excellent stability.

Preparation and InVitro Evaluation of Protective Effects of Quercetin-Loaded Solid Lipid Nanoparticles on Human Hair Against UV-B Radiation.

The aim of this study was to investigate the protective effect of quercetin loaded on solid lipid nanoparticles (SLN) in protecting human hair from ultraviolet-B (UV-B) light invitro. In this study, solvent-emulsified diffusion method was used to fabricate nanoparticle formulations and then particle size, loading, and drug release tests were performed from different formulations. Variables include oily part proportion, liquid to solid oil part ratio, and surfactant to lipid ratio. The optimal formulation was prepared by examining the eight formulations and optimizing them. Six groups of hair with different treatments were exposed to UV light for 600 h and the changes were investigated by examining four factors: RMS (root mean square average, the microscopic profile peaks and valleys), peak to valley roughness, the amount of chemical changes by Fourier transform infrared spectroscopy (FTIR), and the amount of protein loss. The selected formulation had a suitable particle size, loading percent, and release rate for penetration to hair. Quercetin-loaded SLN controlled RMS factor, peak to valley roughness, and reduced chemical changes and protein loss compared to other treatments. The optimize formulation showed positive effects in protecting the hair strands from UV-B radiation.

Novel dissolution methods for drug release testing of Long-Acting injectables

Long-acting parenteral drug products are a popular choice for therapeutic areas requiring long term treatment. These products range from dispersed systems such as drug suspensions and polymeric microspheres to in situ forming polymeric implants. The lack of reliable drug release testing methods for these drug products not only impedes the development of new drug products but also affects generic drug development. Current release methods suffer from a range of problems such as high variability, poor reproducibility, poor discriminatory ability, lack of depot-like structure formation (that could mimic the in vivo situation). Moreover, shorter duration (less than a week) of release renders them unsuitable for in vitro-in vivo correlations (IVIVCs). To overcome these issues, novel adapters were developed for both USP-type-II & IV apparatus. These adapters were validated and assessed using the long-acting injectable (LAI) suspension drug product Depo Provera 150® as well as its Q1/Q2 equivalents. For USP-type-IV apparatus, two open adapter designs (conical and ellipsoidal shaped cavity with volume capacities of 50 µl and 1 ml, respectively) were developed. A closed conical adapter design with a volume capacity of 0.05 ml was developed for USP apparatus type-II. All three novel adapter designs effectively retained the suspensions, achieved release durations of 3–6 weeks with good reproducibility, minimal variability (RSD≤5%) and had good discriminatory ability. Based on this, the adapter-based dissolution methods were deemed suitable for IVIVC development of long-acting injectables. A successful Level A IVIVC was developed for Depo SubQ Provera 104® and its Q1Q2 equivalents using USP apparatus type IV with a conical adapter design. The closed adapter design for apparatus type-II was also investigated for suitability with risperidone in situ forming implants. The adapter was able to securely retain and maintain the shape of the in situ forming implants and resulted in release profiles of up to one month with good discriminatory ability and low standard error (RSD≤5%). These novel adapters hold promise of wide use for in vitro release testing of different long-acting parenteral drug products.

Electrospraying as a Means of Loading Itraconazole into Mesoporous Silica for Enhanced Dissolution.

Mesoporous silica particles (MSPs) have been investigated as potential carriers to increase the apparent solubility and dissolution rate of poorly water-soluble drugs by physically stabilising the amorphous nature of the loaded drug. In preparing such systems, it is recognized that the loading method has a critical impact on the physical state and performance of the drug. To date, there has been very limited investigation into the use of electrospraying for loading drugs into mesoporous silica. In this study, we further explore the use of this approach, in particular as a means of producing amorphous and high drug-loaded MSPs; the study includes an investigation of the effect of drug loading and MSP concentration on the formulation performance and process. A comparison with rotary evaporation, a more widely utilised loading technique, was conducted to assess the relative effectiveness of electrospraying. The physical state of the drug in the formulations was assessed using powder X-ray diffraction (PXRD) and differential scanning calorimetry (DSC). The drug release profiles were determined by a comparative in vitro drug release test. Electrospraying successfully produced formulations containing amorphous drug even at a high drug loading. In contrast, while itraconazole was present in amorphous form at the lower drug-loaded formulations produced by rotary evaporation, the drug was in the crystalline state at the higher loadings. The percentage of drug released was enhanced up to ten times compared to that of pure itraconazole for all the formulations apart from the highest loaded (crystalline) formulation prepared by rotary evaporation. Supersaturation for at least six hours was maintained by the formulations loaded with up to 30 mg/mL itraconazole produced by electrospraying. Overall, the results of this study demonstrate that electrospraying is capable of producing amorphous drug-loaded MSPs at high loadings, with associated favourable release characteristics. A comparison with the standard rotary evaporation approach indicates that electrospraying may be more effective for the production of higher loadings of amorphous material.

Formulation and investigation of differently charged β-cyclodextrin-based meloxicam potassium containing nasal powders

Nasal systemic drug delivery may provide an easy way to substitute parenteral or oral dosing, however, the excipients have an important role in nasal formulations to increase the permeability of the mucosa and prolong the residence time of the drug. In this work, we aimed to produce meloxicam potassium monohydrate (MXP) containing nasal powders by a nano spray drier with the use of a neutral, an anionic and a cationic β-cyclodextrin as permeation enhancers, and (polyvinyl)alcohol (PVA) as a water soluble polymer. The following examinations were performed in order to study the effect of the applied excipients on the nasal applicability of the formulations: laser scattering, scanning electron microscope measurement, XRPD, DSC and FTIR measurements, adhesivity, in vitro drug release and permeability tests through an artificial membrane and RPMI 2650 cells. Based on our results, spherical particles were prepared with a size of 1.89–2.21 µm in which MXP was present in an amorphous state. Secondary interactions were formed between the excipients and the drug. The charged cyclodextrin-based formulations showed significantly higher adhesive force values regardless of the presence of PVA. The drug release was fast and complete. The passive diffusion of MXP was influenced not only by the charge of the cyclodextrin, but the presence of PVA, too. The permeation of the drug was enhanced in the presence of the anionic cyclodextrin testing it on RPMI 2650 cell model.

Measuring Erosion of Biodegradable Polymers in Brimonidine Drug Delivery Implants by Quantitative Proton NMR Spectroscopy (q-HNMR)

Erosion of biodegradable polymeric excipients, such as polylactic acid (PLA) and polylactic-co-glycolic acid (PLGA), is generally characterized by microbalance for the remaining mass of PLA and/or PLGA and Gel Permeation Chromatography (GPC) for molecular weight (MW) decrease. For polymer erosion studies of intravitreal sustained release brimonidine implants, however, both microbalance and GPC present several challenges. Mass loss measurement by microbalance does not have specificity for excipient polymers and drug substances. Accuracy of the remaining mass by weighing could also be low due to sample mass loss through retrieval-drying steps, especially at later drug release (DR) time points. When measuring the decrease of polymer MW by GPC, trace amounts of polymeric degradants (oligomers and/or monomers) trapped inside the implants during DR tests may not be measurable due to sensitivity limitations of the GPC detector and column MW range. Previous efforts to measure remained PLGA weight of dexamethasone micro-implants using qNMR with external calibration have been performed, however, these measurements do not account for chemical structure changes (i.e. LA to GA ratio changes from time zero) of PLGA implants during drug release tests. Here, a qNMR method with an internal standard was developed to monitor the following changes in micro-implants during drug release tests: 1. The remaining overall PLA/PLGA mass. 2. The remaining lactic acid (LA), glycolic acid (GA) unit and PLGA's lauryl ester end group percentages. 3. The trace content of PLA/PLGA oligomers as degradants retained in the implants. Unlike microbalance analysis, qNMR has both specificity for drug substance, excipient polymer, and accuracy due to minimal implant loss during sample preparation. Compared to the overall PLA/PLGA remaining mass generally monitored in erosion studies, the percentage of remaining LA, GA, and the ester end group provide more information about the microstructure change (such as hydrophobicity) of PLA/PLGA. Additionally, the qNMR method can complement GPC methods by measuring the change of remaining PLA and PLGA oligomer concentrations in brimonidine implants, with tenfold less sample and no MW cutoff. The qNMR method can be used as a sensitive tool for both polymer excipient characterization and kinetics studies of brimonidine implant erosion.

Formulation and Evaluation of Nicotinamide Microsponges – The First Step Towards the Development of a Novel Topical Dosage Form

The objective of this work was to formulate and analyze microsponges of nicotinamide. The said formulation was created using the emulsion solvent diffusion technique, and a 3 level two factor-based factorial design was applied to optimize the effect of the stabilizer (X1), as well as drug (X2), amounts on the entrapment efficiency (Y1) and average particle size (Y2). Various parameters, such as flow characteristics, percentage yield, drug concentration, in-vitro drug release tests, entrapment efficiency, and scanning electron microscopy (SEM), were evaluated. All parameters were found to be within the acceptable range. Design Expert 13 was employed to optimize the microsponges, and the optimal batch was determined by examining the desirability data. From this analysis, the optimal amounts of drug and stabilizer were found to be 302.87 and 59.71 mg, respectively. The reliability of the preparation and evaluation of the optimized batch was confirmed by a less than 5% discrepancy between the observed and predicted values of parameters. SEM images revealed that the microsponges were prepared with uniform and spherical morphology. The study concluded that nicotinamide microsponges were successfully prepared and evaluated. Further steps will involve incorporating this formulation into a novel topical dosage form.

Mechanical Properties, Drug Release, Biocompatibility, and Antibacterial Activities of Modified Emulsified Gelatin Microsphere Loaded with Gentamicin Composite Calcium Phosphate Bone Cement In Vitro.

Bone defects are commonly addressed with bone graft substitutes; however, surgical procedures, particularly for open and complex fractures, may pose a risk of infection. As such, a course of antibiotics combined with a drug carrier is often administered to mitigate potential exacerbations. This study involved the preparation and modification of emulsified (Em) crosslinking-gelatin (gel) microspheres (m-Em) to reduce their toxicity. The antibiotic gentamicin was impregnated into gel microspheres (m-EmG), which were incorporated into calcium phosphate bone cement (CPC). The study investigated the effects of m-EmG@CPC on antibacterial activity, mechanical properties, biocompatibility, and proliferation and mineralization of mouse progenitor osteoblasts (D1 cells). The average size of the gel microspheres ranged from 22.5 to 16.1 μm, with no significant difference between the groups (p > 0.05). Most of the oil content within the microspheres was transferred through modification, resulting in reduced cytotoxicity. Furthermore, antibiotic-impregnated m-EmG did not compromise the intrinsic properties of the microspheres and exhibited remarkably antibacterial effects. After combining with CPC (m-EmG@CPC), the microspheres did not significantly hinder the CPC reaction and produced the main product, hydroxyapatite (HA). However, the compressive strength of the largest microsphere content of 0.5 wt.% m-EmG in CPC decreased significantly from 59.8 MPa of CPC alone to 38.7 MPa of 0.5m-EmG@CPC (p < 0.05). The 0.5m-EmG@CPC composite was effective against Staphylococcus aureus (S. aureus) and Escherichia coli (E. coli) in drug release and antibacterial tests. Compared with m-EmG alone, the 0.5m-EmG@CPC composite showed no toxicity to mouse fibroblast cells (L929). Additionally, the proliferation and mineralization of mouse osteoblastic osteoprogenitor cells (D1 cells) did not have a negative impact on the 0.5m-EmG@CPC composite over time in culture compared with CPC alone. Results suggest that the newly developed antibacterial 0.5m-EmG@CPC composite bone cement did not negatively affect the performance of osteoprogenitor cells and could be a new option for bone graft replacement in surgeries.

Cellulose Acetate and Polycaprolactone Fibre Coatings on Medical-Grade Metal Substrates for Controlled Drug Release.

This study explores a method that has the potential to be cost effective in inhibiting biofilm formation on metallic prostheses, thereby preventing rejection or the requirement for replacement. A cost-effective metal alloy used in biomedical implants was chosen as the substrate, and ibuprofen (Ibu), a well-known anti-inflammatory drug, was selected for drug release tests for its widespread availability and accessibility. Multilayer coatings consisting of cellulose acetate (CA), polycaprolactone (PCL), and chitosan (CHI), with or without ibuprofen (Ibu) content, were applied onto medical-grade stainless steel (SS-316 type) through electrospinning, electrospray, or blow spinning. The adhesion of the CA, PCL, and layered CA/PCL membranes, with thicknesses ranging from 20 to 100 μm, to SS substrates varied between 0.15 N and 0.22 N without CHI, which increased to 0.21 and 0.74 N, respectively, when a CHI interlayer was introduced by electrospraying between the SS and the coatings. Although drug release in a simulated body fluid (SBF) medium is predominantly governed by diffusion-driven mechanisms in all single- and multilayer coatings, a delayed release was noted in CA coatings containing Ibu when overlaid with a PCL coating produced by blow spinning. This suggests avenues for further investigations into combinations of multilayer coatings, both with and without drug-imbued layers.

Injective hydrogel loaded with liposomes-encapsulated MY-1 promotes wound healing and increases tensile strength by accelerating fibroblast migration via the PI3K/AKT-Rac1 signaling pathway

Failed skin wound healing, through delayed wound healing or wound dehiscence, is a global public health issue that imposes significant burdens on individuals and society. Although the application of growth factor is an effective method to improve the pace and quality of wound healing, the clinically approved factors are limited. Parathyroid hormone (PTH) demonstrates promising results in wound healing by promoting collagen deposition and cell migration, but its application is limited by potentially inhibitory effects when administered continuously and locally. Through partially replacing and repeating the amino acid domains of PTH(1–34), we previously designed a novel PTH analog, PTH(3–34)(29–34) or MY-1, and found that it avoided the inhibitory effects of PTH while retaining its positive functions. To evaluate its role in wound healing, MY-1 was encapsulated in liposomes and incorporated into the methacryloyl gelatin (GelMA) hydrogel, through which an injectable nanocomposite hydrogel (GelMA–MY@Lipo, or GML) was developed. In vitro studies revealed that the GML had similar properties in terms of the appearance, microstructure, functional groups, swelling, and degradation capacities as the GelMA hydrogel. In vitro drug release testing showed a relatively more sustainable release of MY-1, which was still detectable in vivo 9 days post-application. When the GML was topically applied to the wound areas of rat models, wound closure as well as tensile strength were improved. Further studies showed that the effects of GML on wound repair and tensile strength were closely related to the promotion of fibroblast migration to the wound area through the controlled release of MY-1. Mechanically, MY-1 enhanced fibroblast migration by activating PI3K/AKT signaling and its downstream molecule, Rac1, by which it increased fibroblast aggregation in the early stage and resulting in denser collagen deposition at a later time. Overall, these findings demonstrated that the nanocomposite hydrogel system promoted skin wound healing and increased tensile strength, thus offering new potential in the treatment of wound healing.

Drug Release Study of Polyvinyl Alcohol-Gelatin-Montmorillonite Bionanocomposite Hydrogel Drug Delivery Systems Loaded with Clindamycin

One of the challenges facing medical science is the proper formulation of drug delivery systems for the correct transfer of active pharmaceutical ingredients to the body. Polymer and nanocomposite hydrogels have been considered ideal options in the preparation of drug delivery systems due to their proper properties, such as hydrophilicity and biocompatibility. In this, our research, described in this manuscript, the drug release from polyvinyl alcohol (PVA)-gelatin-montmorillonite (MMT) bionanocomposite hydrogel drug delivery systems loaded with clindamycin was studied. The structural and physical properties of prepared nanocomposite hydrogels were investigated using X-ray diffractometry (XRD), field emission scanning electron microscopy (FESEM), Fourier-transform infrared spectroscopy (FTIR), Brunauer-Emmette-Teller (BET) analysis, gel fraction and swelling tests. The results showed that by adding MMT clay to PVA-gelatin hydrogels, the amount of gel fraction increased, and due to the decrease in the size of the pores, the amount of swelling decreased. The results of the drug release tests showed that the release rate of clindamycin was inversely related to the percentage of MMT added to the nanocomposite hydrogel. The results also showed that the shape of the drug delivery system and its dimensions affected the release rate of clindamycin. The dominant mechanism of drug release in all samples was found to be Fickian transport. Considering the favorable in-vitro drug release performance of our PVA-gelatin-MMT nanocomposite hydrogels in the release of clindamycin, it was concluded that they are suitable options for preparing practical drug delivery systems with controlled drug release ability.

Caracterização de nanopartículas de ferrita de cobalto e avaliação de seu efeito tóxico em camundongos experimentais

This study investigated the characterization of cobalt ferrite nanoparticles (CoFe2O4) prepared by the pulsed laser deposition (PLD) method, using various techniques such as energy-dispersive X-ray spectroscopy (EDX), X-ray diffraction (XRD), scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), and in vitro drug release test (IVRT). It also evaluated the toxicity of these nanoparticles on liver, spleen, heart, and kidney tissues using a mouse model. CoFe2O4 nanoparticles were synthesized from an aqueous solution containing 1mg of CoFe2O4 powder dissolved in DMSO and RPMI serum-free media. XRD analysis revealed the characteristic peaks of the spinel lattice of cubic-shaped cobalt ferrite nanocrystals, with an average crystallite size of 12 nm calculated using Scherrer’s formula. SEM and EDX were used to study the surface morphology and chemical compositions, respectively. The in vivo experiments determined the LD50 of CoFe2O4 to be 3000 mg/kg body weight. Administration of CoFe2O4 nanoparticles at a dosage of 75 mg/kg body weight for 14 days did not cause any changes to the histological structure of the tissues in the mouse model, indicating their potential biocompatibility.

Thermo-activated in situ rectal gel preparation for Ibuprofen using eutectic mixture.

This study aimed to develop a thermosensitive in situ gel formulation for rectal delivery of Ibuprofen as an efficient alternative dosage form. Utilizing poloxamer 188, poloxamer 407, and HPMC via cold technique method, a thermosensitive in situ gel was successfully prepared. The concentration of Ibuprofen in the formulations was 1.2 % (w/w). The prepared gels underwent assessment for clarity, gelation temperature, gelation time, gel strength, spread ability, syringe-ability, pH, viscosity, FTIR, and drug content. The selected formulations exhibited a gelation temperature within the range of 30 °C to 36 °C, with consistent amount of drug soluble in the formulations (93 % - 110 %). Mucoadhesive studies, in vitro release tests, ex vivo modeling of drug release, kinetic studies modeling, and histopathology testing were also conducted. The formulation comprising 18 % poloxamer 407, 12 % poloxamer 188, and 1 % sodium chloride (FS15) demonstrated suitable gelation temperature and desirable drug release rate. In vitro drug release tests indicated completion within one hour for both FS10 (20 % P407 & 10 % P188) and FS15 (18 % P407 & 12 % P188), with consistent and predictable release patterns observed through kinetic modeling analysis. Microscopic histopathology examination confirmed the safety of the selected formula, exhibiting no irritation in the mucosal membrane of the sheep. In conclusion, Ibuprofen thermosensitive in situ gel presents a promising and convenient strategy as a rectal carrier and an alternative dosage form to solid suppositories.