Drug Release Studies Research Articles

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

<i>Introduction</i>: 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. <i>Aim</i>: 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. <i>Results</i>: 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. <i>In vitro</i> drug release studies revealed sustained drug release over 4 hours, with a maximum release of 69.50 ± 1.77% observed for batch F-1. <i>Conclusion</i>: 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.

Formulation Development and Evaluation of Atorvastatin Calcium Extended-Release Tablets

Atorvastatin calcium is an antihyperlipidemic agent that acts as HMG- COA reductase inhibitor. The objectives of the current research are to evaluate Atorvastatin calcium release from sustained-release tablets. FTIR analysis reveals that drug and polymer have no interaction. The tablets were created utilizing the wet granulation process by using various concentrations of polymer like HPMC. The prepared extended-release tablets have been assessed for friability, thickness, drug content, hardness, and in-vitro drug release studies. From the release analysis at high concentrations demonstrate better release than HPMC low concentration. The in-vitro release data findings indicate that HPMC polymer exhibits a better release rate at 18 hours showing 97.63.

Formulation and Evaluation of Electrospun Nanofiber Mats of Curcumin and Leaf Extract of Tinospora cordifolia: Designed for Accelerating Diabetic Wound Healing

Traditional herbs like Tinospora cordifolia and curcumin have many therapeutic benefits. However, curcumin’s limited bioavailability is a problem. Electrospun nanofibers are an answer because they increase the effective surface area greatly, and make drug delivery better in almost all aspects. The combination in the form of nanofibers can be greatly useful in the treatment of diabetic wound healing, where curcumin, the known antibacterial and anti-inflammatory element, plays an important role. It is observed that when combined with extract of leaves of T. cordifolia, which has known antidiabetic and wound healing actions, blended in the chitosan polymer, which is itself a weak antibacterial compound hence can be one of the solutions to the menace of bacterial resistance which is very common in diabetic wound healing. This research aims to create and test electrospun nanofiber mats of curcumin and T. cordifolia leaves extract blended in chitosan as a base polymer in the treatment of diabetic wound healing. Leaves of the plant T. cordifolia, which were collected from the institute’s botanical garden, were subjected to drying and then prone to solvent extraction using methanol and acetone, resulting in the production of bioactive extracts. The curcumin was obtained as a gift sample from Sanjay Chemicals, Mumbai. Nanofibers were electrospun from chitosan, T. cordifolia leaf extract and curcumin. Characterization included scanning electron microscope (SEM), water contact angle measurement, TGA/DSC analysis, drug release studies, fourier-transform infrared (FTIR) analysis, swelling tests and in-vitro release profiling. The nanofiber mats of curcumin and leaves extract of T. cordifolia using chitosan as a base polymer were prepared and evaluated at various parameters. The results we found are very promising. The nanofibers formed by using electrospinning techniques show good content uniformity as well as good diameter which was checked using SEM. The study confirmed no component interactions using differential scanning calorimetry (DSC). The good hydrophilicity of mats was found to ensure good retention time. The study concluded with the formation of a novel formulation that can fight the menace of bacterial resistance, which is very common in the diabetic wound healing process. The formulation will ensure not only countering bacterial resistance but also the faster healing of diabetic wounds, as T. cordifolia leaves extract is known to improve angiogenesis and tissue remodeling.

The Development of an Innovative Ophthalmic In-situ Gel Containing Posaconazole

The goal of this study was to create and test various in-situ gel formulas for administering posaconazole to the eye to treat fungal keratitis. They used an in-situ gelling method to help posaconazole stay in the eye mucosa longer, which made it easier for the body to use. To make in-situ gel preparations, polymers such as sodium alginate, poloxamer 407, and poloxamer 188 were used in a cold method. Finally, there was 0.2% (w/w) posaconazole in the mixtures. The pH, drug content, viscosity, gelling capacity, and temperature at which the solution turns into a gel were all checked on the recipes. It was between 32 and 34℃ when each blend turned into a gel. There was about the same amount of drugs in all of them. It was also worked out how much of the antifungal and in-vitro drugs these mixtures would release. Everyone in the drug release study showed signs of long-lasting release. To sum up, in-situ gels that contain posaconazole could be a good way to use optical drug delivery to change how fungus diseases act.

Effect of Lyophilization on Characteristics of Iloperidone Nanosuspension

Objective: The primary objective of this study is to develop the nanosuspension formulation of iloperidone and to check the effect of lyophilization on different characteristics of iloperidone nanosuspension.Methods: Solvent-antisolvent method with probe ultrasonication was used for the formulation of nanosuspension. The nanosuspension was then converted into lyophilized form by using mannitol as a cryoprotectant and then evaluated for various parameters, including particle size, saturation solubility, scanning electron microscopy (SEM), thermal analysis, fourier-transform infrared (FTIR), in-vitro drug release study. Result: From the study it was observed the increase in concentration of cryoprotectant while lyophilization has increased the particle size of nanosuspension. As there was an increase in particle size after lyophilization, there was a decrease in saturation solubility. In-vitro drug release also indicates a slight decrease in drug release after lyophilization. Overall, lyophilization might be used in the improvement of stability of nanosuspension, parameters must be chosen carefully for the process of lyophilization in order to obtain nanosuspension with good characteristics.

Mucoadhesive aprepitant-loaded nanostructured lipid carriers containing sulfhydryl surfactant for enhanced oral drug bioavailability

The objective of the study was to design mucoadhesive drug-loaded nanostructured lipid carriers (NLCs) for enhancing the bioavailability of a model BCS Class IV drug aprepitant (APT). For this purpose, polyethoxylated surfactant (polyoxyethylene 20 oleyl ether) was thiolated, and mucoadhesive NLCs were designed through nano-template engineering technique using thiolated surfactant, Span 60 (lipophilic surfactant), labrasol (hydrophilic surfactants), miglyol (liquid lipid), stearic acid (solid lipids), and PEG 6000 as a stabilizer. Mucoadhesive NLCs were characterized via size, ζ (zeta potential), polydispersity index (PDI), and scanning electron microscopy (SEM). Moreover, NLCs were evaluated for drug loading capacity and entrapment efficiency, stability, safety, drug release, mucoadhesion, and permeation studies. Furthermore, in-vivo studies were conducted on Sprague-Dawley rats to prove enhanced oral bioavailability of APT. The APT-loaded NLCs revealed a particle size of 185 ± 12 nm, zeta potential of about −23.5 ± 3 mV, a PDI of 0.190 ± 0.01, having spherical shape, with 6.7 ± 0.8 % and 86 ± 3 % drug loading and entrapment efficiency, respectively. The APT-loaded NLCs were found stable at different conditions and demonstrated the sustained release of the drug. NLCs were found safe as more than 80 % cells were found viable after 24 h. Moreover, drug-loaded mucoadhesive NLCs showed 3.8-fold improved mucoadhesive properties as compared to control. Mucoadhesive NLCs were found less permeable due to disulfide bond formation with mucus. In-vivo studies confirmed that APT-loaded mucoadhesive NLCs exhibited 2.56-fold improved Cmax. Furthermore, 24.8 % relative bioavailability (Fr) was reached for APT-loaded mucoadhesive NLCs as compared to 9.8 % for APT suspension. On the basis of all the above-stated findings, it can be decided that these NLCs are suitable nanocarriers for delivering the aprepitant orally.