Percentage Drug Release Research Articles

FORMULATION OF VITEX NEGUNDO ETHOSOMAL LOADED TOPICAL HERBAL GEL AND ITS EVALUATION FOR ARTHRITIS TREATMENT

The current research aims to develop and test a system of vesicular drug carriers for topical drug administration of Vitex negundo Linn. to provide sustained drug delivery. The ethosomes of V. negundo Linn. were produced using thin-film hydration, and their in vitro drug release profiles, size, drug content, and other characteristics were examined. To attain the desired results, for drug release and entrapment effectiveness, the composition of lecithin and ethanol was changed to form ethosomes. The ethosomal size of the vesicle of the optimized formulation batch was measured to be the units 13.47 nm with -3.97 mV as zeta potential. The percent drug release of ethosomal gel was 83.24 %, and the percent entrapment efficiency was 89.40 %. The formation of spherically shaped vesicles was confirmed by optical and scanning electron microscopy observations. It was observed that as the ethanol concentration increased, the formulation’s in vitro profile for drug release increase, and lipid concentration decreases.

Development and evaluation of redox-responsive alginate–SS–ibuprofen derivative based anti-tumor target drug delivery system for the controlled release of doxorubicin

Nowadays, self-assembled polymeric micelles from amphiphilic polymer conjugates are urgently needed to enhance drug targeting and release efficiency. On account of the excellent properties of alginate and the redox-responsiveness of disulfide bonds, a redox-sensitive alginate–SS–ibuprofen derivative (LSA–SS–IBU) based anti-tumor target drug delivery system was created by attaching the hydrophobic ibuprofen (IBU) onto the hydrophilic alginate molecular skeleton through disulfide linkages for glutathione (GSH) triggered delivery of doxorubicin hydrochloride (DOX). The structure and self-assembly behavior of the synthesized LSA–SS–IBU was systematically evaluated by FT-IR spectrometer, 1H NMR spectrometer, fluorescence spectrophotometer (FM), transmission electron microscope (TEM) and dynamic light scattering (DLS). Furthermore, the in vitro release of drugs from the LSA–SS–IBU micelles loaded with DOX was examined, along with the assessment of their cytotoxicity to HeLa cells. The resultant LSA–SS–IBU had a critical micelle concentration (CMC) value of 0.19 mg/mL that was able to self-assemble into the spherical micelles with the particle size and zeta potential of 148.2 ± 4.3 nm (PDI = 0.25) and −47.2 ± 0.4 mV, respectively. At a mass ratio of 3:10 for DOX/LSA–SS–IBU, the LSA–SS–IBU micelles achieved drug loading ratio (DLR) and encapsulation efficiency (EE) values of 12.2 % and 46.3 %, respectively. Furthermore, the in vitro drug release study indicated that the total drug release percentage of the drug-encapsulated LSA–SS–IBU micelles in PBS with the presence of 10 mmol/L GSH for 12 h exceeded 67.0 %, demonstrating a substantial increase compared to that in GSH-free PBS. The in vitro cytotoxicity findings indicated that LSA–SS–IBU had good biocompatibility, while the IC50 value and the cell viability of DOX-loaded LSA–SS–IBU micelles cultured with HeLa cells for 48 h was 2.2 μg/mL and less than 20.1 %, respectively, which could significantly inhibit the growth of HeLa cells. Therefore, redox-responsive LSA–SS–IBU micelles had potential applications in cancer therapy for hydrophobic anti-tumor drug delivery.

DESIGN AND OPTIMIZATION OF NANO ENCAPSULATED BERBERIS ASIATICA BIO COMPOUNDS

Objective: The current study goal is to develop and optimize nanoencapsulated biocompounds of Berberis asiatica (BCBA) utilizing the ionic gelation process to target the kidney for antiurolithiatic activity. Methods: Nanoencapsulated BCBA was prepared employing the ionic gelation method. Box Behnken Design (BBD) 3-factor, 3-level is used to examine the effects of formulation parameters and to enhance the desired responses. Characterization studies include Fourier transform infrared (FTIR), X-ray diffraction (XRD), particle size, zeta potential, scanning electron microscopy (SEM), and transmission electron microscopy (TEM) performed to study the quality of optimized nanoparticles. Results: Mathematical equations and response surface plots were used to relate the dependent and independent variables. Diagnostic charts were used to show the varied factor level permutations. The percentages of entrapment efficiency (% EE) and drug release (% DR) used in evaluation studies of optimized biocompounds of Berberis asiatica nanoparticles (OBCBANPs) were determined to be 83.7% and 78.33%, respectively. The Fourier transform infrared (FTIR) results showed that chitosan, sodium tripolyphosphate (NaTPP), and BACB were compatible. Due to chitosan and NaTPP gelation in the case of OBCBANPs, X-ray diffraction (XRD) analyses have acknowledged the crystalinity. The particle size and zeta potential of the optimized formulation, found to be 95.4 nm and 31 mV, respectively, indicate the nanoparticles are in the nano range and possess extreme stability by preventing particle convergence. Scanning Electron Microscopy (SEM) and Transmission Electron Microscopy (TEM) studies reveal that the optimized formulation nanoparticles are spherical in shape, homogeneous, and have little aggregation. The accelerated stability studies showed that the optimized formulation was stable at different temperatures and relative humidity. Conclusion: The stable optimized formulation was prepared, evaluated, and characterized. BBD is employed to optimize the formulation by minimizing the number of experimental runs and enhancing the desired responses. The optimized formulation further needs to investigate the invivo studies for antiurolithiatic activity by targeting the kidney.

Aceclofenac loaded microspheres: Formulation and evaluation of novel preprogrammed drug delivery for the treatment of arthritis

Arthritis is a widespread joint disorder globally, the patient completely dependent on NSAIDs which are administered after a fixed interval to subside the pain. This work aims to establish a preprogrammed drug delivery system of aceclofenac with a predetermined lag time for the treatment of arthritis. This new preprogrammed formulation microsphere reduces the time-dependent dose administration as it steadily releases the drug in the blood circulation reducing side effects and increasing patient compliance. Aceclofenac (ACF) loaded polymer microspheres were prepared by a new emulsification and crosslinking method using glutaraldehyde as cross-linking agent. Microspheres were prepared in 6 batches using different polymers like sodium alginate, guar gum and chitosan, alone, as well as in combinations. The type and quantity of polymers were changed in every batch while the amount of aceclofenac was unvarying. The microspheres were then evaluated for the particle size, drug content, percentage yield, percentage entrapment efficiency and percentage drug release followed by noting the lag time. The microsphere loaded with aceclofenac were formulated and evaluated, the result showed that all the preparations showed a good lag time (2–3 ​h), but chitosan (alone) gave the highest lag time, which fulfills the aim of pre-programmed drug delivery system. Preprogrammed drug release has been achieved from the microspheres over a period of 0–7 ​h, consistent with the demand for chronotherapeutic drug delivery for the treatment of arthritis. The major signification of the preparation technique includes short processing time and the lack of exposure of the ingredients to high temperatures. Aceclofenac-loaded microspheres offer a promising avenue for arthritis treatment, ensuring sustained drug release. Their potential clinical implications include enhanced therapeutic efficacy, reduced side effects, and improved patient compliance. Future directions may involve personalized formulations, targeted delivery systems, and exploring applications beyond arthritis, expanding the scope of this innovative drug delivery approach.

Preparation and characterization of brain-targeted polymeric nanocarriers (Frankincense-PMBN-lactoferrin) and in-vivo evaluation on an Alzheimer's disease-like rat model induced by scopolamine

Experiments have demonstrated that frankincense may offer protection against scopolamine-induced Alzheimer's disease by mitigating cholinergic dysfunction and inhibiting inflammatory mediators. Nevertheless, its instability and limited water solubility lead to diminished medicinal efficacy. In this study, we utilized PMBN (poly [MPC-co-(BMA)–co-(MEONP)]) as a nanocarrier for targeted brain drug delivery of frankincense, employing lactoferrin as a ligand for precise targeting. Characterization of nanoparticle properties was conducted through FTIR and FESEM analysis, and the in-vitro drug release percentage from the nanoparticles was quantified. To induce Alzheimer's-like dementia in rats, scopolamine was intraperitoneally administered at a dose of 1 mg/kg/day for 14 days. Subsequently, behavioral assessments (Y-maze, passive avoidance test, tail suspension test) were performed, followed by evaluations of acetylcholinesterase (AChE), reduced glutathione (GSH), catalase (CAT), and brain histopathology at the conclusion of the treatment period.The results revealed that the nanoparticles had a size of 106.6 nm and a zeta potential of −3.8 mV. The maximum release of frankincense in the PBS environment from PMBN nanoparticles was 18.2 %, in accordance with the Peppas model. Behavioral tests indicated that targeted drug nanoparticles (F-PMBN-Lf) exhibited the capability to alleviate stress and depression while enhancing short-term memory in scopolamine-induced animals. Additionally, F-PMBN-Lf counteracted the scopolamine-induced elevation of AChE activity and GSH levels. However, it resulted in decreased activity of the antioxidant enzyme CAT compared to the scopolamine group. Histological analysis of brain tissue suggested that F-PMBN-Lf exerted a notable neuroprotective effect, preserving neuronal cells in contrast to the scopolamine-induced group. It appears that the polymer nanoparticles containing this plant extract have introduced a novel neuroprotective approach for the treatment of Alzheimer's disease.

Fabrication, design, and in vivo investigation of mesoporous silica-based docetaxel trihydrate nanoparticles for colonic drug delivery

BackgroundMesoporous silica-loaded docetaxel trihydrate nanoparticles are the potential to target drug delivery toward a specific region with high stability and predictable release at the target region. They have large surface areas and mesoporous structures with large pore volumes, leading to high bioavailability and therapeutic efficacy at the disease site. This study demonstrates how nanoparticles can be prepared using an emulsion technique.ResultsThe ratios of eudragit S100 to eudragit L100 polymers, along with phosphatidylcholine, were varied according to the response surface methodology. Differential scanning colorimetry and fluorinated transmitted infrared spectroscopy studies showed that mesoporous silica particles were successful. All formulations had average particle sizes ranging from 70.65 to 143.01 nm, with a range of zeta potential from 17.6 ± 026 to 21 ± 011. In vitro drug delivery studies were achieved for all formulations with a zeta potential of 17.6 ± 026 to 21 ± 011. As per the statistical optimization by RSM that response model for percentage drug loading (Y1) was found to be 0.0002 which is p-value < 0.05. Hence, the model is significance. Accordingly percentage drug release at 6 h. (Y2) p-value was found to be 0.0001 and percentage drug release at 10 h (Y3) p-value was found to be 0.0002, respectively. So all the models are significant. After oral administration of the docetaxel, plasma levels were measured in vivo bioavailability testing of docetaxel. Docetaxel nanosuspension had a significantly higher Cmax amount than docetaxel microsuspension (98.03 ± 23.40 ng/ml and 213.67 ± 72.21 ng/ml, respectively, with tmax 45 min). Docetaxel was more bioavailable in nanosuspension formulations, according to a bioavailability test of rats.ConclusionThe results suggested that the mesoporous silica could be a great potential nanocarrier in colonic delivery with optimal drug content and controlled release docetaxel trihydrate.

Formulation, Characterization, and Evaluation of β-Cyclodextrin Functionalized Hypericin Loaded Nanocarriers.

St. John's wort in western Europe has been extensively utilized for the treatment of mild to moderate depression. Hypericin, a red pigment, is found to be responsible for its antidepressant activity. The aim of the current study was to prepare a nanoemulsion (O/W) of hypericin designed for immediate delivery of the drug to the brain for the treatment of depression. The nanoemulsion was prepared by means of a homogenization technique, and that was followed by its physicochemical evaluation. Tween-80, Span-80, β-cyclodextrin, ethanol, and eucalyptus oil were utilized for the manufacturing of the nanoemulsion. Morphological studies have revealed globular structures of nanosize that were confirmed by the zeta analysis. The consistency of particles was revealed by the low polydispersity values. pH values of all formulations lay within the range of nasal pH. The viscosity of the prepared formulations was affected by the increase in concentrations of β-cyclodextrin. After passing from the centrifugation and freeze-thaw studies, the prepared formulations showed good stability. Formulation F2 having a composition of oil phase (0.125 mL), aqueous phase (1.25 mL), and β-cyclodextrin (8%) showed the best results out of all the formulations, and F2 had a pH of 5.7, 5.35 cP viscosity, 1.332 refractive index, 148.8 globule size, and -10.8 zeta potential. The mean percentage drug release and in vitro and ex vivo percentage drug permeations were observed to be 71.75, 76, and 75.07%, respectively. Meanwhile, formulation F2 showed the maximum drug release and permeation. In vivo behavior studies including the open field test, elevated plus maze test, and tail suspension test were conducted to see the antidepressant effect of hypericin along with comparison with a commercially available treatment. In conclusion, the prepared formulation shows good efficacy as an antidepressant and can be considered as a natural alternative over synthetic drugs.

In situ gastric floating gel of atazanavir sulphate for sustained release: formulation, optimization and evaluation.

Aim: Atazanavir sulphate belongs to BCS class II drug, its oral bioavailability is limited due to its rapid first-pass metabolism and P-gp efflux. Materials & methods: The insitu floating gel using the complexed drug was prepared by ion gelation method and optimized the formulation as per 32 full factorial design. Results: Floating lag time of optimized formulation was found to be 18sand percentage drug release of 94.18±0.18 % at the end of 16h. The concentration of gelling polymer affects drug release and a floating lag time and vice versa. Conclusion: Insitu floating gel of atazanavir sulphate was found promising to sustain drug release due to an increased gastric residence time, which leads to enhanced potential therapy.

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

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

Formulation and Evaluation of Cola acuminata Gum-based Mucoadhesive Sustained-release Matrix Tablets of Diclofenac Sodium.

This study aimed to evaluate Cola acuminata gum (CAG) for the formulation of mucoadhesive sustained-release matrix tablets of diclofenac sodium. Different batches of granules containing CAG and 100 mg of DS in ratios 0.5:1, 1:1, 2:1, and 3:1 were prepared, compressed into tablets, and evaluated for mucoadhesive strength, swelling index, and drug release in SGF (pH 1.2) and SIF (pH 7.4). Swelling indices and mucoadhesive strengths of the tablets were pH-dependent. Swelling indices of 56 ± 2.03 to 121 ± 2.19% and mucoadhesive strengths of 7.25 ± 1.45 to 15.43 ± 2.71 g/cm2 obtained at pH 7.4 were significantly higher (p<0.05) than swelling indices of 25 ± 2.43 to 47 ± 3.15% and mucoadhesive strengths of 5.52 ± 0.76 to 9.22 ± 1.95 g/cm2 obtained at pH 1.2. The percentage release of DS from the matrix tablets at pH 1.2 after 2 h (T2h) was insignificant. However, the percentage of drug release at pH 7.4 was significant for all the batches and dependent on the CAG concentration. The drug release was in the order of batches containing 3 g (80.44 ± 7.75) < 2 g (86.35 ± 5.65) < 1 g (90.08 ± 6.14) < 0.5 g (99.70 ± 3.90). The time for maximum drug release was 7 h (T7h) for CAG containing 0.5 g and 10 h (T10h) for other batches. This study showed that CAG could be useful for mucoadhesive sustained drug delivery.

In-vivo Estimation of Optimized Floating Microspheres Design by QBD approach

In order to regulate its release, avoid repeated dosing, and consequently maximize bioavailability, it is essential to develop and construct floating microspheres of glipizide. According to Strubel et al., HPMC and EC were combined to form glipizide-loaded floating microspheres using a solvent evaporation technique. Drug loading, particle size, and percent drug release were used as response factors in the formulation optimization process, which took into account polymer concentration and stirring rate as independent variables.The bulk density, tapped density, flowability, and particle size of the formulation batches were all evaluated. Its in-vitro performance was assessed using the standard pharmacopoeal assays as well as other procedures, including yield (%), drug polymer compatibility (FTIR scan), and tapped density (%). Analysis of compressibility particle size, drug entrapment effectiveness, surface topography (SEM), and an in vitro release research. with a yield of 88.30±0.53%, an ideal drug loading of 85.50±0.55%, and a preferred buoyancy of 91.93±0.61%, tiny to big and spherical microspheres were created at 40°C using a 1:6 polymer, 2% Tween 80, and that temperature. The development of a stable emulsion and equally sized internal phase droplets was largely dependent on the emulsifying agent. A crucial element in the emulsification process is the propeller's stirring speed. Additionally, it influences the droplets' size and shape, which has an impact on the microspheres. The decision was made to incorporate stirring rate and polymer concentration as independent variables in the experimental design while keeping the other variables fixed as a result of the debate that was just had. Measurements of the hypoglycemic response brought on by oral administration were used to determine the in vivo effectiveness of the optimized batch in healthy normal Wistar rats (250–300gm).

Antibody-conjugated pH-sensitive liposomes for HER-2 positive breast cancer: development, characterization, in vitro and in vivo assessment

The object of the current study was to develop and evaluate trastuzumab-conjugated Paclitaxel (PTX) and Elacridar (ELA)-loaded PEGylated pH-sensitive liposomes (TPPLs) for site-specific delivery of an anticancer drug. In this study, paclitaxel is used as an anticancer drug which promotes microtubules polymerization and arrest cell cycle progression at mitosis and subsequently leading to cell death. The single use of PTX causes multiple drug resistance (MDR) and results failure of the therapy. Hence, the combination of PTX and P-glycoprotein inhibitor (ELA) are used to achieve maximum therapeutic effects of PTX. Moreover, monoclonal antibody (trastuzumab) is used as ligand for the targeting the drug bearing carriers to BC. Thus, trastuzumab anchored pH-sensitive liposomes bearing PTX and ELA were developed using thin film hydration method and Box-Behnken Design (BBD) for optimizing various formulation variables. The optimized liposomes undergo characterization such as vesicle size, PDI, and zeta potential, which were observed to be 122 ± 2.14 nm, 0.224, and −15.5 mV for PEGylated pH-sensitive liposomes (PEG-Ls) and 134 ± 1.88 nm, 0.238, and −13.98 mV for TPPLs, respectively. The results of the in vitro drug release study of both formulations (PEG-Ls and TPPLs) showed enhanced percentage drug release at an acidic pH 5 as compared to drug release at a physiological pH 7.4. Further, the in vitro cytotoxicity studies were performed in the SK-BR-3 and MDA-MB-231 cell lines. The cellular uptake study of FITC-loaded TPPLs in SK-BR-3 cells showed greater uptake than FITC-loaded PEG-Ls, while in MDA-MB-231 cells there was no significant difference in cell uptake between FITC-loaded TPPLs and FITC-loaded PEG-Ls. Hence, it can be concluded that the HER-2 overexpressing cancer cell line (SK-BR-3) was showed better cytotoxicity and cell uptake of TPPLs than the cells that expressed low levels of HER2 (MDA-MB-231). The in vivo tumor regression study, TPPLs showed significantly more tumor burden reduction i.e. up ∼74% as compared to other liposomes after 28 days. Furthermore, the in vivo studies of TPPLs showed a minimal toxicity profile, minimal hemolysis, higher tumor tissue distribution, and superior antitumor efficacy as compared to other formulations. These studies confirmed that TPPLs are a safe and efficacious treatment for breast cancer.

QbD Design, Formulation, Optimization and Evaluation of Trans-Tympanic Reverse Gelatination Gel of Norfloxacin: Investigating Gene-Gene Interactions to Enhance Therapeutic Efficacy.

Traditional otic drug delivery methods lack controlled release capabilities, making reverse gelatination gels a promising alternative. Reverse gelatination gels are colloidal systems that transition from a sol to a gel phase at the target site, providing controlled drug release over an extended period. Thermosensitive norfloxacin reverse gelatination gels were developed using a Quality by Design (QbD)-based optimization approach. The formulations were evaluated for their in vitro release profile, rheological behavior, visual appearance, pH, gelling time, and sol-gel transition temperature. The results show that the gelation temperatures of the formulations ranged from 33 to 37 °C, with gelling durations between 35 and 90 s. The drug content in the formulations was uniform, with entrapment efficiency ranging from 55% to 95%. Among the formulations, F10 exhibited the most favorable properties and was selected for a stability study lasting 60 days. Ex-vivo release data demonstrate that the F10 formulation achieved 95.6percentage of drug release at 360 min. This study successfully developed thermosensitive norfloxacin reverse gelatination gels using a QbD-based optimization approach. The selected formulation, F10, exhibited desirable properties in terms of gelling temperature, drug content, and release profile. These gels hold potential for the controlled delivery of norfloxacin in the treatment of ear infections.

Enhancement of apixaban's solubility and dissolution rate by inclusion complex (β-cyclodextrin and hydroxypropyl β-cyclodextrin) and computational calculation of their inclusion complexes.

Apixaban (AP) is a factor X inhibitor, an orally active drug that inhibits blood coagulation for better prevention of venous thromboembolism. It has poor solubility, dissolution rate and low bioavailability. The aim of this study was to improve the aqueous solubility and dissolution rate of oral AP as a step to enhance its bioavailability by preparing it as an inclusion complex with beta- and hydroxy propyl beta-cyclodextrin. A simple, rapid method of analysis of AP was developed using ultraviolet spectrophotometry (UV) and partially validated in terms of linearity, precision and accuracy, recovery, and robustness. AP was prepared as a complex with beta cyclodextrin (βCD) and hydroxy propyl beta cyclodextrin (HPβCD) in weight ratios 1:1, 1:2, and 1:3 by kneading, solvent evaporation and spray drying methods and characterized by Fourier transfer infra-red (FTIR), differential scanning calorimetry (DSC), and percent drug content in each of the prepared complex. Using the computer simulation, the interactions of AP with βCD and HPβCD were investigated. The phase solubility study showed that the solubility of AP was greatly enhanced from 54×10-3 mmol /L to 66 mmol/L using HPβCD with acceptable stability constant. Computer docking supports the formation of a stable 1:1 complex between AP and CD's. The dissolution test results showed that the complex gave a significantly higher percentage of drug release (95%) over one hour compared to the free AP (60%) (p<0.05). AP- HPβCD complex in the ratio of 1:2 (w/w) can significantly improve the solubility and in vitro dissolution rate of AP.

Development and Evaluation of Buccal Mucoadhesive patches of Losartan Potassium

Buccal mucoadhesive patches of losartan potassium were formulated using hydroxypropyl methyl cellulose grades - K4M, K15M, K50M and Eudragit L100 polymers by the method of solvent casting. The prepared formulations were characterized for mechanical and physicochemical parameters like thickness, surface pH, uniformity of weight, swelling index, folding endurance, percentage moisture loss, drug content, in vitro dispersion and in vitro residence time. Further, in vitro drug release study was performed with the use of freshly prepared egg membrane as the semi-permeable membrane. The best formulation (F6) exhibited higher percentage of drug release 97.26%±0.41 at the end of 8 h. The sustained release of losartan potassium was found to be attained up to 8 h duration.

Functionalized mesoporous silica for drug delivery of poorly soluble polyphenols: Synthesis, characterization, and antimicrobial action

The synthesis of mesoporous silica nanoparticles (MSN) and their functionalization have gained significant attention in various biomedical fields. MSNs are nanoscale particles composed of silica with ordered pore structures and high surface areas, which make them excellent candidates for a wide range of applications, including drug delivery, imaging, biosensing, and tissue engineering. The focus of the present study is to explore the role of 12-tungstophosphoric acid (TPA) functionalized nMCM-48 for drug delivery of two weakly soluble polyphenols; curcumin, and quercetin, for effective antimicrobial action. Quercetin (Q) and curcumin (C) are simultaneously encapsulated in TPA-functionalized nMCM-48 to achieve C-TPA/nMCM-48 and Q-TPA/nMCM-48, nanocomposites respectively. The TPA functionalized nMCM-48 exhibited high pore volume, pore diameter and high surface area, the primary requirements for effective drug loading and release. The nanocomposite were characterized using several analytical methods, including FESEM, EDX, BET, XRD and FTIR. The FESEM analysis, demonstrating retainment of uniform spherical shape of the particles and homogeneous dispersion of drugs C or Q, in Q-TPA/nMCM-48 and C-TPA/nMCM-48. The EDX gives the confirmation of drug-loaded carriers, C-TPA/nMCM-48 and Q-TPA/nMCM-48 validates the presence of all elements indicating the successful loading of both C and Q. The high drug loading content 84% and 86% in the case of C and Q over C-TPA/nMCM-48 and Q-TPA/nMCM-48, respectively, was observed due to the high porosity of the material. In-vitro drug release studies for C-TPA/nMCM-48 and Q-TPA/nMCM-48 were carried out at physiological temperatures and different pH conditions. The percentage of drug release observed in case of C-TPA/nMCM-48 was 69% and for Q-TPA/nMCM-48 was 67%. The antimicrobial efficacy of nano systems was studied by bacterial growth curve analysis, zone of inhibition, MIC studies, and morphological analysis of cells. The nanocomposites exhibited enhanced antimicrobial efficiency due to the synergistic effect of a polyphenol drug molecule (C or Q) and TPA in nMCM-48 matrices. The bacterial growth curve was significantly affected and a prominent growth inhibition of microbes was observed in the presence of drug loaded samples C-TPA/nMCM-48, Q-TPA/nMCM-48. The antimicrobial efficiency of C-TPA/nMCM-48, Q-TPA/nMCM-48 was carried out against E.coli and the minimum inhibition concentration values were 25 μg/mL and 25 μg/mL, respectively. The zone of inhibition for C-TPA/nMCM-48 was detected as 1.5 ± 0.2 mm and for Q-TPA/nMCM-48 as 1.3 ± 0.3 mm against E.coli. The intricate interactions between drugs and TPA within nMCM-48 is a key facet that controls the properties of nanocomposite as a drug delivery system.

BOX-BEHNKEN DESIGN-BASED DEVELOPMENT AND CHARACTERIZATION OF POLYMERIC FREEZE-DRIED NANOPARTICLES OF ISRADIPINE FOR IMPROVED ORAL BIOAVAILABILITY

Objective: This study aimed to develop and optimize isradipine-loaded polymeric freeze-dried nanoparticles prepared by solvent shifting method with the help of the experiment design for improving oral drug bioavailability and minimizing dosing intervals. Methods: Isradipine is a potent anti-hypertensive drug that is matrixed in polymeric freeze-dried nanoparticles using solvent shifting. In this work, a 3-factor, 3-level box-Behnken design was used to optimize the process parameters like a drug: PLA concentration (A), poloxamer 407 concentration (B), and stirring speed (C). In addition, responses were measured as dependent variables such as percentage drug release, particle size (nm), Zeta potential (mV), and % entrapment efficiency. Results: Mathematical equations and response surface plots were used to relate the dependent and independent variables. The optimization model exhibited 97.36 % drug release, 153.14 nm particle size,-25.9 mV Zeta potential, and 78.25% entrapment efficiency, respectively. The observed responses were in close agreement with the predicted values of the optimized process. Fourier transform infrared spectroscopy, morphological studies, and in vitro drug release studies characterized the prepared polymeric nanoparticles. Conclusion: The improved freeze-dried polymeric nanoparticle samples exhibited an in vitro drug release rate of more than 90% at 24h. Based on in vivo pharmacokinetic parameters, the isradipine-loaded polymeric nanoparticles show better bioavailability than pure drug's suspension form.

Formulation and evaluation of extended-release tablets of trimetazidine HCL

The present study was undertaken with an aim to formulate develop and evaluate Trimetazidine HCL extended release matrix tablets using different polymers as release retarding agent. Pre formulation study was done initially and results directed for the further course of formulation. Based on Pre formulation studies different batches of Trimetazidine HCL were prepared using selected excipients. Powders were evaluated for tests Angle of repose, Bulk density, tapped density, compressibility index, and Hausner ratio before being punched as tablets. It was concluded that the tablets of batch F9 had considerable swelling behaviors and in vitro drug release. Percentage drug release in 8 hr is 80.77. It was observed that tablets of batch F9 followed the Huguchi release profiles. From the results and discussion it is concluded that formulation of Extended release matrix tablet of HCL containing HPMC K-15 (19.44%) and Hyper mellose (19.44%), Ethyl cellulose (19.44%) batch F9 can be taken as an ideal or optimized formulation Extended release matrix tablet for 8 hour release as it fulfills the requirements for extended release matrix tablet.

Design and In-vivo Evaluation of Quercetin Nanosponges-based Buccal Tablets of Quercetin

The objective was to increase the bioavailability of quercetin by creating a controlled release formulation using nanosponges based on cyclodextrin. Based on the early testing, a 3-factor, 3-level Box-Behnken design with quercetin was loaded into nanosponges using the freeze-drying process. The prepared nanosponges were examined after being described and made into tablets. The quercetin-loaded nanosponges have particle sizes ranging from 36.45 to 135.27 nm, encapsulation efficiencies ranging from 42.37 to 88.44%, and drug release percentages at 6 hours ranging from 53.04 to 82.64%. The FTIR, DSC, and XRD investigations validated the Quercetin interaction with nanosponges. The medicine released from the nanosponges buccal tablets in-vitro at a rate of 99.75%, and stability testing showed no significant changes within six months after the nanosponges were transformed into tablets. In-vivo studies in rats showed that quercetin optimised nanosponges tablets Cmax of 6.27 ± 0.06 ng/mL was significantly higher (p

Formulation and Evaluation of Floating Microspheres of an Antidiabetic drug

Abstract: The primary objective of this work was to create Metformin floating microspheres to achieve longer retention in the upper GIT, which improves absorption and bioavailability. The microspheres were created using a solvent evaporation process with various ratios of rate controlling polymers ethyl cellulose and Carbopol 940, with Metformin employed at a fixed ratio in each formulation. A (1:1) mixture of dichloromethane and ethanol, with tween 80 as a surfactant. The produced microspheres were tested for percentage yield, particle size, entrapment efficiency, buoyancy, and drug release in vitro. The influence of polymer concentration on various parameters was studied. According to the findings, increasing the concentration of ethyl cellulose improved drug release from floating microspheres. The formulation F6 was selected as best formulation, and it has drug release of 94.22% at 12 hrs. entrapment efficiency 98.8%, buoyancy 94.2%.