Dissolution Profiles Research Articles

Formulation, Optimization and Evaluation of Solid Dispersion of Deferasirox Using Factorial Design

Deferasirox, an oral iron-chelating agent, is a poorly soluble drug (Biopharmaceutical Classification System class II) having insufficient solubility in physiological fluids resulting in low bioavailability of the drug. The idea behind the present study was to explore the prospects of solid dispersion as a prolific method to enhance the dissolution rate of drug using a water soluble polymer. The solid dispersion was prepared by the solvent evaporation technique using Polyvinyl pyrrolidone with different drug to carrier and solvent ratio. Formulations were characterized through attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR), differential scanning calorimetry (DSC), Powder X-ray diffraction (XRD), and in vitro release studies. A 32 factorial design was implemented to obtain optimum solubility, % yield, and optimization of solid dispersion (SD) also quantitates the influence of PVP on the solubility and dissolution profile. Thedrug-to-carrier and solvent ratio was chosen as independent variable, while %yield, drug content, and saturation solubility were chosen as dependent variables. The results showed that the optimized formulation of SD-DFX was able to significantly enhance its solubility. The SD containing a dispersion of Deferasirox with PVP show an exceptional rise in the solubility. This study describes the development of solid dispersion that significantly improved the solubility and bioavailability of DFX. The FTIR studies indicate the interaction between the drug and polymer. The DSC and XRD analysis indicated that the drug was in an amorphous state when dispersed in the polymer. It is resolved that the SD method significantly improves the solubility and dissolution rate, which could also be exploit for other poorly water soluble drug candidates. Keywords: Deferasirox , Polyvinyl pyrrolidone, solid dispersion, Factorial design, Solubility

Release profile of encapsulated microparticles based on Landolphia owariensis (Apocynaceae) extract contained in suppositories for the treatment of hemorrhoidal crisis

Introduction: Hemorrhoidal disease is one of the most frequent causes of anal complaints. The general aim of this study was to evaluate the release profile of the encapsulated drug, in order to overcome the limitations of conventional galenic forms, while maintaining their efficacy. Methods: Determination of the active ingredient contained in Landolphia owariensis extract was carried out by UV-Visible spectrophotometry. Release studies were carried out in a continuous flow cell. The dissolution profile of the suppository containing microparticles was compared to the dissolution profile of suppositories containing the unencapsulated extract and to that of Landolphia owariensis extract-based microparticles. Results: The percentage of active ingredient released from suppositories containing microparticles and those containing the extract alone was 69.47% and 80.01% respectively. Flavonoid release from suppositories containing microparticles was slower, with a release rate of 6.31µg/mm, slightly close to the release rate of extract based microparticles (7.37µg/mn); in contrast, in vitro flavonoid release from suppositories containing the extract was faster (19.85µg/mm). Conclusion: Release trials have shown the influence of the sodium alginate matrix system on PA release kinetics. These innovative suppositories will help improve compliance and the treatment of hemorrhoidal crisis. Keywords: Microparticles, Suppositories, Landolphia owariensis, Hemorrhoids, In vitro release

Design and Evaluation of Gastro-Retentive Floating Tablets of Ibandronic acid

The objective of this study is Preparation and evaluation of gastro-retentive floating tablets of Ibandronic acid by direct compression method polymers or combination. In this study, Ibandronic acid, the most commonly used biphosphonate for treating osteoporosis, was formulated as gastro retentive dosage form (GRDF) tablets to enhance its oral bioavailability. GRDDs are an approach to prolong gastric residence time, there by targeting site-specific drug release in the upper GIT for local or systemic effect. GRDF tablets of Ibandronic acid (200 mg) were characterized with the effects of Carbopol 934P, HPMC 4KM and Na-CMC at various ratios on swelling, floating, physical integrity. A prolonged dissolution profile of Ibandronic acid GRDF tablets developed in this study was observed for its thickness, friability, hardness, drug content and in-vitro drug release. Formulated Floating tablets of Ibandronic acid gave satisfactory results for various physicochemical parameters like hardness, friability, thickness, weight variation and content uniformity. Sodium bicarbonate has predominant effect on the buoyancy lag time, while HPMC K4M has predominant effect on total floating time and drug release. From the study it is evident that a promising controlled release floating tablets of Ibandronic acid can be developed to increase gastric residence time and thereby increasing its bioavailability. Both doses significantly reduced the occurrence risk of new vertebral fractures by 50–52 percent when compared to the effects of the placebo drug. Keywords: Gastro retention, Ibandronic acid, floating tablet, Carbopol, GRDF, GRFT.

Formulation and Evaluation of Immediate-Release Oral Tablets Containing Magnesium Aluminum Silicate-Loaded Simvastatin

Background: Simvastatin (SIM) is a lipid-lowering agent to prevent disorders caused by clogged blood vessels. Because of its low solubility, it has low bioavailability. The adsorption technique is effective in improving drug solubility and dissolution rate. Objective: To use magnesium aluminum silicate (MAS) as an adsorbent in combination with Soluplus® as a hydrophilic polymer to formulate SIM as immediate-release tablets (IRTs). Methods: We used the solvent evaporation method to make MAS-loaded SIM in the presence of Soluplus®, making sure that the ratio of SIM to MAS to SOLU was 1:6:3. We then used this mixture to make IRTs. Using the direct compression method, we made all of the SIM-IRT formulas. We used diluents like Avicel®PH102, Avicel®PH101, and starch, as well as super disintegrants like Crospovidone (CP), Croscarmellose sodium (CCS), and sodium starch glycolate (SSG). We evaluated these formulas for their weight variation, hardness, friability, disintegration time, drug content, and dissolution profile. Results: We prepared the tablet formula (T5) using MAS-loaded SIM, Avicel®PH102 as a diluent, and CCS 3% as a super disintegrant. This formula showed the shortest disintegration time (0.61 min) and best drug release in phosphate buffer pH 7.0, releasing more than 80% of the drug within 30 minutes. Conclusion: Using suitable excipients, adsorption was an efficient method to enhance the solubility of SIM for preparation as IRTs.

PREDICTION OF SULFAMETHOXAZOLE AND TRIMETHOPRIM PLASMA LEVELS FROM TABLETS AND DISSOLUTION MEDIA OF PHYSIOLOGICAL RELEVANCE

Objective: To estimate plasma concentrations-time profiles of Sulfamethoxazole (SMZ) and Trimethoprim (TMP) from fixed-dose combination formulations through in vitro data of dissolution media of physiological relevance and a convolution model. Methods: Dissolution profiles of SMZ/TMP tablets (400/80 mg) were obtained with USP paddle apparatus at 100 rpm and 900 ml of 0.1 N HCl, pH 4.5 acetate buffer, and pH 6.8 phosphate buffer. The reference drug product and two generic formulations were tested. Drugs were quantified by a derivative method. Dissolution profiles were compared with model-dependent and independent methods. SMZ/TMP plasma levels were simulated with dissolution data and published in vivo information. Percent of prediction error (PE) for peak plasma concentration (Cmax) and area under the curve from zero time to infinity (AUC0-inf) at each condition were calculated. Results: In all used conditions, similar dissolution profiles were found excepting for TMP at pH 1.2 (f2<50). The in vitro release performance for reference and generic formulations was explained by the Weibull function only for SMZ at pH 6.8 and TMP at pH 4.5. Values of PE>19% for both generic formulations were found with TMP at pH 1.2. Conclusion: Significant differences in TMP dissolution profiles of generic formulations at pH 1.2 reflect the subsequent differences found in predicted Cmax and AUC0-inf.

Opportunities and Challenges: Process Raman for the Real-Time Release Testing (RTRT) of Extended-Release Formulations

The use of a process analytical technology has been demonstrated using near-infrared spectroscopy for continuous manufacturing of pharmaceutical formulations and is within the scope of the U.S. Food and Drug Administration's real-time release testing initiative. While effective for simple formulations, this preliminary study investigates whether such a spectroscopic surrogate application can replace pharmaceutical dissolution testing for extended-release formulations. In this study, we will assess the use of process Raman spectroscopy for real-time dissolution testing. Extended-release tablet formulations often accomplish the release rate delay through the addition of gelling agents. In this work, hydroxypropyl methylcellulose (HPMC) polymers were used to formulate extended-release niacin tablets. Process Raman spectroscopy was evaluated as a tool to effectively model dissolution profiles to determine if the optical technique has the ability to differentiate HPMC polymers from the background and be selective for the polymer type employed. Our preliminary work indicates that while Raman can effectively detect and monitor the niacin response of the tablet formulations, there are not enough unique spectral features between the different HPMC polymers to selectively resolve their responses. Additional measurements and chemometric analysis might suggest otherwise. Thus, for extended-release tablet applications with continuous manufacturing, further dissolution surrogate development is needed.

Effect of basket mesh size on the hydrodynamics of a partially filled (500 mL) USP rotating basket dissolution testing Apparatus 1

The USP Rotating Basket Dissolution Testing Apparatus 1 is listed in the USP as one of the tools to assess dissolution of oral solid dosage forms. Baskets of different mesh sizes can be used to differentiate between dissolution profiles of different formulations. Here, we used Particle Image Velocimetry (PIV) to study the hydrodynamics of the USP Apparatus 1 using baskets with different mesh openings (10-, 20- and 40-mesh) revolving at 100 rpm, when the vessel was filled with 500 mL. The velocity profiles throughout the liquid were found to vary significantly using baskets of different mesh sizes, typically increasing with increased size of the opening of the basket mesh, especially for axial and radial velocities. This, in turn, resulted in a significantly different flow rate through the basket, which can be expected to significantly impact the dissolution rate of the drug product. A comparison between the results of this work with those of a previous study with a 900-mL fill volume (Sirasitthichoke et al., Intern. J. Pharmaceutics, 2021, 607: 120976), shows that although the hydrodynamics in the USP Apparatus 1 changed with fill level in the vessel, the flow rate through the basket was not significantly affected. This implies that tablets dissolving in the two systems would experience similar tablet-liquid medium mass transfer coefficients, and therefore similar initial dissolution rates, but different dissolution profiles because of the difference in volume.

Development of Response Surface Approach for Determination of Paracetamol, Chlorpheniramine Maleate, Caffeine and Ascorbic Acid by Green HPLC Method: A Desirability-Based Optimization.

Design of experiment is an efficient and cost-effective tool to optimize the chromatographic separation of a multicomponent mixture. The central composite design was conducted to develop and optimize a green high performance liquid chromatography (HPLC) method for simultaneous quantitation of a quaternary mixture of paracetamol, chlorpheniramine maleate, caffeine and ascorbic acid in their pharmaceutical dosage form as well as the determination of their dissolution profile. A five-level three-factor model was performed to investigate the effect of mobile phase composition, pH and flow rate on enhanced resolution and short run time. Analysis was performed using a Kinitex EVO C18 column and a mobile phase composed of methanol: 0.02M phosphate buffer pH3.3 (34:66, v/v) at 1.0mL/min using photodiode array detection. Optimum chromatographic separation was achieved in <6min with a desirability of 0.999. Linearity was achieved over a range of 1.00-300.00, 1.00-50.00, 2.00-50.00 and 2.00-100.00μg/mL for paracetamol, chlorpheniramine maleate, caffeine and ascorbic acid, respectively, with a limit of detection (<0.1μg/mL). The greenness profile was evaluated using the analytical eco-scale and Analytical GREEnness Metric Approach with values of 81 and 0.77, respectively.

3D-printed immediate release solid dosage forms: a patent evaluation of US11622940B2.

Three-dimensional (3D) printing is one of the most flexible technologies for preparing tablets, offering controlled drug release profiles. The current patent describes the preparation of immediate-release 3D-printed tablets of hydrochlorothiazide to improve disintegration and dissolution profile. The patent involves the preparation of drug-loaded filament via hot-melt extrusion and utilizing the same filaments for printing 3D-printed tablets using fused deposition modeling. The tablets were printed with different shapes and sizes by incorporating channels within the tablet spaces, termed as gaplets. The introduction of channels within the tablet design improves the disintegration and dissolution profile of the drug significantly. The morphological characteristic of 3D-printed tablets was studied by using scanning electron microscopy and revealed the presence of gaplets in the tablets.

Development and In Vitro Evaluation of Aceclofenac Buccal Film.

This study aimed to formulate and characterize aceclofenac buccal film formulations made of different polymers and evaluate the effects of polymer type on buccal film properties. Five polymer types, namely hydroxypropyl methylcellulose (HPMC), sodium carboxymethylcellulose (SCMC), polyvinyl alcohol (PVA), Eudragit S100, and Eudragit SR100, were used to prepare aceclofenac buccal film formulation either separately or combined by solvent-casting method. These formulations were evaluated in terms of physical appearance, folding test, film weight and thickness, drug content, percentage of elongation, moisture uptake, water vapor permeability, and in vitro drug release. The addition of Eudragit polymer in most of the produced buccal films was unacceptable with low folding endurance. However, the dissolution profile of buccal films made from PVA and Eudragit SR100 provided a controlled drug release profile. Buccal films can be formulated using different polymers either individually or in combination to obtain the drug release profile required to achieve a desired treatment goal. Furthermore, the property of the buccal films depends on the type and concentration of the polymer used.

FORMULATION AND EVALUATION OF FILM COATED TABLETS CONTAINING ACECLOFENAC AND PARACETAMOL

FORMULATION AND EVALUATION OF FILM COATED TABLETS CONTAINING ACECLOFENAC AND PARACETAMOL

Comparison of diterpenoid contents and dissolution profiles of selected Andrographis paniculata crude and extract capsules.

Andrographis paniculata (AP) has been approved by the Thai government for the treatment of mild cases of COVID-19 patients. Increasing use of AP products requires quality control to ensure efficacy and safety. At present, there is no requirement for dissolution test of AP products in the Thai Herbal Pharmacopoeia (THP). This work aimed to examine the contents and dissolution profiles of active diterpenoids, andrographolide (AP1), 14-deoxy-11,12-didehydroandrographolide (AP3), neoandrographolide (AP4), and 14-deoxyandrographolide (AP6) in AP capsules available in Thai markets. Four extract products (EXT. A-D) and three crude powder products (CRD. A-C) were tested for contents by using HPLC-DAD. Dissolution profiles of four diterpenoids were investigated in different media (pH 1.2, 4.5, 6.8, and 0.01 N HCl + SLS) with apparatus II (paddle type). The AP1 contents were 1.99%-2.90% w/w for crude capsules and 2.84%-16.27% w/w for extract capsules. In the dissolution test, the dissolution percentages of four diterpenoids from crude capsules were higher than those from extract capsules except EXT. A. AP1 in most extract products (EXT. B, C, D) was dissolved in all dissolution media at a lower percentage than the other three diterpenoids. EXT. A (aqueous extract) was the only extract capsule showing the amounts of all diterpenoids dissolved in all media >80% in 45 min. The study demonstrated that AP1 content in AP products complied with the acceptance criteria in the THP (80%-120%), and the weight variation also met the United States Pharmacopeia (USP) requirements. However, different dissolution profiles of AP products may lead to different bioavailability of diterpenoids and further affect their efficacy.

Apixaban and clopidogrel in a fixed-dose combination: Formulation and in vitro evaluation

Fixed-dose combination (FDC) products represent a novel, safe, and cost-effective formulation. Combined use of anticoagulant and antiplatelet medications is common among comorbid cardiovascular patients. This study aimed to formulate FDC tablets for Apixaban and Clopidogrel, as prophylaxis and treatment of thrombo-embolic events. FDC tablets were developed by combining small tablets of Immediate-Release Clopidogrel 75 mg and Extend-Release Apixaban 5 mg through direct compression and wet granulation. Particularly, Apixaban tablets were developed using design expert software, and various types and concentrations of polymers were entered. For Clopidogrel tablets, various diluents were used to develop the formulation. Then, the dissolution profile for each formula was studied. Finally, the optimized formulations were encapsulated within hard gelatin capsules. Apixaban formulation followed zero-order with super case Ⅱ transport mechanism as the dominant mechanism of drug release. The Apixaban drug release rate was affected by the type and concentration of the polymers in the formulation (P < 0.05). As the HPMC concentration was increased, Apixaban release was retarded. For, Clopidogrel, the formulated tablets with spray-dried lactose filler and sodium stearyl fumarate lubricant were found to be stable with good properties. In conclusion, the optimum formulation yielded Clopidogrel and extended-release Apixaban for 24 h with the desired in vitro drug dissolution.

Simulated acetaminophen plasma profiles from fixed-dose combination formulations: studies using the flow-through cell dissolution method

The aim of this work was to simulate acetaminophen plasma profiles from two fixed-dose combination formulations (acetylsalicylic acid, acetaminophen, and caffeine of generic vs. reference formulation) and in vitro dissolution data generated by the flow-through cell apparatus (laminar flow of 16 ml/min, 22.6 mm cells and 0.1 M phosphate buffer pH 7.4). Results were compared with in vitro release information of USP apparatus type II (paddle at 100 rpm and 900 ml of same dissolution medium). Dissolved drugs until 60 min were determined with a ratio-derivative spectrophotometric method. To compare dissolution profiles of each drug, dissolution efficiency and mean dissolution time were calculated. To predict in vivo behavior a convolution approach as well as acetaminophen published information were used. Peak plasma concentrations and area under the curve (zero time to infinity) were considered and values of predicted error for these pharmacokinetic parameters were established. When comparing dissolution profiles with Student’s t-tests significant differences were found (p &lt; 0.05). All values of predicted error showed satisfactory results since only data generated by the flow-through cell dissolution method achieved &lt; 10% for each pharmacokinetic parameter. It is important to carried out in vivo studies with used formulations to corroborate the obtained results.

Can in vitro/in silico tools improve colonic concentration estimations for oral extended-release formulations? A case study with upadacitinib

Upadacitinib, classified as a highly soluble drug, is commercially marketed as RINVOQ®, a modified-release formulation incorporating hydroxypropyl methylcellulose as a matrix system to target extended release throughout the gastrointestinal (GI) tract. Our study aimed to explore how drug release will occur throughout the GI tract using a plethora of in vitro and in silico tools. We built a Physiologically-Based Pharmacokinetic (PBPK) model in GastroPlus™ to predict the systemic concentrations of the drug when administered using in vitro dissolution profiles as input to drive luminal dissolution. A series of in vitro dissolution experiments were gathered using the USP Apparatus I, III and IV in presence of biorelevant media, simulating both fasted and fed state conditions. A key outcome from the current study was to establish an in vitro-in vivo correlation (IVIVC) between (i) the dissolution profiles obtained from the USP I, III and IV methods and (ii) the fraction absorbed of drug as deconvoluted from the plasma concentration-time profile of the drug. When linking the fraction dissolved as measured in the USP IV model, a Level A IVIVC was established. Moreover, when using the different dissolution profiles as input for PBPK modeling, it was also observed that predictions for plasma Cmax and AUC were most accurate for USP IV compared to the other models (based on predicted versus observed ratios). Furthermore, the PBPK model has the utility to extract the predicted concentrations at the level of the colon which can be of utmost interest when working with specific in vitro assays.

Investigating the Influence of Processing Conditions on Dissolution and Physical Stability of Solid Dispersions with Fenofibrate and Mesoporous Silica.

The study aimed to enhance the solubility of the poorly water-soluble drug, fenofibrate, by loading it onto mesoporous silica, forming amorphous solid dispersions. Solid dispersions with 30% fenofibrate were prepared using the solvent evaporation method with three solvents (ethyl acetate, acetone, and isopropanol) at different temperatures (40 °C, boiling point temperature). Various characteristics, including solid-state properties, particle morphology, and drug release, were evaluated by different methods and compared to a pure drug and a physical mixture of fenofibrate and silica. Results revealed that higher solvent temperatures facilitated complete amorphization and rapid drug release, with solvent choice having a lesser impact. The optimal conditions for preparation were identified as ethyl acetate at boiling point temperature. Solid dispersions with different fenofibrate amounts (20%, 25%, 35%) were prepared under these conditions. All formulations were fully amorphous, and their dissolution profiles were comparable to the formulation with 30% fenofibrate. Stability assessments after 8 weeks at 40 °C and 75% relative humidity indicated that formulations prepared with ethyl acetate and at 40 °C were physically stable. Interestingly, some formulations showed improved dissolution profiles compared to initial tests. In conclusion, mesoporous silica-based solid dispersions effectively improved fenofibrate dissolution and demonstrated good physical stability if prepared under appropriate conditions.

Dissolution Profiles of Immediate Release Products of Various Drugs in Biorelevant Bicarbonate Buffer: Comparison with Compendial Phosphate Buffer

PurposeThe purpose of this study was to clarify the extent to which the dissolution profiles of immediate release (IR) products of various drugs differ between biorelevant bicarbonate buffer (BCB) and compendial phosphate buffer (PPB).MethodsThe dissolution profiles of the IR products of fifteen poorly soluble ionizable drugs were measured in BCB and PPB. BCB was set to be relevant to the small intestine (pH 6.8, 10 mM). The pH was maintained using the floating lid method. The Japanese pharmacopeia second fluid (JP2, 25 mM phosphate buffer, nominal pH 6.8) was used as compendial PPB. The compendial paddle apparatus was used for the dissolution tests (500 mL, 50 rpm, 37°C).ResultsIn 11/15 cases, a difference in dissolved% (< 0.8 or > 1.25-fold) was observed at a time point. In 4/15 cases, the ratio of the area under the dissolution curve was not equivalent (< 0.8 or > 1.25-fold). In the cases of free-form drugs, the dissolution rate tended to be slower in BCB than in JP2. In the case of salt-form drugs, a marked difference was observed for the cases that showed supersaturation. However, no trend was observed in the differences.ConclusionsMany IR products showed differences in the dissolution profiles between biorelevant BCB and compendial PPB. With the floating lid method, BCB is as simple and easy to use as PPB. Biorelevant BCB is recommended for dissolution testing.

Enhancement in Dissolution Profile of Cilnidipine by Nanonization Technique: Optimization by Box-Behnken design

Objectives: Cilnidipine has limited 25-30% of bioavailability due to BCS class II category drug. The aim of present work was to improve the solubility followed by dissolution rate of cilnidipine by formulation of nanosuspension. Materials and Methods: The nanosuspensionwas developed usingnanoprecipitation techniqueaidingultra-sonication with solvent (Dimethyl sulfoxide), antisolvent (water) and stabilizer (polyvinyl alcohol). The nano formulation was statistically optimized using Design Expert software by theBox-Behnken design. The concentration of Poly Vinyl Alcohol, Volume of Antisolvent and Stirring Time were considered as independent factors whereas Particle size and polydispersity index were considered as dependent factors. Results: The particle size of nanosuspension was found 178.57nm with narrow polydispersity index of 0.130. The microscopy study confirmed amorphous nature particles with rough surface. The zeta potential of 4.55 ±2.78 for optimized formulation finds stability of formulation during storage. The differential scanning calorimetry study and X-ray diffraction pattern showed the crystalline cilnidipine drug was converted to amorphous form upon precipitation into nanoparticles. Due to the nanonization of cilnidipine, the dissolution profile was noted as 92.41±3.56% which was significantly improved as compared with plain drug release data. The stability data showed satisfactory result for 2 months. Conclusion: It is summarized that the nanoprecipitation technique with ultra-sonication is approaching method for the formulation of homogenous nanosuspension with uniform sized dispersion of cilnidipine. Therefore, it can be assumed that the upon the enhancement in dissolution rate, the cilnidipine loaded nanosuspension may lead to improved absorption of drug from intestine followed by significant improvement in bioavailability.

Formulation, Optimization and Evaluation of Ticagrelor Liquisolid Tablets for Enhanced Solubility

Purpose The study aims to use liquisolid compacts technology as a novel carrier to enhance Ticagrelor's solubility and release profile. Method: Formulation of liquisolid tablets was developed using the Design of Experiment (DOE) approach where the drug Ticagrelor was dispersed in PEG-600 and incorporated into carrier material (Neusilin US2) in the mortar, the liquid drug was permitted to absorb in the second stage. Aerosil-200 was used as a coating material, and Magnesium stearate and Sodium starch Glycolate were used as Lubricant and Disintegrating Agent respectively. The formulations were optimized and the carrier-to-coating ratio and mixing Aerosil-200 with Neusilin US2 effect on drug release from the formulation was investigated. The prepared liquisolid compacts were subjected to micrometric characterization, post-compression parameters, Fourier Transform Infrared Spectroscopy (FTIR), and Differential Scanning Calorimetry (DSC). Result: The cumulative drug release of all formulations in dissolution media varies from 82% to 96% and Formulation F9 showed a maximum cumulative drug release of about 96%. The drug contents of all formulations ranged from 91.06% to 99.01%. Disintegration time for all 1-9 formulations, clearly, all compositions disintegrate in less than 10 minutes. The cumulative drug release of all formulations varies from 82% to 96% Formulation F9 showed a maximum cumulative drug release of about 96% and the conventional tablet showed a cumulative drug release of about 80 %. The optimized liquisolid formulation F8 outperformed the other batches in terms of flow and compressibility across all formulations. Conclusion: Therefore, as per the results, it can be inferred that Ticagrelor, when formulated by a liquisolid approach, produce ameliorated dissolution and stability profile.

Dissolution and antioxidant potential of apigenin self nanoemulsifying drug delivery system (SNEDDS) for oral delivery

Self-nanoemulsifying drug delivery systems (SNEDDS) have been used to improve the oral bioavailability of various drugs. In the current study, apigenin was developed as SNEDDS to solve its dissolution problem and enhance oral bioavailability and antioxidant potential. SNEDDS were prepared by mixing Gelucire 44/14, Tween 80, and PEG 400 under controlled conditions. The droplet of diluted SNEDDS demonstrated a spherical shape with a size of less than 100 nm and a neutral charge. The very fast self-emulsification was obtained within 32 s, and the transmittance values exceeded 99%. The highest drug loading was 90.10 ± 0.24% of the initial load with the highest %encapsulation efficiency of 84.20 ± 0.03%. FT-IR and DSC spectra showed no interaction between components. The dissolution in buffer pH 1.2, 4.5, and 6.8 showed significantly higher dissolved apigenin than the apigenin coarse powder. The dissolution profiles were fitted to the Korsmeyer–Peppas kinetics. The cellular antioxidant activities in Caco-2 cells were approximately 52.25–54.64% compared to no treatment and were higher than the apigenin coarse powder (12.70%). Our work highlights the potential of SNEDDS to enhance the dissolution and permeability of apigenin and promote antioxidant efficacy, which has a strong chance of being developed as a bioactive compound for nutraceuticals.