Solid Dispersion Approach Research Articles

Surface Solid Dispersion of Ketoconazole on Trehalose Dihydrate using Spray Drying to Achieve Enhanced Dissolution Rate.

Ketoconazole (K) is a poorly water-soluble drug that faces significant challenges in achieving therapeutic efficacy. This study aimed to enhance the dissolution rate of ketoconazole by depositing spray-dried ketoconazole (SK) onto the surface of ground trehalose dihydrate (T) using spray drying. Ketoconazole-trehalose surface solid dispersions (SKTs) were prepared in ratios of 1:1 (SK1T1), 1:4 (SK1T4), and 1:10 (SK1T10), and characterized them using particle size analysis, scanning electron microscopy, powder X-ray diffraction, and in vitro dissolution studies. Results showed that the dissolution rates of the dispersions were significantly higher than those of pure ketoconazole, with the 1:10 ratio showing the highest dissolution rate. The improved dissolution was attributed to the formation of a new crystalline phase and better dispersion of ketoconazole particles. These findings suggest that the surface solid dispersion approach could be a valuable method for enhancing the bioavailability of poorly water-soluble drugs.

Formulation and evaluation of novel orodispersible tablet by drug-drug solid dispersion of metoprolol tartrate and hydrochlorothiazide

This study investigates the effect of a novel drug-drug solid dispersion approach on the dissolution of hydrochlorothiazide in a fixed-dose combination with metoprolol tartrate. Solid dispersions of hydrochlorothiazide and metoprolol tartrate (12.5 mg: 25 mg) were prepared using the solvent evaporation technique. These dispersions were characterized by differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FTIR). The prepared solid dispersions, along with selected excipients, were compressed into orodispersible tablets and evaluated for precompression and post compression parameters. The solubility of hydrochlorothiazide was observed to increase with the concentration of metoprolol tartrate, as demonstrated by phase solubility studies and comparative solubility studies. Stability studies on the tablets indicated no significant changes in disintegration time, dissolution profile, or overall stability. The findings of this study suggest that the novel drug-drug solid dispersion approach is promising for enhancing the dissolution of poorly soluble drugs, when combined with soluble drugs in fixed-dose combinations.

Enhancement of Dissolution Rate of Piperine Using Solid Dispersion Approach and Evaluation of Its Antioxidant Activity

Enhancement of Dissolution Rate of Piperine Using Solid Dispersion Approach and Evaluation of Its Antioxidant Activity

Versatile DNA extraction from diverse plant taxa using ionic liquids and magnetic ionic liquids: a methodological breakthrough for enhanced sample utility

BackgroundThere is a growing demand for fast and reliable plant biomolecular analyses. DNA extraction is the major bottleneck in plant nucleic acid-based applications especially due to the complexity of tissues in different plant species. Conventional methods for plant cell lysis and DNA extraction typically require extensive sample preparation processes and large quantities of sample and chemicals, elevated temperatures, and multiple sample transfer steps which pose challenges for high throughput applications.ResultsIn a prior investigation, an ionic liquid (IL)-based modified vortex-assisted matrix solid phase dispersion approach was developed using the model plant, Arabidopsis thaliana (L.) Heynh. Building upon this foundational study, the present study established a simple, rapid and efficient protocol for DNA extraction from milligram fragments of plant tissue representing a diverse range of taxa from the plant Tree of Life including 13 dicots and 4 monocots. Notably, the approach was successful in extracting DNA from a century old herbarium sample. The isolated DNA was of sufficient quality and quantity for sensitive molecular analyses such as qPCR. Two plant DNA barcoding markers, the plastid rbcL and nuclear ribosomal internal transcribed spacer (nrITS) regions were selected for DNA amplification and Sanger sequencing was conducted on PCR products of a representative dicot and monocot species. Successful qPCR amplification of the extracted DNA up to 3 weeks demonstrated that the DNA extracted using this approach remains stable at room temperature for an extended time period prior to downstream analysis.ConclusionsThe method presented here is a rapid and simple approach enabling cell lysis and DNA extraction from 1.5 mg of plant tissue across a broad range of plant taxa. Additional purification prior to DNA amplification is not required due to the compatibility of the extraction solvents with qPCR. The method has tremendous potential for applications in plant biology that require DNA, including barcoding methods for agriculture, conservation, ecology, evolution, and forensics.

Supersaturable diacyl phospholipid dispersion for improving oral bioavailability of brick dust molecule: A case study of Aprepitant

This study aims to investigate the potential use of polymer inclusion in the phospholipid-based solid dispersion approach for augmenting the biopharmaceutical performance of Aprepitant (APT). Initially, different polymers were screened using the microarray plate method to assess their ability to inhibit drug precipitation in the supersaturated solution and HPMCAS outperformed the others. Later, the binary (BD) and ternary (TD) phospholipid dispersions were prepared using the co-solvent evaporation method. Solid-state characterization was performed using SEM and PXRD to examine the physical properties, while molecular interactions were probed through FTIR and NMR analysis. In vitro dissolution studies were performed in both fasted and fed state biorelevant media. The results demonstrated a substantial increase in drug release from BD and TD, approximately 4.8 and 9.9 times higher compared to crystalline APT in FaSSIF. Notably, TD also showed a lowered dissolution difference between fed and fasted states in comparison to crystalline APT, indicating a reduction in the positive food effect of APT. Moreover, we assessed the impact of polymer inclusion on permeation under in vitro biomimetic conditions. In comparison with the crystalline APT suspension, both BD and TD demonstrated approximately 3.3 times and 14 times higher steady-state flux (Jss values), respectively. This can be ascribed to the supersaturation and presence of drug-rich submicron particles (nanodroplets) along with the multiple aggregates of drug with phospholipids and polymer in the donor compartment, consequently resulting in a more substantial driving force for passive diffusion. Lastly, in vivo pharmacokinetic evaluation demonstrated the enhanced absorption of both TD and BD over the free drug suspension in the fasted state. This enhancement was evident through a 2.1-fold and 1.3-fold increase in Cmax and a 2.3-fold and 1.4-fold increase in AUC0-t, respectively. Overall, these findings emphasize the potential of polymer-based phospholipid dispersion in enhancing the overall biopharmaceutical performance of APT.

Formulation and Evaluation of Biopolymer Incorporated Nanogel of Nabumetone

ABSTRACT: The objective of this research was to improve the solubilization, dissolution rate, and thereby anti-inflammatory activity of the BCS class II drug Nabumetone (NSAID). A solid dispersion (SD) approach with Gelucire 50/13 was used to enhance the solubility. Microwave-induced fusion method was used for the development of SD, as it demonstrated a remarkable increase in the solubility and dissolution rate of pure drugs when compared to traditional solid dispersions. A number of parameters of the SD were evaluated in vitro, including solubility, dissolution, and Fourier Transformed Infrared Spectra obtained (FT-IR). The rate of dissolution was inclined to betterment with the drug: polymer ratio 1:0.5 showing drug release 99.60 ± 29. The objective of the work was to evolve a Nanogel for topical delivery of Nabumetone. The emulsification-diffusion method was used to create nanogel using the polymers Carbopol-940, Gelucire-50/13, and triethanolamine as gelling agents. Chitosan was added to the formulation as a biopolymer. Menthol was employed as a penetration enhancer. Using the spontaneous emulsification-diffusion method, six distinct formulations of Nabumetone-loaded Nanogel were successfully created and evaluated for particle size, zeta potential, thermodynamic stability, and rheology study. Using a cellophane membrane, the gels were examined for diffusion study further, and drug content, viscosity, spreadability, pH, and clarity were accessed. The formulation F4 batch had the best in-vitro drug release profile, with a 96.04% release rate over 270 minutes. Optimized gel F4 underwent a skin irritation study on Wistar rats and passed the test. The topical application of Nabumetone as Nanogel proved to be an effective approach to drug delivery.

DESIGN OF EXPERIMENTS AND OPTIMIZATION OF AMORPHOUS SOLID DISPERSION OF A BCS CLASS IV ANTI-PLATELET DRUG THROUGH FACTORIAL DESIGN

Objective: The aim of this study was to evaluate and optimize the amorphous solid dispersion of a low-soluble BCS Class IV anti-platelet drug using factorial design in line with the Quality by Design (QbD) principle. Methods: Ticagrelor, a low-soluble anti-platelet agent, was used as the model drug for the current study. A solid dispersion technique was explored to improve the dissolution of ticagrelor. The extent of amorphization of ticagrelor with the solid dispersion approach was evaluated with powder X-Ray diffraction (p-XRD) and differential scanning calorimetry (DSC). The principle of factorial design (FD) was adopted to optimize the formulation of ticagrelor solid dispersion. Design Expert® 13 (Stat-Ease Inc., Minneapolis, MN, USA) was explored for the Design of experiments (DoE) and Statistical evaluation. The experiments were designed with three factors at two levels (a 23-factor design) and two responses. The significance of the model was evaluated by analysis of variance (ANOVA) and fit statistics. Various statistical parameters such as sequential p-values, lack of fit, squared correlation coefficient (R2), adjusted R2, and adequate precision were considered in fit statistics. Results: The crystalline ticagrelor has completely amorphized, as indicated by the powder x-ray diffraction (p-XRD) and differential scanning calorimetry (DSC) of the solid dispersion of ticagrelor prepared with copovidone VA 64 and vitamin E TPGS through solvent evaporation technique. An increase in ticagrelor dissolution by 10.7 fold was possible through solid dispersion technology. The lack of fit F-values of 0.11 and 0.00 in the factorial model for response dissolution at 10 min and disintegration time, respectively, are indicative of a good fit. The ANOVA and the fit statistics for the selected factorial model were found to be significant. Conclusion: A solid dispersion technique with carrier copovidone VA 64 and vitamin E TPGS could enhance the dissolution of ticagrelor significantly, to an extent of 10.7 fold. Factorial design is an important tool in optimizing the amorphous solid dispersion of ticagrelor and establishing the design space.

INVESTIGATION OF SOLID DISPERSION APPROACH FOR THE IMPROVEMENT OF PHARMACEUTICAL CHARACTERISTICS OF TELMISARTAN USING A CENTRAL COMPOSITE DESIGN

Objective: The goal of this study was to use a solid dispersion approach to improve the aqueous solubility and dissolution rate of Telmisartan. Methods: Design of experiment trials was conducted following a central composite design with different combinations of polymers and stirrer rpm and the selected responses (drug release, entrapment efficiency) were determined. The selected optimized formulation was characterized by Fourier-transform infrared spectroscopy, differential scanning calorimetry, scanning electron microscopy, and X-ray diffraction, which reflected the changes that occurred in API and excipients after conversion in to the formulation. Results: In the design of experiments, central composite design was implemented and it was observed that polymers concentration (polyvinyl pyrrolidine K25, polyethylene glycol 4000) and stirrer rpm were having a significant impact on the responses (drug release, entrapment efficiency), and variables were having p-value<0.05 which reflected the significant impact. The results of stability study showed a significant no decrease in drug assay values, which reflected the stability behavior of the formulation. The results of comparative dissolution studies revealed that the optimized formulation have improved the drug solubility and dissolution rate. Conclusion: It can be concluded that optimized telmisartan-loaded solid dispersion improved the solubility and dissolution rate of Telmisartan. The optimized formulation was having release>85% release within 30 min. Further, the stability of the formulation was also assessed under the accelerated condition as per ICH which reflected their stability. So, this approach can be employed for improving dissolution rate of other BCS II class drugs.

Formulation and Characterization of Solid Dispersion of Oxcarbazepine

The purpose of the current study was to use the solid dispersion approach to improve the solubility of the medication oxcarbazepine, which is only moderately water soluble. The antiepileptic medication oxcarbazepine is used to treat seizures. Due to its high permeability and low water solubility, it falls under BCS class II. To prevent issues of this nature, it was imperative to increase the solubility of oxcarbazepine in accordance with British Pharmacopoeia (BP) solubility criteria since pure oxcarbazepine falls under the category of being only very slightly soluble. Solid dispersion technique has been used to try and increase the solubility of pure oxcarbazepine. Oxcarbazepine is also extensively metabolized by the liver. Attempt has been made to formulate solid dispersions containing oxcarbazepine to improve its solubility and dissolution rate to avoid first pass metabolism; to avoid difficulty.

Atorvastatin calcium formulation development followed by pharmacokinetic with in vitro and in vivo correlation (IVIVC) with employing soluplus and hydroxy propyl methyl cellulose with optimization

Objectives The goal of this study was to evaluate different proportions of solid dispersions and formulations by employing various carriers in order to improve solubility of poorly soluble atorvastatin calcium. Materials and methods Solid dispersions can be created using the Solvent Evaporation technique. In comparison to pure drug, (Hydroxy propyl methyl cellulose) HPMC (1:1) indicated as (Solid dispersion) SD1, HPMC E5 (1:2), HPMC E5 (1:4), HPMC (1:1.5) designated as SD2, SD3, SD4, drug caffeine (1:0.5) and caffeine (1:1), denoted as SD5, SD6. The Design Expert software used to 2 level factorial design, the three independent components of X1: are ratios of solid dispersion equivalent (drug:HPMC:soluplus), X2:Superdisintegrant (Primellose), and X3:Surfactant (Sodium lauryl sulphate) was used to do analysis of variance (ANOVA), 3D surface plots, counter plots, optimization, and desirability. Fourier-transform infrared spectroscopy was used to investigate drug-excipient compatibility. Marketed tablets (uncoated tablets manufactured by ‘Revat Laboratories limited) with optimized tablet composition were used in the comparative trials (A2) and Pharmacokinetics. Results and discussion The solid dispersion approach greatly increased the amount of atorvastatin calcium released. The values of f1 and f2 were determined to be 1.89 and 77.78, respectively, and the dissolution profiles of the optimized formulation (A2) and the market tablet were found to be significance. The optimized formula did better on the desirability level (0.975), indicating that it was a good fit. To determine dose bioavailability and to see if there is an in-vitro-in-vivo link. Conclusion The formulations were successfully developed using factorial design, and can be further used for oral delivery of antilipidemic agents is atorvastatin calcium. The model’s predictability and validity were demonstrated when the experimental values matched the expected values. The in vitro-in vivo correlation was good in pharmacokinetic experiments, indicating a significant improvement.

Novel nano-crystalline solid dispersion of nobiletin with improved dissolution behavior and oral absorption

The present study aimed to develop a novel formulation of nobiletin (NOB, a citrus polymethoxylated flavone) by nano-crystalline solid dispersion (nCSD) approach for improving dissolution behavior and oral absorption. NOB-loaded nCSD (nCSD/NOB) was prepared by a wet-milling and freeze-drying systems. Physicochemical properties of nCSD/NOB were characterized in terms of crystallinity, dissolution behavior, particle size distribution, and surface morphology. An analytical method was developed and validated, and a pharmacokinetic study was conducted after oral administration of nCSD/NOB to rats. NOB particles in nCSD/NOB appeared to be crystalline, and the mean diameter was calculated to be ca. 120 nm. In water and acidic condition (pH 1.2), dissolution rates of NOB in nCSD/NOB were ca. 31- and 32-fold higher than those in crystalline NOB, respectively. After oral administration of nCSD/NOB (20 mg-NOB/kg) to rats, nCSD/NOB showed enhanced exposure of NOB compared with crystalline NOB, as evidenced by 12-fold increase of Cmax. The absolute oral bioavailability of NOB in nCSD/NOB was calculated to be ca. 13%, showing 15-fold enhancement compared with that in crystalline NOB. From these findings, the nCSD approach would be efficacious for improving oral absorption of NOB, leading to its enhanced nutraceutical potential.

Carvedilol Precipitation Inhibition by the Incorporation of Polymeric Precipitation Inhibitors Using a Stable Amorphous Solid Dispersion Approach: Formulation, Characterization, and In Vitro In Vivo Evaluation.

An amorphous solid dispersion (ASD) of carvedilol (CVL) was prepared via the solvent evaporation method, using cellulose derivatives as polymeric precipitation inhibitors (PPIs). The prepared ASDs existed in the amorphous phase, as revealed by X-ray powder diffraction (XRPD) and scanning electron microscopy (SEM). The Fourier-transform infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC) results confirmed the compatibility between CVL and the polymers used. The ASDs characteristics were evaluated, with no change in viscosity, a pH of 6.8, a polydispersity index of 0.169, a particle size of 423-450 nm, and a zeta potential of 3.80 mV. Crystal growth inhibition was assessed for 180 min via an infusion precipitation study in simulated intestinal fluid (SIF). The interactions between the drug and polymers were established in great detail, using nuclear magnetic resonance (NMR) spectroscopy, nuclear Overhauser effect spectroscopy (NOESY), and Raman spectroscopy studies. Dielectric analysis was employed to determine the drug-polymer interactions between ion pairs and to understand ion transport behavior. In vivo oral kinetics and irritation studies performed on Wistar rats have demonstrated promising biocompatibility, stability, and the enhanced bioavailability of CVL. Collectively, the stable ASDs of CVL were developed using cellulose polymers as PPIs that would inhibit drug precipitation in the gastrointestinal tract and would aid in achieving higher in vivo drug stability and bioavailability.

Formulation Characterization and Pharmacokinetic Evaluation of Amorphous Solid Dispersions of Dasatinib.

The aim of this study was to improve the physicochemical properties and oral bioavailability of dasatinib (DST) by the amorphous solid dispersion (ASD) approach using cellulose acetate butyrate (CAB) as a carrier. Various formulations of ASD (DST:CAB 1:1 to 1:5) were prepared by the solvent evaporation method. ASDs were characterized for physicochemical attributes, stability and pharmacokinetics. Scanning electron microscopy, Fourier transformed infrared, X-ray powder diffraction, and differential scanning calorimetry confirmed the transformation of the crystalline drug into amorphous phase. ASD formation resulted in a 3.7-4.9 fold increase in dissolution compared to DST or physical mixture. The ASDs formulation exhibited relative stability against transformation from the unstable amorphous phase to a stable crystalline phase that was indicated by spectral and X-ray powder diffraction data, and insignificant (p > 0.05) decrease in dissolution. Tmax, Cmax and AUC0-∞ of ASD were 4.3-fold faster and 2.0 and 1.5 fold higher than the corresponding physical mixture. In conclusion, the ASD of DST significantly improved dissolution and oral bioavailability which may be translated into a reduction in dose and adverse events.

A Comprehensive Review on Solid Dispersion Technique to Enhance the Solubility and Bioavailability of Poorly Water-Soluble Drugs

The majority of the time, oral administration of medications to patients is chosen. However, many medications have limited uses in oral delivery due to their low solubility. In the pharmaceutical industry, improving a drug's water solubility is a primary goal. One of the most crucial elements affecting bioavailability and dissolution rate is solubility. By using different polymers, the solid dispersion approach improves the bioavailability and dissolution rate of poorly soluble medicines. In this review, techniques for solid dispersion were examined, along with the characterization of solid dispersions.

Dissolution enhancement of Enzalutamide by solid dispersion approach

Enzalutamide (ENZ) is a BCS class II, fast crystallizing, a hydrophobic compound that has solubility limited absorption in vivo. Ternary solid dispersion of Enzalutamide was prepared with water-soluble polymers Soluplus (SOL) and Poloxamer P 188 (POL) by solvent evaporation spray drying technique. Initially, different ratios of Soluplus: Poloxamer and solvents were used to prepare Ternary solid dispersions of Enzalutamide and evaluated for the dissolution enhancement property. The prepared solid dispersion was characterized by FTIR spectroscopy, Differential scanning calorimetry (DSC), X-ray diffraction (XRD) analysis, Scanning electron microscopy (SEM), Particle size distribution (PSD) by Malvern and Physico-chemical analysis. FTIR spectroscopy shows that there was no interaction between the ENZ and polymers. DSC and XRD analysis show that conversion to amorphous form of ENZ in ternary SD, which enhances the dissolution rate. In vitro dissolution studies and Ex-vivo intestinal absorption studies clearly show that the prepared solid dispersion enhanced the dissolution and ex-vivo intestinal absorption of ENZ compared with pure ENZ.

A Study on Improving Bioavailability of Paclitaxel through different Novel Drug Delivery Approaches

Paclitaxel (PTX) obtained from the bark of Taxus brevifolia (Pacific yew tree) is a well-known potent drug used for treatment of breast, lung and ovarian cancer. PTX is stated to be a novel antimicrotubule agent. PTX acts by assembling the microtubule from tubulin dimmers and stabilizing of microtubules by prevention of polymerization. Thus it affects the cell division of the cancer cells by interrupting the spindle formation. PTX on application in cancer treatment it shows to have low aqueous solubility use of vehicles like Cremophore EL and ethanol, which on application shows hypersensitivity reaction. So to reduce the toxicity due to these vehicles three main dosage forms are seen to be developed for application of PTX in chemotherapy by researchers throughout the world. Namely; Nano-Particle Approaches, Liposomal approach, Solid Dispersion approach. Nanoparticles are utilized for purposes like decreasing toxicity and minimizing adverse effects of drug molecules and enhancing drug release. Liposomes are capable of containing more amount of PTX and are capable of long term stability, toxicity reduction when compared to other dosage form. Solid dispersions are more effective compared to other methods of particle size reduction to improve the drug solubility. So it can be stated that developing dosage forms like these for reduction of toxicity and efficacious application of PTX in chemotherapy is important.

NEVIRAPINE SOLID DISPERSION: DESIGN, DEVELOPMENT AND EVALUATION

The objective of the present investigation was to enhance the solubility and dissolution rate of BCS class II drug nevirapine through scalable and commercially feasible solid dispersion approach by using Soluplus® (BASF) as hydrophilic carrier. The solid dispersion produced by melting method (1:5 weight ratio) exhibited highest solubility ~ 15 folds greater than pure drug. The changes in DSC, PXRD, and SEM validated the formation of solid dispersion and transformation of drug from crystalline to amorphous form. Besides, selected solid dispersion had better flow properties and higher dissolution rate than nevirapine. Furthermore, the two dissolution profiles were different (f2 value 33). Hence, preparation of nevirapine-soluplus® solid dispersion by melting method could be an appropriate pharmaco technical strategy to enhance the solubility and dissolution rate of nevirapine and probably other BCS class II drugs.

Solid Dispersion Preparation by Different Methods to Improve Solubility & Dissolution Simvastatin

The improvement of a pure drug's solubility and dissolution rate in the treatment of hyperlipidemia. Simvastatin is a 5-percent absolute bioavailability selective competitive inhibitor of HMG Co-A reductase. For the selection of the carrier, a preliminary solubility investigation of solid dispersion was performed, and solid dispersion was made using Hydroxy Propyl Methyl Cellulose (HPMC) and gum acacia. Solid dispersion of medication with polymer was created and studied for solubility and in-vitro dissolution profile. Solid dispersion of drug with polymer has shown an increase in solubility and improved dissolution rate. On the obtained formulations, further FTIR, X-Ray, Scanning electron microscopy, and Differential scanning calorimetry experiments were conducted. The existence of amorphous form in a solid dispersion made with polymer in a 1:5 ratio is verified by characterization research. The research also showed that using a solid dispersion approach with Polymer, the dissolving rate of a pure medication may be significantly increased.

Design of Experiment Approach to Assess the Effect of Formulation Variables on Extrusion and Spheronization of Telmisartan and Cilostazol Loaded Pellets and its Pharmacokinetic Study

Background: Solubility is an important parameter that affects the availability of drug in systemic circulation. Drugs having poor solubility belonging to BCS class II eventually result in lower dissolution and bioavailability. Hence, improvement of solubility is a challenging task. Hence the present work focuses on using solid dispersion and inclusion complex approach for both telmisartan and cilostazol belonging to BCS Class II drugs. Objective: The present study was carried out to improve apparent solubility of telmisartan and cilostazol (BCS-Class II drugs) and optimization as pellets along with its pharmacokinetic study. Methods: Phase solubility study was carried out to screen the excipients such as, PVPK30, PVA, HPMC E5 and β-CD. Solvent evaporation method was adopted to prepare the solid dispersions and inclusion complex of both drugs. Pellets were optimized by extrusion spheronization method using 32 factorial design and characterized by morphology, drug content, DSC, FTIR, XRD, SEM, in- -vitro studies and drug content study. Results: Phase solubility study showed improved apparent solubility of telmisartan with HPMC E5 (1:3) by solid dispersion and cilostazol with β-CD (1:3) using inclusion complexation method. Drug characterization did not reveal any incompatibility. Formulation was optimized on the basis of acceptable pellet properties, including acceptable spherical shape and micromeritics properties. The percent friability of all batches was found to be less than 1%. The optimized pellets of both drugs prepared with micro crystalline cellulose provided desirable maximum release with acceptable release profile. Conclusion: The formulated pellets when studied in vivo showed superior pharmacokinetic profile. The drawback associated with apparent solubility and bioavailability of both drugs can thus be alleviated by use of novel pellet formulation.

Recent Advances in Delivering Strategies of Domperidone: Challenges and Opportunities

Domperidone (DMP), a potent gastroprokinetic and antiemetic drug, exhibits poor aqueous solubility and limited oral bioavailability. Therefore, to develop oral preparations with optimized oral bioavailability, the pharmacokinetic parameters of DMP need to be controlled. The present review aimed to discuss the physicochemical characteristics of DMP causing its unfavorable oral delivery, to explore the viable oral formulation approaches, and to propose some recent formulation approaches that can mitigate the above mentioned difficulties in delivering DMP. In this study, some effective strategies in terms of pharmacokinetic behavior of DMP have been comparatively discussed. It has been recommended that, the amorphous solid dispersion approach could be more convincing from the scalability perspective along with its significant improvement in dissolution behavior and oral bioavailability. Finally, some future perspectives of these strategies have also been addressed to facilitate efficient formulation development.