PVP K30 Research Articles

Application of design of experiments for development and characterization of coprocessed excipients using Lapidium Sativum

The development of novel excipients with enhanced functionality has been explored using particle engineering by co-processing. The aim of this study was to improve the functionality of Lapidium Sativum for direct compression by co-processing with MCC pH 101 and PVP K30 in optimized proportions. Design of Experiment (DoE) was employed to optimize the composition of the co-processed excipient using the desirability function and other supporting studies as a basis for selecting the optimized formulation. The co-processed excipient was thereafter developed by the method of spraydrying. Flow and compaction studies of coprocessed excipient were carried out in comparison to its parent component and physical mixture. Tablets were prepared by direct compression (DC) containing Venlafaxine hydrochloride (100 mg) as a model for poor compressibility. Tablets produced with CPE were satisfactory and conformed to USP specifications for acceptable tablets. The application of DoE was successful in optimizing and developing a starch-based co-processed excipient that can be considered for direct compression tableting.

Effect of combination of some Polymers with Carbopol 940 on Pregabalin Release Rate from Emulgels

Topical Emulgels of Pregabalin were formulated using Carbopol 940 in combination with (PVP k90, PEG 200, PEG 1000, HPMC K15M) to obtain the optimal formula in terms of drug release rate. Physical appearance, pH, viscosity, stability, drug content, In-vitro drug release, Differential scanning calorimetry and Fourier transform infrared spectroscopy, were tested in all formulas and evaluated to determine the best one. All formulations had good physical properties and stability, F2 which contains Carbopol 940 0.4% and HPMC K15M 0.4% gave the best drug release rate: (30% in 20 min and 93% in 360 min). But F3 which contains Carbopol 940 0.4% and PEG 200 10% showed the less release rate at 360 min: (64%). F2 showed Korsmeyer–Peppas model Kinetic release. So F2 was the best formula because it released drug since 10 min and still to 360 min (6 hours), thus F2 can be used to obtain rapid analgesic effect and avoid CNS-mediated side effects of Pregabalin.

Formulation and Evaluation of Buccal Disintegrating Tablet of Anticonvulsant Drug

Oral and Buccal delivery is currently the gold standard in the pharmaceutical industry where it is regarded as the safest, most convenient and most economical method of drug delivery having the highest patient compliance. To troubleshoot such problems a new dosage form known as Buccal and orally disintegrating tablet, has been developed which rapidly disintegrate and dissolve in saliva and then easily swallowed without need of water which is a major benefit over than conventional dosage form. In addition, patients suffering from dysphasia, motion sickness, repeated emesis and mental disorders prefer such preparation because they cannot swallow large quantity of water. the immediate release of medication and for instant release at desire location in which the drug is absorbed distributer and easily metabolized. e.g. To prepare and characterize buccal tablets of Gabapentin using different super disintegrants such as Cross povidon, PVP K30, Micro crystalline cellulose. This types of formulation of improving solubility of drug and development of Buccal drug delivery system.

Polymer Coated Polymeric (PCP) microneedles for sampling of drugs and biomarkers from tissues

The Polymer Coated Polymeric (PCP) microneedles were fabricated using PVP K30 in the core and ethyl cellulose in the coating. The PCP microneedles do not disintegrate in the tissue upon insertion and rather stays intact and allows diffusion of drugs and analytes across the membrane both inward and outward. In this project the potential use of PCP microneedles for sampling analytes from the dermal tissue was explored. The amount of analyte sampled depended on the concentration in the tissue, physicochemical properties of the analyte and duration of insertion of the array in the tissue. Further, an advanced type of PCP microneedle array was fabricated by entrapping absorbent beads in the core microneedles. The adsorbent enabled the PCP microneedles to recover significantly higher amount of analyte from the tissue.

Preparation, optimization and bioavailability studies of the bergenin solid dispersion pellets

In this study, the bergenin solid dispersion pellets (BN-SDP) were prepared using fluidized bed technology by spraying the bergenin (BN) and PVP K30 mixed solution onto the blank pellets. The preparation technology was also optimized by the central composite design response surface methodology. The three significant parameters including air inlet speed, temperature, and injection speed were obtained as 11.6 m/s, 34.3 °C, and 9.0 mL/min, respectively, and drug loading around 12.5%. In vitro results showed that the cumulative release percentages of the BN-SDP were 100% within 20 min. Furthermore, the FTIR, XRD, and DSC findings presented a clear binding pattern between BN and PVP K30 along with amorphous properties in the BN-SDP. The Tmax was earlier for BN-SDP and the Cmax increased one time with BN as a reference, On the other hand, the AUC0-∞ were 536.15 ± 20.64 μg·h/mL and 361.70 ± 35.93·μg h/mL for the BN-SDP and BN, respectively. The oral bioavailability of BN-SDP was enhanced by 1.48 folds in comparison with BN suspension, indicating the solid dispersion technology can increase the oral bioavailability of the BN.

Solubility Enhancement of Pioglitazone by Solid Dispersion Method

The major challenge with conventional dosage forms of Pioglitazone is poor aqueous solubility. Through this study are to improve its aqueous solubility by preparing its solid dispersion by fusion method using various carriers that will improve its absorption and subsequent bioavailability. The solid dispersions of Pioglitazone were prepared using PEG-4000, PEG-6000 and PVP K30 as carrier, using fusion method. Solid dispersions of Pioglitazone were prepared using PEG-4000, PEG-6000 and PVP K30 as carrier, using fusion method and total 9 formulation (F1-F9) were prepared. Tablets were prepared (TF5) from the optimum formulation (F5). The prepared tablets (TF5) were subjected to evaluation for parameters like shape and size, weight variation, hardness, friability, disintegration time, drug content etc. The solid dispersion (F5) as well as the tablet (TF5) showed greater rate and extent of dissolution as compared to pure drug.
 Keywords: bioavailability, dissolution rate, PEG, PVP K30, solid dispersion, Pioglitazone

Osmolality of Excipients for Parenteral Formulation Measured by Freezing Point Depression and Vapor Pressure - A Comparative Analysis.

To investigate the difference in methods to determine the osmolality in solutions of stabilizers used for long-acting injectable suspensions. The osmolality was measured by freezing point depression and vapor pressure for 11 different polymers and surfactants (PEG 3350, 4000, 6000, 8000, 20,000, PVP K12, K17 and K30, poloxamer 188, 388 and 407, HPMC E5, Na-CMC, polysorbate 20 and 80, vitamin E-TPGS, phospholipid, DOSS and SDS) in different concentrations. Independently of the measuring method, an increase in osmolality with increasing concentration was observed for all polymers and surfactants, as would be expected due to the physicochemical origin of the osmolality. No correlation was found between the molecular weight of the polymers and the measured osmolality. The osmolality values were different for PVPs, PEGs, and Na-CMC using the two different measurement methods. The values obtained by the freezing point depression method tended to be similar or higher than the ones provided by vapor pressure, overall showing a significant difference in the osmolality measured by the two investigated methods. For lower osmolality values (e.g. surfactants), the choice of the measuring method was not critical, both the freezing point depression and vapor pressure could be used. However, when the formulations contained higher concentrations of excipients and/or thermosensitive excipients, the data suggests that the vapor pressure method would be more suited.

Aceclofenac-Loaded Microspheres Prepared by Vesicular Ionotropic Gelation to Minimize Drug-induced Gastric Ulcers in Rats.

Aceclofenac is a non-steroidal anti-inflammatory drug and a potent analgesic. However, its oral ingestion may cause gastrointestinal problems, including dyspepsia, abnormal pain, nausea, diarrhea, and ulcerative colitis. This study aimed to prepare vesicular-based enteric microspheres containing aceclofenac by ionotropic gelation technique to minimize gastric irritation in rats. The micron-size vesicles were prepared by the ionic-orifice gelation method. Three types of vesicularbased microcapsules containing aceclofenac were prepared by employing sodium alginate as the coating material in combination with Eudragit L100, Eudragit S100, and polyvinylpyrrolidone PVP K90. The drug to sodium alginate to polymer ratios were 1:0.5:0.5, 1:1:1, and 1:1.5:1.5, respectively. Gelation of sodium alginate was induced by the dropwise addition of calcium chloride solution (10 % w/v). Aceclofenac-loaded microspheres were evaluated in terms of aceclofenac content and in vitro drug release, and FTIR, DSC, and XRD were used for physicochemical evaluation of some selected formulae. The effects of microencapsulation on aceclofenac-induced ulcerative activity in male Wistar rats were also investigated. The results indicated no interaction between aceclofenac and microcapsules forming polymers. In addition, microcapsules formulations M1, M4, and M7 gave maximal protection in acidic pH and optimal release in alkaline pH. The histopathological studies revealed that the reduction of ulceration is evident from the macroscopic and microscopic studies, which showed complete protection of the tissue morphology with no ulcers, indicating the effectiveness of the microcapsules system against aceclofenac-induced gastric ulceration in rats again. Ionotropic gelation seems to be a simple, efficient technique to prepare aceclofenac-loaded microspheres with a reduced risk of gastric ulceration. It is possible to overcome the problem of gastric damage while utilizing aceclofenac by avoiding the exposure of the drug to the ulcer-prone area of the gastrointestinal tract.

Influence of dispersing solvent on curcumin dissolution from solid dispersions prepared using hydroxypropyl methylcellulose-polyvinylpyrrolidone K30

Background: Preparation of lipophilic compounds into solid dispersion formulations (SDs) has been credited with increasing their dissolution rate. Understanding the role of the dispersing solvent is crucial to the SDs preparation. Drug/carrier-solvent immiscibility may decrease the dissolution rate. Aim: This work aimed to study the effect of different dispersing solvents on a curcumin dissolution. Method: A solvent evaporation method was used in the SD preparation. The formulation was prepared at 30% w/w drug load contained Curcuma longa and a carrier mixture of Hydroxy Propyl Methylcellulose (HPMC)/ Polyvinylpyrrolidone K30 (PVP K30). As for the dispersing solvent, the study used ethanol, ethyl acetate, and ethanol/ethyl acetate solvent mixture. The dissolution profile was obtained and analysed for the dissolution-efficiency (DE). Result: The DE values of 38.5%, 37.8%, and 32.0% were obtained using ethanol, ethyl acetate, and ethanol-ethyl acetate mixture. Conclusion: The results show that there is a significant impact of using different SD solvents on curcumin dissolution.

Mechanisms of synergistic inhibition of hydrophilic amino acids with kinetic inhibitors on hydrate formation

The effects of hydrophilic amino acids on hydrate formation are a global hot spot of research, and yet the mechanisms behind such effects need to be further investigated. The mechanism of synergism between hydrophilic amino acids and hydrate kinetic inhibitors has not been clarified. Given the aforementioned, this research analyzes the effects of L-arginine, glycine, and their combination with PVP K90 and VC-713 on the formation of tetrahydrofuran (THF) hydrates, and manages to systematically reveal the relevant mechanisms by integrating various experimental methods. It is shown that L-arginine and glycine can disturb water molecules and reduce their activity, and thus they present both kinetic and thermodynamic inhibition effects. The combinations of 0.5 wt%–5.0 wt% L-arginine and glycine with 0.5 wt%–1.0 wt% kinetic inhibitors are found with synergistic inhibition effects on hydrate formation, and the combination of 4.0 wt% glycine with 1.0 wt% VC-713 is associated with the best synergistic inhibition performance.

Preparation and evaluation of matrix type of transdermal patches containing anti –diabetic drug

The current research aims to formulate and evaluated medicated transdermal patches containing an anti-diabetic drug. A good penetration enhancer would improve drug delivery from various polymer-based transdermal patches. Transdermal patches of the matrix type are made. Using various PVP K30, MC ratios and solvent evaporation techniques. All prepared formulations were tested for weight variation, thickness, drug content, moisture content, moisture uptake, flatness, and in vitro drug release. Bath F3 was optimised formula from all formulation baths shows linear zero order release for 24 hours, with a cumulative percentage of drug diffusion of 87.35% from 4cm2 patches. It has been determined that polymer concentration. When the concentration of PVP K30 increases in the primary layer, the in – vitro diffusion rate increases, and when the concentration of PVP K30 decreases, the drug diffusion decreases. It allows for more controlled drug release from the patch.

Vardenafil Oral Dispersible Films (ODFs) with Advanced Dissolution, Palatability, and Bioavailability

Oral, quick response, and on demand, also known as a spontaneous oral treatment for erectile dysfunction, is highly needed by both patients and physicians. Vardenafil is selective (fewer side effects) and more effective in difficult-to-treat conditions than sildenafil. This study aims at fostering the dual objectives of using biomolecules such as artificial sweetening agents to solubilize and mask the bitterness of vardenafil loaded on biodegradable polymeric materials (PVA, MC, SA, and PVP K30) to fabricate oral, fast-dissolving films (vardenafil ODFs) in the mouth without the need for water to ingest the dosage form. Furthermore, coprecipitated-dispersed mixtures of vardenafil and three sweeteners (sorbitol, acesulfame K, and sucralose) were prepared and characterized using FTIR, DSC, and solubility studies. Moreover, eight different vardenafil ODFs were prepared using the solvent-casting method. Modified gustatory sensation test, in vitro disintegration, and release studies were performed. In addition, the optimized ODF (F8) was compared with the commercial film-coated tablets pharmacokinetically (relative bioavailability, onset, and duration of actions were estimated). The results indicated that the three sweetening agents had comparable solubilizing capacity. However, both sucralose- and acesulfame K-based ODFs have a more enhanced sweet and palatable taste than sorbitol-sweetened ODF. The SA- and PVP K30-based ODFs showed significantly faster disintegration times and release rates than MC. In conclusion, PVA has good film-forming properties, but a higher ratio of PVA adversely affected the disintegration and release characteristics. The % relative bioavailability for ODF was 126.5%, with a superior absorption rate constant (Ka) of 1.2-fold. The Cmax and estimated Tmax were compared to conventional film-coated tablets.

Lower coordination Co3O4 mesoporous hierarchical microspheres for comprehensive sensitization of triethylamine vapor sensor

Monitoring and detecting triethylamine (TEA) vapor are essential in the organic synthesis industry. Two-dimensional Co3O4 nanosheets with large surface areas and multiple active sites are ideal for fabricating chemiresistive gas sensors. However, the face-to-face stacking owing to the high surface energy of nanosheets, would cover up the active sites, obstruct gas diffusion, raise contact resistance, which all hinder its utilization for TEA detection. Herein, the Co3O4 mesoporous nanosheets were assembled into hierarchical microspheres by adding the structure-directing agent PVP K30 and combined with a proper annealing temperature, which optimized their grain size, specific surface area, pores structure, oxygen vacancies, and the atomic ratio of Co2+ to Co3+. And these ultimately improved the detection capability of TEA. The sensor based on Co3O4 sphere-300 exhibits the highest sensor response of 34.1–100 ppm TEA and a low detection limit (0.5 ppm) at a low working temperature of 150 °C. The promising properties are mainly due to the combination of several advantages that facilitate simultaneous chemical and electronic sensitization. This work prepared a high-performance TEA gas sensor and verified the improvement of comprehensive sensitization on the gas-sensing performance of two-dimensional metal oxide semiconductors.

Formulasi dan Evaluasi Tablet Effervescent dari Ekstrak Buah Tampoi (Baccaurea macrocarpa)

Tampoi is one of the many plants found in East Kalimantan, has secondary metabolic content in the form of saponins, flavonoids, and alkaloids, and has antioxidant activity. The antioxidants produced by the human body are not sufficient to fight free radicals, therefore the body requires the intake of antioxidants from the outside, so to help increase public interest in consumption, researchers are interested in making preparations in the form of extracts and formulated as effervescent tablets from tampoi fruit extract which are useful as antioxidants and increase immunity. The purpose of this study was to determine a good formula for making effervescent tablets from tampoi fruit extract with variations of PVP K30 as a binder. Making tablets using direct compression method with an evaluation of effervescent powder including the angle of repose test, flow rate, setting, compressibility, and moisture of the powder. Evaluation of effervescent tablets included organoleptic test, weight uniformity test, tablet friability test, tablet hardness test, and tablet dissolving time test. The results obtained in the evaluation of the effervescent powder, the angle of repose test has met the requirements, while the test for flow velocity, sizing, compressibility, and moisture of the powder has not met the requirements. The results of the physical evaluation of the tablet weight uniformity test on F1 and F2 were in accordance with the requirements, the tablet friability test on F3 and F4 had met the requirements, the F3 tablet hardness test had met the requirements, and the tablet dissolving time test resulted that all formulas met the requirements with the best formula namely F1 which has the fastest tablet dissolution time. The conclusion of the study from the evaluation of the dissolving time which is the main parameter of the effervescent tablet preparation of tampoi fruit extract, the best formula was obtained, namely F1 with a PVP K30 concentration of 0.5 mg resulting in a tablet dissolving time of 01.99 minutes.

Forced Solid-State Oxidation Studies of Nifedipine-PVP Amorphous Solid Dispersion.

In the present study, the oxidative degradation behavior of nifedipine (NIF) in amorphous solid dispersions (ASDs) prepared with poly(vinyl pyrrolidone) (PVP) with a short (K30) and a long (K90) chain length was investigated. The ASDs were prepared via dry ball-milling and analyzed using Fourier transform infrared (IR) spectroscopy, X-ray scattering, and differential scanning calorimetry. The ASDs were exposed to accelerated thermal-oxidative conditions using a pressurized oxygen headspace (120 °C for 1 day) and high temperatures at atmospheric pressure (60-120 °C for a period of 42 days). Additionally, solution-state oxidative degradation studies showed that pure NIF degrades to a greater extent than in the presence of PVP. Electronic structure calculations were performed to understand the impact of drug-polymer intermolecular interactions on the autoxidation of drugs. While no drug degradation was observed in freshly prepared ASD samples, alkyl free radicals were detected via electron paramagnetic resonance (EPR) spectroscopy. The free radicals were found to be consumed to a greater extent by PVP K30- than PVP K90-based ASDs upon exposure to high oxygen pressures. This was consistent with the greater solid-state oxidative degradation of NIF observed in ASDs with PVP K30 than with PVP K90. As no drug recrystallization occurred during this study period, the lower glass-transition temperature and presumed greater molecular mobility of PVP K30 and its ASD as compared to the PVP K90 system appear to contribute to the greater drug degradation in PVP-K30-based ASDs. The extent and the rate of oxidative degradation were higher in the case of PVP-K30-based ASD as compared to that in PVP-K90-based ASD, and the overall degradation increased with an increase in temperature. IR spectral analysis of drug-polymer interactions supports the electronic calculations of the oxidation process. We infer that, apart from the initial free radical content, the difference in the extent of drug-polymer intermolecular interactions in ASDs and amorphous stabilization during the forced oxidation experiments contribute to the observed differences in the autoxidative reactivity of the drug in ASDs with different PVP chain lengths. Overall, the chemical degradation of NIF in ASDs with two PVP chain lengths obtained from accelerated solid-state oxidation studies was in qualitative agreement with that obtained from long-term (3 years) storage under ambient conditions. The study highlights the ability of accelerated processes to determine the oxidative degradation behavior of polymeric ASDs and suggests that the polymer chain length could factor into chemical as well as physical stability considerations.

Silica nanofluid in low salinity seawater containing surfactant and polymer: Oil recovery efficiency, wettability alteration and adsorption studies

Production of crude oil from a matured oil reservoir is challenging due to the low recovery factor. Hybrid methods have demonstrated potential in oil recovery from the matured crude oil reservoir. In recent years, the low salinity water with chemicals (viz., surfactant, polymer) and nanoparticles have brought the attention of the researchers due to their ability in altering the interfacial properties of the rock-oil-water systems favorable for crude oil recovery. The current interest by industries in injection fluid (i.e., low salinity water injection) has prompted the invention of a hybrid oil recovery agent for matured crude oil reservoirs. In the current study, a novel silica-based hybrid nanofluids (NFs) of variable silica nanoparticles (NPs) concentration in low salinity seawater with anionic surfactant (AOT: dioctyl sodium sulfosuccinate) and polymer (PVP–K30: polyvinylpyrrolidone) (sometimes referred to as SMART LowSal) are used as an injection fluid in a sand-pack reactor. Oil recovery from oil saturated sand-pack reactor is observed to enhance due to NFs (hybrid) injection after secondary recovery. The characteristic study of relative permeability curves discloses that sand surface was initially water-wet and converted to strongly water-wet in the presence of NFs. A nuclear magnetic resonance (1H NMR) study reveals that adsorption of the chemical appeared on the sand surfaces, which could be the reason for wettability alteration, and thereby enhanced oil recovery. Similarly, the scanning electron microscopy (SEM) and energy dispersive X-ray analysis (EDXA) of the sand samples before and after injection disclosed desorption of hydrocarbon from the sand surfaces after NFs injection. An additional 5–10% oil recovery is achieved after chemical flooding due to the injection of NFs. Adsorption isotherm study well agreed with the monolayer adsorption of surfactant on the sand surface.

Development of starch/chitosan expandable films as a gastroretentive carrier for ginger extract-loaded solid dispersion

Gastroretentive expandable films were developed to provide controlled release of ginger extract (GE) for treatment of gastric diseases. The dosage form consisted of ginger extract solid dispersion (GE-SD) loaded in a starch/chitosan composite film, which was subsequently folded and inserted into a hard gelatin capsule. GE-SD was prepared by solvent evaporation using an optimum weight ratio of 1:1 for GE and PVP K30. Expandable films containing GE-SD were prepared by solvent casting combinations of chitosan and either rice-, glutinous rice - or pregelatinized maize starch with glycerin incorporated as a plasticizer. The optimized film formulation prepared from glutinous rice starch, exhibited tensile strength of 5.4 N/cm2 and high expansion in simulated gastric fluid (SGF), resulting in a 2.8-fold increase in area. The films resulted in sustained release of up to 90% of the content of 6-gingerol during 8 h exposure to SGF. Furthermore, the 6-gingerol released from the film displayed dose-dependent cytotoxic activity against AGS human gastric adenocarcinoma cells and anti-inflammatory activity by inhibiting the production of nitric oxide (NO) in LPS-stimulatedRAW264.7cells.

Optimization and Quest of HPMC loaded Stavudine Controlled Release Dosage Development by Central Composite Design utilizing Reduced Factorial Screening Technique

The current research focused on screening and finding the significant independent variables in stavudine loaded tablet, followed by optimizing the best formulation using central composite design. The objective of the study to develop stavudine loaded controlled release tablet utilizing reduced factorial design, followed by optimization technique as well as characterization of prepared tablets. Preliminary trial batches were prepared using different grades of hydroxypropyl methylcellulose. The resolution-IV reduced factorial design was selected to screen the significant independent variables in the dosage form design. A total number of eight runs were prepared and responses were recorded. The signified factors identified by half-normal and Pareto chart. The prepared tablets are evaluated for various physiochemical characterizations. Three dependent responses such as hardness, dissolution at 6 hour and 12 hours are considered in optimization process. Later on, drug-polymer interaction study was carried out. The principal of the study design based on finding the best formulation with prefixed set parameter values utilizing the concept of screening technique. It observed that HPMC K15M (57.18 %), HPMC K100 (66.32 %) and PVP K30 (7.97 %) as best composition in a formulation batch would fulfill the predetermined parameter with specific values.

3D štampa i karakterizacija nosača za dostavu ibuprofena u koštanom tkivu

In this work, a blend of gelatin A (GA) and polyvinylpyrrolidone (PVP K30) was used for semi-solid 3D printing of bone scaffold for ibuprofen (IBU) delivery. The cross-linking of the obtained scaffold was performed with a 1% glutaraldehyde (GTA) solution, followed by lyophilization. The thermal and mechanical properties, as well as drug release profiles, and drug kinetics of prepared scaffolds were investigated. The cross-linked and lyophilized scaffold has shown good thermal stability, mechanical properties, and prolonged release of IBU following the Fickian diffusion process.

Effect of Spray Drying Method on the Properties of Glimepiride-loaded Solid Dispersion

Glimepiride (GLI) is a third-generation sulfonylurea class antidiabetic drug that has low aqueous solubility. The objective of this study was to evaluate the effect of solvents in the development of GLI-loaded solid dispersions (GLISD) using spray drying technique. Two GLI-SD were prepared by adding GLI, polyvinylpyrrolidone (PVP K30), and sodium lauryl sulfate (SLS) in an ethanol/water mixture (solvent evaporation, SE) and water only (surface attached, SA). Intrinsic saturated solubilities and in-vitro dissolution were evaluated and compared to the GLI powder and physical mixture (PM). In addition, physicochemical studies such as scanning electron microscopy, differential scanning calorimetry, and X-ray diffraction were also evaluated. We found that the solubility of GLI was significantly improved by both the preparation methods. The SE method showed 4,960-fold improvement while the SA method displayed 2,900-fold enhancement, which is equivalent to the PM. The in-vitro dissolution studies showed that both methods had a higher release rate, about 1.3-fold for SE and 2-fold for SA, as compared to pure GLI powder. However, GLI release slightly decreased with time for the SA method. Furthermore, solid-state characterizations also revealed that most of the crystalline drug was transformed to the amorphous form in both GLI-SD. Thus, these results indicate that choice of the solvent system plays an important role in the spray drying technique which affects the solubility, dissolution, and crystallinity of poorly soluble drugs such as GLI.