Form Of Solid Dispersion Research Articles

Simultaneous Delivery of Curcumin and Resveratrol via In Situ Gelling, Raft-Forming, Gastroretentive Formulations.

Curcumin and resveratrol are polyphenolic compounds that have been shown to exhibit synergistic therapeutic properties including anti-inflammatory, anticancer, and antiulcer activities, which may be exploited for the treatment of gastric diseases. However, both compounds have poor aqueous solubility and rapid metabolism, resulting in a low oral bioavailability. In situ gelling, liquid formulations were developed to produce a gastroretentive, raft-forming delivery vehicle to improve bioavailability. Solid dispersions containing a mixture of curcumin and resveratrol with Eudragit® EPO (Cur/Res-SD) were first prepared using solvent evaporation, to improve the solubility and dissolution of the compounds. Solid dispersions of a weight ratio of 1:10 curcumin/resveratrol to Eudragit® EPO were subsequently incorporated into in situ gelling, liquid formulations based on the gelling polymers, sodium alginate (low viscosity and medium viscosity), pectin, and gellan gum, respectively. Calcium carbonate and sodium bicarbonate were included to produce carbon dioxide bubbles in the gel matrix, on exposure to gastric fluid, and to achieve flotation. Moreover, the calcium ions acted as a crosslinking agent for the hydrogels. Optimized formulations floated rapidly (<60 s) in simulated gastric fluid (pH = 1.2) and remained buoyant, resulting in the gradual release of more than 80% of the curcumin and resveratrol content within 8 h. The optimized formulation based on medium-viscosity sodium alginate exhibited enhanced cytotoxic activity toward human gastric adenocarcinoma cell lines (AGS), compared with unformulated curcumin and resveratrol compounds, and increased anti-inflammatory activity against RAW 264.7 macrophage cells compared with the NSAID, indomethacin. These findings demonstrate that in situ gelling, liquid formulations, loaded with a combination of curcumin and resveratrol in the form of solid dispersions, show potential as gastroretentive delivery systems for local and systemic effects.

Sertaconazole-PLGA nanoparticles for management of ocular keratitis

Ocular fungal infections can pose severe health conditions that may develop into vision impairment and blindness. Sertaconazole (STZ) is a widely used antifungal; however, its low aqueous solubility restricts its topical application for managing ocular keratitis. This investigation aimed to develop polymeric nanoparticles as delivery carriers to improve the ophthalmic availability of STZ for treating fungal keratitis. The impact of STZ solid dispersion incorporation within polymeric nanoparticles for in vitro drug release enhancement was also evaluated. STZ-laden PLGA NPs were formulated via nanoprecipitation technology, using a 24-full factorial layout to optimize the formulation. The formed nanoparticles were assessed for encapsulation efficiency percentage, hydrodynamic size, surface charge, and polydispersity index. The selected formula exhibited a particle size of 305.9 ± 4.36 nm, an entrapment efficiency (EE%) of 98.8 ± 0.008%, a surface charge of 22.57 ± 0.23 mV, and a low polydispersity index, indicating a uniform size distribution. Incorporating STZ in a solid dispersion form with PEG 2000 at a 1:3 w/w drug-to-carrier ratio increased the hydrodynamic size of the PLGA NPs. However, no significant variation in the entrapment efficiency percentage was recorded. The developed STZ-solid dispersion-loaded PLGA NPs have round-shaped structures. DSC and FTIR spectroscopy data indicated drug amorphization with successful loading within the PLGA matrix. Introducing the drug as a solid dispersion within PLGA NPs resulted in enhancing the rate of drug dissolution at initial time intervals, followed by a controlled drug release over 24 h. STZ-PEG2000-laden PLGA NPs enhanced permeability through rabbits’ corneas (Papp), 2.5-fold higher versus STZ-loaded PLGA NPs. The antimycotic activity of the developed formulation was tested against Candida albicans, and a 4-fold reduction in the MIC value was detected upon applying the nanoparticles’ formulation embedding STZ solid dispersion versus that containing the free drug. In conclusion, the formulation of solid dispersions of STZ loaded in PLGA nanoparticles may serve as a starting point for an efficient approach to the ocular delivery of hydrophobic medications and a viable setup for the upcoming research in animal models of fungal keratitis.

Polymeric microparticles in solid dispersion form containing the hormone triiodothyronine (T3) for treatment of hypothyroidism: development, synthesis and physical-chemical and morphological characterization

O hipotiroidismo é uma doença metabólica comum, a qual se apresenta por baixa concentração de hormônio tireoidiano por síntese deficitária e/ou baixa sensibilidade aos hormônios pelos seus receptores, sendo seu tratamento normalmente feito com reposição hormonal a partir de monoterapia de Levotiroxina (L-T4), fármaco originado da molécula sintética de tiroxina que apresenta ação de pró-hormônio. O hormônio ativo para a glândula tireoide é a triiodotironina (T3), porém não é muito usado devido sua rápida degradação no organismo. Devido a isso, esse trabalho teve como objetivo desenvolver uma dispersão sólida com T3, sendo essa proposta baseada no esperado aumento de estabilidade, efeito terapêutico e, consequentemente, a meia-vida do fármaco através da microtecnologia. A dispersão sólida foi sintetizada com PEG 6000 e polissorbato 80 e elaborada a partir do método de evaporação do solvente. Em seguida, foi parcialmente caracterizada físico-quimicamente e morfologicamente através de métodos analíticos como termogravimetria (TG), calorimetria exploratória diferencial (DSC), espectroscopia de absorção no infravermelho (IR), bem como por através da microscopia eletrônica de varredura (MEV), sendo que tais análises indicaram a formação de um sistema eficaz e inovador para a liberação de fármacos.

Combined Triazole Disinfectants and Their Influence on the Growth and Development of Spring Wheat Seedlings

Seed treatment with fungicides is a crucial link in the plant protection system, and systemic drugs give the best effect. Therefore, it is very important to develop scientific foundations for the preparation of complex preparations with a low rate of consumption of the active substance and the inclusion of plant growth regulators that enhance growth processes and the yield of the main crop. In recent years, the directions of modification of known and practiced fungicides by various methods, including methods of mechanochemistry, have been promising. The problem of creating both new substances and their effective formulations remains urgent. Taking into account the prospects and high efficiency of triazole fungicides in the system of complex plant protection, the creation of multicomponent seed protectants of grain crops is proposed. The purpose of this study was to develop preparations based on tebuconazole (TBC) and propiconazole (PPC) in the form of solid dispersions (SD) and to study their biological activity on spring wheat plants in the conditions of the Trans-Urals. At the same time, the retardant effect of these triazoles was also studied with the help of the domestic growth regulator Floroxan. The use of new preparations on spring wheat made it possible to reduce the damage to the culture by root rot by 85–87%, productive bushiness increased by 6–11% compared to the control without treatment. A reliable increase in crop yield of 2.2 c/ha or 14% was obtained using preparation 2 (TD of the composition TBC : PPC : AG : silica = 1 : 1 : 7 : 1 + Phloroxane when the polysaccharide (AG) and the auxiliary substance of silica are included in the composition). The inclusion of the growth regulator Floroxan in the composition of the mordant mixture reduced the antioxidant effect of tebuconazole and stimulated the growth and development of wheat seedlings. It was proved that such a biological effect was achieved in conditions of drought of varying intensity during the growing season of 2021–2022.

ИССЛЕДОВАНИЕ ФАРМАКОКИНЕТИКИ ТВЕРДОДИСПЕРСНОЙ И КРИСТАЛЛИЧЕСКОЙ ФОРМ АНТИВИРУЛЕНТНОГО СРЕДСТВА ФТОРТИАЗИНОН У КРЫС

Prevalent drug resistance of pathogenic bacteria is a major concern for healthcare. Decreased bacterial susceptibility to antibiotics reduces treatment efficiency, putting lives of patients at risk. To overcome this issue, a novel anti-virulence drug Fluorothiazinon (FT) was developed. The drug inhibits type three secretion system and flagella motility of many Gram-negative bacteria. It showed therapeutic activity against a number of pathogenic microorganisms, such as Pseudomonas aeruginosa, Acinetobacter baumannii, Chlamydia trachomatis and Salmonella enterica Typhimurium among others. To find appropriate form for subsequent drug development solid dispersion and crystalline forms of FT were manufactured. In this study we aimed to investigate pharmacokinetics of FT in two forms to find the formulation with higher bioavailability. For comparative pharmacokinetics study rats were allocated to receive a single oral dose 50 mg/kg of the drug in either solid dispersion or crystalline forms. Determination of FT and its metabolite was carried out by high-performance liquid chromatography – tandem mass-spectrometry analysis. Our results show that the solid dispersion form of Fluorothiazinon has a higher oral bioavailability of 235.4% compared to the crystalline form in rats. Therefore, solid dispersion form was demonstrated to be more suitable for dug development to have enhanced bioavailability, leading to increased absorption and possible improved therapeutic potential of the developed drug based on pharmacokinetics data.

Improving the Dissolution rate of Mefenamic acid by preparing Solid Dispersions with Polyethylene glycol 4000

The low solubility of drugs is the main reason for the decrease in bioavailability and, consequently, the therapeutic effect. Solid dispersions prepared using water-soluble polymers are a promising approach to solving this problem while maintaining the hydrophobic nature of the drug and reducing the dose load. The aim of this study was to enhance the solubility and the dissolution rate of mefenamic acid by formulating it in the form of solid dispersions. The solid dispersions were prepared by kneading method using polyethylene glycol 4000 as a carrier in various proportions. The dissolution test was performed for two hours in phosphate buffer (pH=8) and the drug release kinetics were studied using several mathematical models. The results showed that polyethylene glycol enhanced the dissolution rate of mefenamic acid in prepared formulations, and the higher the ratio (carrier: drug), the faster the drug dissolved. The best fit to the kinetic model was observed with the Higuchi and Ritger-Peppas models, indicating drug release via Fickian diffusion.

Generation of cellulose from Saccharum officinarum pseudostem bagasse and its application as solubility enhancer in albendazole solid formulation

Formulations of poorly aqueous soluble drugs in different polymers based on solid dispersion method have been used to improve its solubility and drug bioavailability. The aim of this study was to formulate albendazole solid dispersion utilising cellulose obtained from saccharum officinarum pseudostem bagasse and characterised. Herein, a 32 factorial design was used to factor out 9 combinations of the generated cellulose (GC) and lactose. In each case, the combination was blended with albendazole, processed using solvent-evaporation technique and adjuvant into a solid dispersion form (SD). The SD was granulated with starch and lubricated with magnesium stearate. Thermal analysis based on differential scanning calorimetry (DSC) and Fourier transmission infrared spectrophotometer (FT-IR) were carried out on the cellulose, drug and the granules. The micromeritic properties of the granules, and drug entrapment efficacy and dispersion-number of aqueous constitution of the granules were determined. The DSC result showed amorphous GC and granules. FT-IR analysis showed no compatibility or interaction problem based on the functional peaks observed. The granules exhibited micromeritics properties (p &gt; 0.05); rate of consolidation &lt; 0.43 and Carr’s indices &lt; 23.53, drug entrapment efficacy &gt; 93 % and dispersion-number &lt; 4.33. The granules dissolution rates after 10 and 60 mins were &gt; 94.11 % and &gt; 68.52 % respectively. These granules properties peaked with the GC and lactose combination at 20 % each. Albendazole formulation based on the cellulose obtained from sugarcane showed a promised alternative for improved dissolution and possible bioavailability enhancement.

IMPROVEMENT OF DISSOLUTION RATE OF REPAGLINIDE BY UTILIZING SOLID DISPERSION TECHNIQUE

The recent study's objective was to prepare and evaluate the Repaglinide (RG) solid dispersion. RG is poorly water soluble, BCS class II drug. Repaglinide solid dispersion (RG-SD) was prepared by solvent evaporation method using different proportion of PVP K30. The prepared RG-SD was evaluated for solubility studies, drug content, in vitro dissolution, DSC studies and XRD studies. DSC and XRD studies results indicate that RG exists in amorphous form in solid dispersion. The solubility of pure RG was enhanced from 34.41±0.68 to 370.3±1.52 μg/mL in distilled water at 370 C. RG-SD (RG:PVP K30) (1:10) showed high burst release (65%) in the first 30 min. Current research concludes that Repaglinide solid dispersions using PVP-K30 (1:10) as a carrier in solid dispersions showed promising results in enhancement of repaglinide properties. KEYWORDS: Repaglinide, Solid Dispersion, PVK K30, Dissolution Rate, Solvent evaporation

Interaction of polymers with bile salts – Impact on solubilisation and absorption of poorly water-soluble drugs

Formulating poorly soluble drugs with polymers in the form of solid dispersions has been widely used for improving drug dissolution. Endogenous surface-active species present in the gut, such as bile salts, lecithin and other phospholipids, have been shown to play a key role in facilitating lipids and poorly soluble drugs solubilisation in the gut. In this study, we examined the possible occurrence of interactions between a model bile salt, sodium taurocholate (NaTC), and model spray dried solid dispersions comprising piroxicam and Hydroxypropyl Methylcellulose (HPMC), a commonly used hydrophilic polymer for solid dispersion preparation. Solubility measurements revealed the good solubilisation effect of NaTC on the crystalline drug, which was enhanced by the addition of HPMC, and further boosted by the drug formulation into solid dispersion. The colloidal behaviour of the solid dispersions upon dissolution in biorelevant media, with and without NaTC, revealed the formation of NaTC-HPMC complexes and other mixed colloidal species. Cellular level drug absorption studies obtained using Caco-2 monolayers confirmed that the combination of drug being delivered by solid dispersion and the presence of bile salt and lecithin significantly contributed to the improved drug absorption. Together with the role of NaTC-HPMC complexes in assisting the drug solubilisation, our results also highlight the complex interplay between bile salts, excipients and drug absorption.

Effects of water-soluble curcuminoid-rich extract in a solid dispersion form (CRE-SD) on the sperm characteristics, longevity and casein kinase II catalytic subunit alpha protein stability in chilled goat semen

The present study evaluated the effects of water-soluble curcuminoid-rich extract in a solid dispersion form (CRE-SD) on goat sperm qualities and sperm protein CSNK2A2 expression during liquid storage. Semen was collected from five fertile goats, using an artificial vagina. Ejaculates with a motility above 70% were cooled to 4 °C using TRIS-citric acid-fructose diluent with 10% egg yolk containing various concentrations of CRE-SD (0, 0.1, 1, 10 and 100 μg/mL). Chilled sperm were evaluated for sperm characteristics, casein kinase II catalytic subunit alpha (CSNK2A2) protein level and oxidative status up to 15 days. After 12 days of preservation, sperm motility, viability, acrosomal integrity and mitochondrial activity were significantly higher in the group preserved with 10 μg/mL CRE-SD as compared with the control group. Supplementation of CRE-SD at this concentration was also able to conserve the CSNK2A2 a significantly higher than that in control group until 9 days of cold storage, possibly by reducing oxidative stress. The molecular mass of the sperm CSNK2A2 protein detected in this study was 37 kDa; it was mostly located in the post-acrosomal region, midpiece and flagellum. These results demonstrate the possibility to use the CRE-SD as a natural antioxidant during liquid semen storage in goats.

Effect of Hydrophilic Carriers for Solubility and Dissolution Enhancement of Sulfamerazine by Solid Dispersions Technique

Aims: The present research was carried out to investigate the effect of hydrophilic carriers in enhancing the solubility and dissolution rate of Sulfamerazine (SMZ) employing the fusion technique of solid dispersions (SD).&#x0D; Methodology: SMZ is an oral antibacterial drug exhibiting a poor dissolution profile and water solubility. SD of SMZ was prepared using poloxamer 407 (PX407) and Polyethylene glycol 6000 (PEG6000) as a hydrophilic carrier by employing the fusion technique.&#x0D; Results: The powder SDs were subjected for solubility, Fourier transform infrared spectrometry (FTIR), Differential scanning calorimetry (DSC), in-vitro dissolution profile, Scanning electron microscopy (SEM), and X-ray diffraction (XRD) study. The FTIR spectral analysis showed no significant incompatibility between drug and carriers and confirmed the presence of SMZ. From XRD and DSC, SMZ indicated the amorphous form in solid dispersion with larger specific surface area, resulting in a better in-vitro rate of dissolution of the drug from solid dispersions than pure drug. However, SD of PX407 (SDSMFF8) indicated higher aqueous solubility than pure SMZ. Further, SDSMFF7 showed higher in-vitro drug release 96.45±0.3% within 60 minutes, and pure drug (18.54±0.8%).&#x0D; Conclusion: In conclusion, enhancing thesolubility and dissolution of SMZ using hydrophilic carriers by solid dispersion technique provides new strategies for broadening its potential clinical application.

A Comprehensive report on Solid Dispersions by Factorial Design

The drugs of present use are lipophilic. Hence there is a need to surge the solubility of these drugs. To encounter this necessity one of the approaches is the formulation of drugs in form of Solid dispersions. Solid dispersions are a type of dispersion having one or extra one API in a torpid carrier at a solid state. We focused on the importance of solid dispersions in pharmaceutical formulation by using factorial design as it was easy to formulate. These solid dispersions are organized by several practises such as solvent technique, supercritical fluid technique and kneading tactic, etc., by referring the several journals, literature and pharmacy magazines we came to know that Solid dispersion are used to improve the solubility of the poor water-soluble drugs and also its bioavailability. At last, we conclude that through these Solid dispersions we can boost the Therapeutic efficiency of hydrophobic drugs by achieving greater solubility.

Enhancing therapeutic potential of poor aqueous soluble herbal drugs through solid dispersion-An overview

BackgroundPoorly water-soluble medicaments continue to be a challenging, however, significant class of herbal drugs for the management of an extensive range of ailments. Solid dispersion (SD) has emerged as one of the most effective formulation approaches to enhance the dissolution of poorly water-soluble herbal drugs. Formulation of solid dispersion is one of the most effective methods to enhance the aqueous solubility of highly lipophilic drugs which belong to BCS class II and IV. An amorphous form of the drug is more unstable and highly soluble in water and is attained by formulating solid dispersion. PurposeThis review explains various physicochemical properties, criteria for carrier selection, and causes of instability of solid dispersion to improve the therapeutic potential of poorly water-soluble herbal drugs. MethodologyTo classify and explain some newer techniques used nowadays along with solid dispersion which could prevent recrystallization and precipitation of drug. Some herbal drugs with high therapeutic value and poor aqueous solubility were also enlisted which could be formulated in the form of solid dispersion to have better oral bioavailability. ResultsThe solid dispersions studies have revealed better performance for the dissolution which might be due to its alteration from crystalline to amorphous form in addition to the adherence of hydrophilic carriers to the surface of poorly water-soluble herbal drugs. These techniques will assist in the formation of a more stable solid dispersion. ConclusionThe application of solid dispersion technique in enhancing the aqueous solubility of poorly aqueous soluble herbal drugs should direct to the constant and enhanced bioavailability, leading to an enhanced therapeutic potential.

High water-soluble curcuminoids-rich extract regulates osteogenic differentiation of MC3T3-E1 cells: Involvement of Wnt/β-catenin and BMP signaling pathway

ObjectiveThe present study aimed to evaluate the effect of a high water-soluble curcuminoids-rich extract (CRE) in a solid dispersion form (CRE-SD) using polyvinylpyrrolidone K30 on osteogenic induction of MC3T3-E1 cells. MethodsCRE was pre-purified using a microwave assisted extraction couple with a Diaion® HP-20 column chromatography. The osteoblastic cell proliferation and differentiation potentials of CRE-SD in MC3T3-E1 cells were tested by cell viability, alkaline phosphatase (ALP) activity, and Alizarin red S activity assays. The mRNA expressions of osteoblast-specific genes and underline mechanisms were assessed by a real time PCR and western blot analysis. ResultsCRE-SD 50 µg/mL increased alkaline phosphatase (ALP) activity, an early differentiation marker of osteoblasts in both MC3T3-E1 cells and non-osteogenic mouse pluripotent cell line, C3H10T1/2, indicating the action of CRE-SD was not cell-type specific. Alizarin red S activity showed a significant amount of calcium deposition in cells treated with CRE-SD. CRE-SD also upregulated the mRNA expression levels of transcription factors that favor osteoblast differentiation including Bmp-2, Runx2 and Collagen 1a, in a dose dependent manner. Western blot analysis revealed that noggin attenuated CRE-SD-promoted expressions of Bmp-2 and Runx2 proteins. siRNA mediated blocking of Wnt/β-catenin signaling pathway also annulled the influence of CRE-SD, indicating Wnt/β-catenin dependent activity. Inhibition of the different signaling pathways abolished the influence of CRE-SD on ALP activity, confirming that CRE-SD induced MC3T3-E1 cells into osteoblasts through Wnt/β-catenin and BMP signaling pathway. ConclusionThese results collectively demonstrate that CRE-SD may be a potential therapeutic agent for the treatment of osteoporosis.

Antibacterial Activity of Mucoadhesive Gastroretentive Drug Delivery System of Alginate Beads Containing Turmeric Extract - PVP Solid Dispersion.

BACKGROUND:Turmeric extract is less effective because the main ingredient of curcumin has a low solubility. Therefore, it is necessary to convert turmeric extract into a solid dispersion form to increase the dissolution of curcumin.AIM:To determine the antibacterial activity of mucoadhesive gastroretentive drug delivery system of alginate beads containing solid dispersion of turmeric extract.METHODS:Turmeric powder was macerated with 96% ethanol for 8 days. The macerate was evaporated with a rotary evaporator at 50°C to obtain concentrated extract. Solid dispersion of turmeric extract was prepared by solvent method by using polyvinylpyrrolidone (PVP) K30 with a ratio of 1: 1 and 1: 2. The solid dispersion of turmeric extract was encapsulated with alginate gel by gelation method. The antibacterial of alginate beads containing solid dispersion of turmeric extract was tested by using hole agar plate diffusion method against Staphylococcus aureus and Escherichia coli as bacterial models.RESULTS:The size of alginate beads containing turmeric extract-PVP solid dispersion was about 1.3 mm. Antibacterial activity test against Staphylococcus aureus and Escherichia coli showed that alginate beads containing turmeric extract-PVP solid dispersion gave stronger antibacterial activity than those containing turmeric extract without solid dispersion. The antibacterial activity of alginate beads turmeric extract-PVP (1: 2) solid dispersion was stronger than those containing turmeric-extract (1: 1) solid dispersion.CONCLUSION:Based on the results of this study it can be concluded that alginate beads containing turmeric extract-PVP solid dispersion gives the stronger antibacterial activity than those containing turmeric extract without solid dispersion.

THE EFFECT OF SOLID DISPERSIONS OF IVERMECTIN AND ALBENDAZOLE WHEN SHEEP EXPERIENCING NODULAR WORM DISEASE IN THE REPUBLIC OF ALTAI

The paper demonstrates the prospects of applying Arabinogalactan for mechanochemical modification of physicochemical and biological properties of antihelminthic substance. The study evaluates the parasitocidal effect of ivermectin (IVER) and albendazole (ABZ) compounds with Arabinogalactan (AG) in the form of solid dispersions (RD) in sheep intestinal helminthiasis. The authors tested compositions of new specimens with the active substance (DV) of ivermectin with three batches of arabinogalactan from different manufacturers in the ratio of 1:10 and compositions of IVER+ABZ+AG in the ratio of 1:1:10. The experiments on parasitocidal activity of compositions in intestinal helminthiasis were carried out on spontaneously invaded sheep in Shebala district of the Republic of Altai, where 16 experimental and 2 control groups of animals were arranged following the principle of analogues. The sheep received the specimens on an individual basis: as a water suspension orally; composition of IVER+AG dosed as 0,1; 0,05 and 0,025 mg per a kilo of animal weight; composition of IVER+ABZ+AG - in calculation of IVER+ABZ - 0,1 and 0,2 mg of water suspension, albendazole 1, 2, 3 and 5 mg per 1 kg of animal weight. The experiment has shown that parasitocidal activity of laboratory samples of mechanical compositions of ivermectin and different in degree of purification of AB lots do not differ significantly. It is supposed that parasitocidal compositions can be used for non-pharmacopoeia AG samples of animals, which will reduce significantly the cost of the specimen. The efficiency of the composition of IVER+AG dosed 0.1 mg per 1 kg of animal weight is significantly higher than that of the initial specimen. Mechanical composition IVER+ABZ+AH dosed 0.2 mg of hemectin and 2 mg of albendazole per a kilo of animal weight is highly effective (100%) against sheep intestinal helminths and it assumes the possibility of significant (five times) decrease of AHZ dose in the composition with AH without loss of helmintocidal activity.

In vivo Absorption Study of Solid Dispersion Containing Atorvastatin Calcium in Human Volunteers

Objectives: Solid dispersion is a unique and promising approach for improving the oral absorption and oral bioavailability of the poorly water soluble drugs. Atorvastatin Calcium (ATV) is an anti-hyper lipidemic agent, It belongs to class II drugs according to the biopharmaceutical classification system (BCS), and undergoes extensive first-pass metabolism after oral absorption exhibiting 12% bioavailability. The Objective of the present study is to investigate the effect of formulating the hydrophobic drug (ATV) in a solid dispersion form on its bioavailability. Methods: ATV solid dispersion (ATV-SD) was prepared by microwave induced fusion method, containing poloxamer188 as a hydrophillic carrier. The resultant ATV-SD was compressed into tablets with other ingredients and was evaluated against pure ATV tablets, in vitro dissolution study was carried out to compare the dissolution profiles of the prepared ATV-SD against the pure form of ATV. In vivo study was conducted using healthy male volunteers (n = 6). A high performance liquid chromatography method was employed to determine the level of drug in human plasma. Results: In vitro dissolution study revealed an enhancement in the dissolution profile of ATV-SD. The study of pharmacokinetics parameters also showed an enhancement after oral administration of ATV-SD tablet when compared with pure ATV tablets, where , the AUC0–60h and Cmax were increased after intake of ATV-SD tablets orally compared with that of pure ATV tablets. Conclusion: All these could be demonstrated that ATV-SD would be prospective means for enhancing higher oral bioavailability of ATV.

The preparation of Garcinia Glycosides solid dispersion and intestinal absorption by rat in situ single pass intestinal perfusion

Garcinia Glycosides is a candidate drug obtained by structural modification of Gambogic Acid (GA), which was acquired through High Throughput Screening(HTS). As Garcinia Glycosides is an effective but insoluble anti-tumor drug, the aim of this study was to obtain a solid dispersion form Garcinia Glycosides by using solvent-melt method so that improve the solubility and dissolution rate. The solid dispersion was characterized by High Performance Liquid Chromatography (HPLC), infrared spectroscopy and evaluated the intestinal absorption of the drug by rat in situ single pass intestinal perfusion. The results showed the increase of solubility, dissolution velocity and absorption compared to other forms. This indicated that solid dispersion could greatly improve the relative bioavailability of Garcinia Glycosides in vivo.

Incorporation With Dendrimer-Like Biopolymer Leads to Improved Soluble Amount and In Vitro Anticancer Efficacy of Paclitaxel

The aim of this study was to explore the solubilization efficacy of octenylsuccinate hydroxypropyl phytoglycogen (OHPP), an amphiphilic dendrimer-like biopolymer, in improving the soluble amount and efficacy of paclitaxel (PTX), a potent anticancer active pharmaceutical ingredient. PTX was incorporated with OHPP in the form of solid dispersion (PTX-OHPP SD), which was characterized for its PTX crystallinity, interactions between PTX and OHPP, PTX soluble amount and dissolution profile, and in vitro inhibitory efficacy against cancer cell lines. The incorporation with OHPP led to the amorphous state of PTX. FTIR spectra showed potential hydrogen bonding between PTX and OHPP, and hydrophobic interaction could play an important role in the association of PTX molecules with OHPP particulates. The soluble amount of PTX with PTX-OHPP SD was >14,000 times that of PTX alone. During dissolution, over 70% PTX dissolved in 5 min and this soluble amount was maintained for at least 180 min. With the 3 cancer cell lines tested, the PTX of PTX-OHPP SD showed a much lower IC50 than the dimethyl sulfoxide–assisted PTX solutions. Based on the result, the mechanism of using OHPP as a highly potent solubilizer for PTX was discussed.

Formulation and evaluation of thermoresponsive polymeric blend as a vaginal controlled delivery system

Thermoresponsive polymers have the ability to undergo rapid changes in response to subtle environmental conditions and make stimuli-responsive materials attractive. They are candidates for minimally invasive, targeted and personalized drug delivery applications. Curcumin (CUR) is a phytochemical compound characterized by its low intrinsic toxicity and a wide variety of therapeutic effects. The modulating of the viscoelastic properties and bioadhesive characteristics of the thermoresponsive hydrogel (poloxamer 407) was achieved using a ternary system formed with chitosan and hydroxypropylmethylcellulose K4M (M20). The curcumin in solid dispersion form (CUR-SD) was used in the hydrogel preparation. The physical–chemical, physiomechanical, oxidative stress properties and antioxidant activity were evaluated and compared. Curcumin in SD form is more soluble and stable than in the physical mixture (PM) or free form. The transition from liquid to gel (Tsol–gel) temperature of the M20-SD formulation occurred at 36 °C. The CUR delivery profiles followed the Hixson–Crowell’s model. The M20-SD formulation showed antioxidant activity and as a strong inhibitor of oxidative stress. Analysis of results suggests that CUR-SD thermoresponsive hydrogel can be used via to the vaginal route for the treatment of mucosal inflammation and infectious disease, including HPV. The elastomeric hydrogel is formed by covalently cross-linked long and flexible polymer chains aggregated with water. The analysis results showed that M20-SD could remain at the application site for a sufficient time to permit the controlled delivery and to improve the therapeutic activity of CUR.