Solid Dispersion Method Research Articles

Development and Characterization of Fast-Dissolving Tablets to Enhance Bioavailability of BCS Class II Drugs by Solid Dispersion Method

Background: Rapid tablet or capsule dissolution requires the tablet to disintegrate and dissolve at a higher rate, enhancing drug dissolution and bioavailability. Suitable disintegrants have shown an appreciable rate of disintegration or dissolution. Using factorial design for formulation to improve bioavailability is a key focus in pharmaceutical research to enhance dissolution Methods: Azelnidipine (Azp) tablets were formulated with Hydroxypropyl β-cyclodextrin (HβCD), β-cyclodextrin (βCD), and Kolliphor HS15 (HS15) to enhance solubility. A 23 factorial design optimized the formulation, focusing on disintegration time (DT) and time for 90% dissolution (T90). Eight formulations (F1-F8) were prepared using the kneading method. Tablets were evaluated for physical properties, drug content, friability, dissolution, and drugexcipient interactions (FTIR and DSC). The optimal formulation (F9) was determined via desirability analysis. Results: Tablets showed acceptable Carr's index (CI), Hausner ratio (HR), and Angle of Repose (AR). Increasing βCD concentration decreased DT, enhancing water absorption and faster dissolution. βCD tablets had the lowest DT among the formulations, with F4 showing the best disintegration. Higher HS15 concentration also reduced DT, with F8 achieving the highest drug release (T90%) within 60 minutes. R² values ranged from 0.922 to 0.994, indicating high predictability. The optimal formulation had a desirability of 1.0, consisting of 3.523 mg HS15, 28.4 mg βCD, and 1.49 mg βCD, with a DT of 102 ± 1.13 seconds and 98% dissolution. FTIR and DSC confirmed no drug–excipient interactions. Conclusion: Optimized super disintegrant concentrations and wet granulation techniques resulted in tablets with strong mechanical properties, rapid disintegration, and consistent drug content. Future research and in vivo studies should explore additional excipient combinations.

Solubility Enhancement of BCS Class II Antibiotic (Azithromycin) by Solid Dispersion Technique by Using Skimmed Milk

Azithromycin has a low water solubility; Hence, dissolution represents a rate-limiting process. The goal of the present investigation is to improve azithromycin dissolution and solubility rate. The purpose of this study was to create, characterize, and test the dissolving characteristics of an Azithromycin solid dispersion with skimmed milk. Formulated tablet of optimized batch compared with marketed formulation and study its drug release and make a formulation that gives the highest rate of solubility. This experiment was conducted utilizing the solid dispersion method. The rationale for solid dispersion is that it produces better results than other methods while costing less. Skimmed milk is used as a carrier to increase the solubility of azithromycin. Azithromycin purity is certified using assessment tests such as HPLC assay, UV spectroscopy, FTIR, and DSC. Azithromycin solid dispersion (Azithromycin in skimmed milk) SD2 consistently performs well in all physiochemical tests as compared to all batches. The designed tablet F2 batch releases the drug more effectively than the marketed one. Azithromycin’s solubility was successfully enhanced by utilizing the solid dispersion method with skimmed milk. Batch SD 2 gives the highest results in all parameters like solubility. Preformulation study, mainly in tablet formulation, also it gives the highest solubility.

Optimization of solid dispersion technique and gliclazide to carrier (PVP K30) ratio for solubility enhancement

Background and objective: Poorly water-soluble dugs provide less dissolution rate and bioavailability; hence, it minimizes the pharmacological effect of orally administered medications. Gliclazide is a sulfonylurea antidiabetic medication of the second generation, used to treat type II diabetes mellitus. It belongs to the class II drugs of biopharmaceutic classification system, indicating that it has high permeability and poor aqueous solubility. The aim of this study is to determine an optimum solid dispersion method and drug to carrier ratio to improve the solubility of gliclazide. Methods: Solid dispersions of gliclazide were formulated with polyvinyl pyrrolidone K30 using various drug to carrier ratios (1:1, 1:3, and 1:5) by utilizing kneading and solvent evaporation methods. Solubility and dissolution rate of solid dispersion formulas were compared with pure drug and co-ground mixtures. The formulations were further evaluated in terms of percentage of yield, drug content, FTIR, SEM, DSC, and XRD studies. Results: The highest solubility improvement of gliclazide was obtained at the ratio 1:5 of gliclazide and PVP K30 utilizing solvent evaporation method, solubility increased about 2.54 folds (98.299 ± 5.77 µg/ml) as compared to pure gliclazide (38.739 µg/ml). Meanwhile, the greatest improvement in gliclazide dissolution rate was observed in the same solid dispersion formula that was about 105.76 % after 30 minutes. FTIR demonstrated no unwanted interaction between the drug and carrier. While, SEM, DSC, and XRD showed crystallinity of the drug was minimized and converted to amorphous form in solid dispersion formula. Conclusion: Based on the investigations of this study, it can be concluded that the drug to carrier weight ratios and preparation methods had the influence on the drug solubility and the release rate. The obtained data revealed that the solvent evaporation is the best method of solid dispersion for enhancing gliclazide solubility using PVP K30 with the ratio 1:5 of the drug and carrier.

Solubility and Dissolution Rate Enhancement of Aceclofenac by Solid Dispersion Employing Kneading and Solvent Evaporation Techniques

Background: Aceclofenac (ACF) is a non-steroidal anti-inflammatory drug with potent anti-inflammatory and analgesic properties. ACF is belongs to BCS class II which has poor solubility in water (practically insoluble) and high permeability that leads to a low dissolution rate and reduced bioavailability. Objective: to enhance the solubility and dissolution rate of ACF using the solid dispersion method (SD) by two common techniques which were solvent evaporation (SE) and kneading (Kn) by using different carriers Mannitol, PVP k30, Soluplus®, and Urea in both techniques at 1:1 and 1:5 wight ratio. Methods: The effects of type of carrier and preparation method on solubility and dissolution rate of SD were studied. Solid dispersions were characterized for their, percentage yield, drug content, drug solubility and in-vitro dissolution rate in comparison with pure drug. Results: The best formula is obtained by the Kn formula (F16) which was formulated by the use of ACF: Soluplus®: with a weight ratio of 1:5 which gave a high percentage yield (99.5%), high drug content (99.8± 0.003%) and the best solubility enhancement which was 361 folds compared to pure ACF and faster dissolution rate which was 80% in 10 minutes compared to 20% for pure drug. Conclusion: the solubility and in-vitro dissolution rate of ACF was efficiently improved when prepared by SD techniques, utilizing both solvent evaporation and kneading methods. Furthermore, the kneading method was superior to solvent evaporation method due to the greater enhancement of solubility and dissolution rate obtained by all carriers and ratios with higher improvement by 1:5 ratio, and can be considered a successful and efficient strategy for solubility and in-vitro dissolution rate improvement of hydrophobic drugs.

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

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

Development of magnetic matrix solid phase dispersion method for the extraction of crystal violet and rhodamine B from sediments based on magnetic ZIF-8 and a deep eutectic solvent

A magnetic matrix solid phase dispersion (MSPD) method based on magnetic ZIF-8 (SDS@MZIF-8) and a deep eutectic solvent was developed and used to the extraction of crystal violet and rhodamine B in lake sediments. SDS@MZIF-8 was prepared and used as the extraction sorbent and dispersant in MSPD. The magnetic property of MZIF-8 facilitated the recovery of the extraction sorbent after the blending step. Hydrophilic deep eutectic solvents were prepared and used as efficient green dispersing solvents in MSPD. The use of magnetic sorbent in MSPD is simple and fast, eliminating some additional steps commonly used in the classical MSPD and shortening the extraction time. The parameters influencing the extraction efficiency were investigated and optimized. Under the optimized conditions, the intra- and inter-day relative standard deviations were less than 4.9 %. The linearity ranged from 2-400 µg g−1 with coefficients of determination higher than 0.9943. The detection and quantification limits of RB and CV varied between 0.3–0.5 μg g−1 and 1.0–1.8 μg g−1, respectively. Finally, the developed method was applied to the analysis of RB and CV in the sediment samples. The recoveries ranged from 93.2 to 107.3 % and the relative standard deviations ranged from 0.8 to 4.9 %. The results suggest a high potential use of the proposed method to determine the organic pollutants in solid samples. Compared with the conventional MSPD extraction technique, the developed method considerably reduced the sample and solvent consumption, offering important environmental benefits.

Formulation and Evaluation of Edoxaban Sublingual Tablets Using HPMC as a Hydrophilic Polymer by Solid Dispersion Method

Formulation and Evaluation of Edoxaban Sublingual Tablets Using HPMC as a Hydrophilic Polymer by Solid Dispersion Method

Synthesis of hydrophobic CuCl/LaA modified by butyltrichlorosilane towards enhanced CO adsorption under humid environment

Cuprous ion modified molecular sieves have been considered as promising CO adsorbents in gas separation or purification industry. However, it persists as a significant challenge to overcome the unfavorable effect of water vapor in the work environment on gas adsorption and separation. Herein, we propose a synthetic strategy using rare earth element La as an additive to form LaOLa coordination bonds followed by surface silanization treatment to construct a hydrophobic SiOSi barrier to significantly improve the stability of Cu+ under humid atmosphere. By successively introducing La3+ and Cu+ into zeolite 5A, CuCl/LaA adsorbents were prepared via ion exchange and solid dispersion methods. And then by silanization modification using toluene as solvent and butyltrichlorosilane (BTS) as hydrophobic agent, hydrophobic CuCl/LaA-BTS adsorbents were prepared. Dynamic adsorption investigation demonstrated that the as-prepared CuCl/LaA-BTS adsorbents possessed hydrophobic surface and consequently the adsorption capacity of CO was enhanced significantly under humid atmosphere. The CO adsorption breakthrough capacity over CuCl/LaA-BTS attained 0.34 mg/g, which was 5.7 times higher than that of zeolite 5A at 40 °C, atmospheric pressure and a relative humidity of RH = 55 %. Moreover, the CO adsorption capacity of CuCl/LaA-BTS retained 0.31 mg/g after four cycle regenerations. This work provides an effective and novel route for synthesizing highly stable cuprous ion modified zeolite adsorbents.

Preparation and Evaluation of Telmisartan Solid Dispersion as Sublingual Tablets

Background: Telmisartan is an antihypertensive angiotensin II receptor antagonist drug commonly used to treat hypertension and renal disease. Based on the Biopharmaceutical Classification System. It’s a Class II poorly soluble drug. Objective: To prepare a sublingual tablet by increasing the dissolution and solubility of Telmisartan utilizing the solid dispersion method. Methods: Three methods were obtained to prepare the solid dispersion of telmisartan: solvent evaporation, Kneading, and microwave method. Each method uses surplus as a hydrophilic carrier in different ratios of 1%, 2%, and 3%. Preparation of ternary solid dispersion by adding potassium carbonate salt to the binary solid dispersion. After that preparing the sublingual tablets by applying a direct compression method, using different types and ratios of superdisintegrants such as crospovidone, croscarmellose and sodium starch glycolate in 5% and 10%. Study the evaluation tests of sublingual tablets, such as friability, hardness, disintegration time and dissolution time. Results: The solid dispersion showed an improvement in solubility over the pure medication. The best result was obtained with the formula (Telmisartan, soluplus and k2co3 salt at 1:1:0.3 ratio) prepared by microwave method, in this method and the high ratio of soluplus, the solubility increased more than the solvent evaporation and kneading method. The selected tablet is prepared using crospovidone 10% as a superdisintegrant that appears disintegration time in 5 seconds and releases in 1 min in dissolution media. Conclusion: The solubility and dissolution of Telmisartan were improved by microwave-based ternary solid dispersion using hydrophilic carriers and salt in a ratio of 1:1:0.3 (drug: carrier: salt). The analysis exerts the increases in wettability, enhanced solubility, and dissolution due to conversion from crystal to amorphous state. Received May. 2023 Accepted Aug. 2023 Published Jan. 2024

Improvement of in vitro dissolution profile of poorly aqueous soluble anti-parasitic agent ivermectin using novel hydrophilic polymeric carriers

Ivermectin (IVM), a BCS Class II drug with weak water solubility, has minimal oral absorption and dissolution. This study aims to enhance the dissolution profile of IVM by performing solid dispersion methods using four hydrophilic polymers: Kollicoat IR, Kollidon 90F, poloxamer 407, and hydroxypropyl methylcellulose (HPMC). The solid dispersion formulations (SDF) were made through physical mixing, solvent evaporation, and melt solvent/fusion. Using three ratios of IVM and hydrophilic carriers (1:1, 1:2, and 1:3), the cumulative release rate of IVM from formulations formed by physical mixing, solvent evaporation, and fusing was much larger than pure IVM (10%). IVM release rates from formulations including Poloxamer 407, Kollicoat IR, and HPMC polymers were 76% (fusion technique), 69% (physical mixing), and 47% (solvent evaporation method). The research demonstrated that fusion optimized drug solubility better than physical mixing and solvent evaporation. The research found that SD of weakly water-soluble IVM with Kollicoat IR/Poloxamer 407 improves its in vitro dissolving profile much better. Bangladesh J. Sci. Ind. Res. 58(4), 209-220, 2023

Preparation and Evaluation of Aceclofenac Solid Dispersion by Fusion Technique and Effervescent Assisted Fusion Technique: Comparative Study

Solid dispersion (SD) is one of the most widely used methods to resolve issues accompanied by poorly soluble drugs. The present study was carried out to enhance the solubility and dissolution rate of Aceclofenac (ACE), a BCS class II drug with pH-dependent solubility, by the SD method. Effervescent assisted fusion technique (EFSD) using different hydrophilic carriers (mannitol, urea, Soluplus®, poloxamer 188, and poloxamer 407) in the presence of an effervescent base (sodium bicarbonate and citric acid) in different drug: carrier: effervescent base ratio and the conventional fusion technique (FSD) were used to prepare ACE SD. Solubility, dissolution rate, Fourier transformation infrared spectroscopy (FTIR), PowderX-ray diffraction study (PXRD), and Differential scanning calorimetry (DSC) were determined for the SD obtained from both techniques as a comparative study. The results showed that EFSD using ACE: Soluplus®: effervescent base in a ratio of 1:2:1 had higher solubility and dissolution rate than that obtained from FSD prepared by ACE: Soluplus® in a ratio of 1:2. However, the two techniques obtained the amorphous form according to XRD and DSC results. It can be concluded that EFSD is a promising method for the solubility and dissolution rate improvement of BCS class II drugs.

Solubility Enhancement of Lansoprazole by using Solid Dispersion Technique

In the existing study focused on the solubility enhancement of lansoprazole by using solid dispersion technique. Lansoprazole is proton pump inhibitor (PPI). Lansoprazole is used for the treatment of gastric ulcer. Lansoprazole is the Class II Drug of Biopharmaceutical Classification system. By using novel solid dispersion methods to enhance the oral solubility of poor water-soluble drug. Lansoprazole has the low solubility and high permeability. Hence to enhance the solubility of lansoprazole we prepared the Lansoprazole solid dispersion (SD) with PVP K30, Poly Ethylene Glycol 6000 (PEG 6000) and Poloxamer 407. Lansoprazoledissolving tablet were formulated using various superdisintegrants like Crospovidone and Sodium Starch Glycolate by Direct compression. The prepared the tablet is evaluated at various parameters like weight variation, hardness, friability, disintegration time, drug content uniformity and In-vitro dissolution. The In-vitro Drug release study of solid dispersions SD6 show the high drug release around 98.93%. Overall, in the all formulations F12 which contains 6%, 3.75% and 10% of Crospovidone, SSG and MCC release the 98.93% drug is the best formulation.

Febuxostat solubilization and stabilization approach using solid dispersion method: Synergistic effect of dicalcium phosphate dehydrate and chitosan

Drug solubilization studies are continuously being conducted. Febuxostat (FBX) has a low solubility in water. This study aims to develop a stable FBX-solid dispersion (SD) formulation using a solvent evaporation method. The solubilization strategy of FBX is to develope an optimal FBX-SD formulation by selecting a solubilizer and carrier through the screening method. The final selected solubilizer, macrogol 15 hydroxystearate and polyoxyl 15 hydroxystearate (Kolliphor® HS-15), is widely used in the pharmaceutical industry as a nonionic solubilizing and emulsifying agent and has low toxicity. Especially when commonly used in developing lipophilic drug formulations, it dissolves well in water and ethyl alcohol. The optimal composition ratio of the formulation (SD4) was FBX:HS-15®:granular dicalcium phosphate dehydrate (DCP-D): A synthetic magnesium aluminometasilicate (Neusilin®UFL2):chitosan = 1:3:3:1:1 (w/w) and showed 3.0-, 2.3-, and 1.1-fold higher dissolution (%) of FBX compared to that of the Feburic tab® in pH 1.2 media, distilled water (DW), and pH 6.8 buffer, respectively. Also, in vitro release and in vitro permeability in SD4 formulation showed higher than that of Feburic tab®. Based on its stability over 6 months, it was confirmed that chitosan acted as a stabilizer. Moreover, due to weak intermolecular interactions, FBX in the SD4 formulation was considered to exist in a mixed state of amorphous and crystalline FBX. In conclusion, the improved dissolution (%) and stability of FBX in SD4 formulation were secured through the synergistic effect of excipients.

Solubility Enhancement, Formulation and Evaluation of Solid Tablet of Tinidazole

To attain the necessary concentration of medication in the systemic circulation for the predicted pharmacological response, solubility the phenomenon of solute dissolving in solvent to produce a homogeneous system is a crucial characteristic to consider. The primary challenge in developing formulations for both novel chemical entities and generics is their low water solubility. Formulation scientists face a significant obstacle in solubility. The Classification of Biopharmaceutics states that APIs from Classes II and IV have reduced bioavailability, dissolution, and solubility. The article covers a range of technologies that can be used to make drugs that aren't very water-soluble more soluble. These include crystal engineering, pharmaceutical salts, drug nanocrystals, solid dispersion methods, polymeric micelle preparation, cosolvents, micelles, microemulsions, and emulsion formation. Physical and chemical drug modifications, crystal engineering, salt formation, solid dispersion, surfactant use, micronization, solid dispersions, nano sizing, cyclodextrin complexation, and other advanced methodologies are primarily described in this review. Other methods also contribute to improving solubility and bioavailability. It was an effort to talk about different complexation methods and to quickly point out their possible uses, as well as their technical and economic limits.

Improving the Bioavailability of Curcumin in Curcuma heyneana by Preparing Solid Dispersion

Curcuma heyneana or Temu Giring contains curcumin which has anti-aging potential and is traditionally used as a body scrub. This potential comes from the active ingredient (curcumin) which can prevent premature aging with its activity as an antioxidant, inhibitor of the tyrosinase enzyme, and inhibitor of the collagenase enzyme. So, it can prevent hyperpigmentation and inhibit the breakdown of collagen which can have an impact on skin aging. Oral dosage forms for anti-aging are starting to be found on the market and becoming a trend because of their convenient use. However, it is known that curcumin as an active ingredient of Temugiring, has poor solubility and bioavailability. The bioavailability of curcumin is low when administered orally due to its low absorption and its stability which decreases significantly when the pH is above 7. This study is a literature review of national and international literature databases that aims to determine the potential for increasing the bioavailability of curcumin using solid dispersion techniques. The results obtained indicate that making Temu Giring extract tablets containing curcumin using the solid dispersion method can increase the bioavailability of curcumin by overcoming the poor solubility, permeability, absorption, and stability of curcumin. By designing the Temu Giring extract using a solid dispersion method, the curcumin can be completely dissolved and released into the stomach. Keywords: Curcuma heyneana, Temu Giring, anti-aging, tablet, curcuminoid, antioxidant, solid dispersion.

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 > 0.05); rate of consolidation < 0.43 and Carr’s indices < 23.53, drug entrapment efficacy > 93 % and dispersion-number < 4.33. The granules dissolution rates after 10 and 60 mins were > 94.11 % and > 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.

Formulation and Characterization of Oral Dispersible Tablet of Aprepitant

The oral route of drug administration is more common and convenient where tablets and capsules emerged as popular dosage form but many patients have dysphasia or difficulty in swallowing which is currently affecting 35% general population. Aprepitant is anti-emetic drug and used in the treatment of chemotherapy in cancer. Fast onset of action is required in this indication there for it was thought to prepare Oral Dispersible Tablet of Aprepitant which would help to avoid first pass metabolism and improve bioavailability also Aprepitant is insoluble in water so, to increase the solubility solid dispersion method (kneading method) was used. Here, Aprepitant ODT is prepared by direct compression method using Polyplasdone XL10 as superdisitegrant and optimized by 32 Full factorial design. Here, Polyplasdone XL10 (x1) and Mannitol(x2) is use as independent variable. while dependent variable are disintegration time and wetting time. Optimized formulation F8 batch showed drug content (98.41±0.91); disintegration time is (18.02±1.20) Wetting time (22.53±0.43). The formulation is stable at 40ºc/75% RH for 30days.

Pluronic® P-123 as a reductant and stabilizing agent for gold nanoparticles (AuNPs) combined with methylene blue for photodynamic and photothermal therapy

The search for more effective drugs and therapies for the treatment of microbial diseases has driven the development of nanomedicine in recent years. In this sense, the present work shows the combination of photodynamic therapy (PDT) and photothermal therapy (PTT) using the photoactive drugs: methylene blue (MB) and gold nanoparticles (AuNPs). The ABA triblock Pluronic® P-123 copolymer was employed both as a micellar nanocarrier and reductant/stabilizing agent for AuNPs. The synthesis of gold nanoparticles (AuNPs) was carried out in situ through the redox process of AuCl3 gold salt in the presence of different concentrations of P-123 ranging from 0.25 % to 8.00 % ( % w/V) following the solid dispersion method. The MB was incorporated into the copolymeric micellar system by passive and active incorporation methods. In general, the system containing 1.00 % and 2.00 % (w/V) of P-123 was the more efficient and reproducible to obtain P-123/AuNPs/MB samples. The AuNPs synthesized presented plasmonic resonance peaks ranging from 535 to 554 nm, characteristic of spherical AuNPs. Dynamic Light Scattering and transmission electronic microscopy confirm the structure of the polymeric micelle around 20 nm and the AuNPs 3 nm diameters. The fluorescence emission showed to be dependent on the excitation wavelength, a promising feature for biological applications, especially when considering an image-guided diagnosis. Furthermore, the Stern-Volmer study by fluorescence quenching with iodide showed that active incorporation favors greater internalization of MB at the hydrophobic core of the micelle. On the other hand, the passive incorporation method placed MB in the most hydrophilic region in the micelle. The photodynamic effect was confirmed by singlet oxygen generation using ABDA as a probe. Thermal Lens spectroscopy and heating studies also confirms the heat generation by the system. In addition, the results point to synergism both in the generation of 1O2 and heat. The in vitro susceptibility of the samples was evaluated in Candida albicans strain. Better antifungal activity was observed in the sample of 2.00 % P-123/AuNPs/MB by Passive incorporation, illuminated with red and green LEDs. The biological study in bacteria strains of E. coli and S. aureus has shown that both percentages of P-123 with MB and AuNPs/MB by passive incorporation were efficient in controlling the evaluated bacteria. In this way, the present work showed promise for the treatment of antimicrobials through the combined therapy of PDT and PTT.

Solid Dispersion Technology for Improving the Solubility of Antiviral Drugs

Most drugs, including antiviral drugs, show low solubility in water, which affects dissolution, bioavailability, and therapeutic effectiveness. Therefore, many antiviral drugs are given in very large doses. One of the efforts to overcome these problems is the application of solid dispersions in which polymers and surfactants can trap drug molecules that are in the amorphous phase. Drugs in a hydrophilic carrier will increase wettability, water absorption capacity, and porosity of particles, so that the drug is released better. This review article will discuss the development of technology in solid-state, how solid dispersion overcomes the lack of solubility and the rate of dissolution of antiviral drugs, and solid dispersion preparation techniques. We also discuss some examples of successful applications of solid dispersion methods to antiviral drugs that have been circulating on the market. Overall, this review article offers information of innovation in the development of antiviral drugs to provide more solid dispersion antiviral drug products.

KRONOFARMASÖTİK İLAÇ TAŞIYICI BASINÇLA KAPLANMIŞ MİNİ TABLETLERİN HAZIRLANMASI VE DEĞERLENDİRİLMESİ

Objective: This study aims to prepare and evaluate time-controlled drug delivery system of telmisartan. Telmisartan has low aqueous solubility, which is its major drawback. The solubility of the drug enhanced by using solid dispersion method and compression coated chronotherapeutic tablets were formulated.
 Material and Method: Solid dispersion of telmisartan was prepared by melting method. Direct compression method was used to prepare telmisartan containing core tablets and tablets were coated by compression-coating method. Prepared tablets were characterized in terms of hardness, diameter, and thickness. In order to demonstrate the pulsatile release, the tablets were subjected to USP Apparatus II dissolution test.
 Result and Discussion: Solid dispersion of telmisartan increased the solubility of telmisartan significantly (p