Aqueous Solubility Of Drug Research Articles

Development and Evaluation of a Water Soluble Fluorometholone Eye Drop Formulation Employing Polymeric Micelle.

Low aqueous solubility of drug causes difficulties in preparation and inconvenience of administration. Polymeric micelles of fluorometholone (FML) using solid dispersion technique were prepared to develop an eye drop formulation with enhanced water solubility. Solid dispersions of FML were prepared at various FML:Soluplus® w/w ratios using solvent evaporation method. A physical mixture was also prepared. Physicochemical characterization was performed with various methods. Ex vivo porcine corneal permeation of polymeric micelle, physical mixture, and commercial product were compared. FML solid dispersion (1:15) showed the highest solubility, which was c.a. 169.6- and 15.3-fold higher than that of pure FML and physical mixture. Characterization showed that the crystalline form of FML changed to amorphous state and polymeric micelles were formed in round micelle. Flucon®, a commercial product of FML, showed significantly large particle size and high poly dispersity index. In contrast, FML polymeric micelle showed submicron size with uniform size distribution. Ex vivo porcine corneal permeation study showed that permeation by polymeric micelles was significantly higher than that by the commercial product and physical mixture. In addition, confocal laser scanning microscopic analysis supported the enhanced porcine corneal tissue permeation property of polymeric micelle. In conclusion, polymeric micelle prepared with solid dispersion using Soluplus® can be a potential nanomedicine for ocular delivery of poorly water-soluble FML.

Effect of solute aggregation on solubilization

Strong self-association of hydrophobic solutes takes place in water. However, solute self-association has often been neglected in understanding the aqueous solubility of drugs as well as their solubilization by excipients, cosolvents and hydrotropes. Based on a rigorous statistical thermodynamic foundation, here we show how to estimate the contribution from solute self-association to solubility and solubilization, based on experimental data such as solubility and the osmotic second virial coefficients. Such data show that solute self-association can indeed be negligible in most common cases of hydrotropic solubilization, Setschenow coefficients and the hydrophobic hydration.

Lipid Based Aqueous Core Nanocapsules (ACNs) for Encapsulating Hydrophillic Vinorelbine Bitartrate: Preparation, Optimization, Characterization and In vitro Safety Assessment for Intravenous Administration.

Vinorelbine bitartrate (VRL) is an antimitotic agent approved by FDA for breast cancer and non-small cell lung cancer (NSCLC) in many countries. However, high aqueous solubility and thermo degradable nature of VRL limited the availability of marketed dosage forms. The current work is focused on the development of lipid based aqueous core nanocapsules which can encapsulate the hydrophilic VRL in the aqueous core of nanocapsules protected with a lipidic shell which will further provide a sustained release. The ACNs were prepared by double emulsification technique followed by solvent evaporation. Box Behnken Design was utilized to optimize the formulation and process variables. Thirteen batches were generated utilizing lipid concentration, surfactant concentration and homogenizer speed as dependent variables (at three levels) and particle size and encapsulation efficiency as critical quality attributes. The ACNs were characterized for particle size, zeta potential, polydispersity index (PDI), entrapment efficiency, morphology by Transmission Electron Microscopy (TEM) and in vitro release. The ACNs were further evaluated for safety against intravenous administration by haemocompatibility studies. Results demonstrated that lipidic nanocapsules enhanced the entrapment efficiency of VRL up to 78%. Transmission Electron Microscopy revealed spherical shape of ACNs with core-shell structure. The GMS-VRL-ACNs showed that release followed Korsemeyer peppas kinetics suggesting Fickian diffusion. Moreover, the compliance towards haemocompatibility studies depicted the safety of prepared nanocapsules against intravenous administration. ACNs were found to be promising in encapsulating high aqueous soluble anticancer drugs with enhanced entrapment and safety towards intravenous administration.

IMPROVEMENT OF DISSOLUTION PROPERTIES OF ALBENDAZOLE FROM DIFFERENT METHODS OF SOLID DISPERSION

Poor aqueous solubility of drugs results in poor absorption and bioavailability. The objective of Solid dispersion technology is to increase the dissolution properties of highly lipophilic drugs, by using different hydrophilic carriers thereby improving their bioavailability. This technology is useful for enhancing the dissolution, absorption and therapeutic efficacy of drugs in dosage forms. Albendazole is a broad-spectrum antihelminthic agent used for the treatment of a variety of parasitic worm infestations. It is practically insoluble in water but slightly soluble in solvents like chloroform, methanol, ethyl acetate, and acetonitrile. The aim of our study was to improve the dissolution profile of Albendazole using HPMC K 100 LV, Kollidon VA64 and Mannitol as carriers by solid dispersion techniques. From the prepared solid dispersion, formulation code CSF5 showed better result where carrier was HMPC K 100 LV at 1:10 ratio in solvent evaporation method. Among the carrier used here to conduct our study, HPMC K 100 LV showed better result for both kneading and solvent evaporation methods. And among the method employed here, solvent evaporation method showed better solubility of drug at 60 min also at 1:10 ratio which was 78.86%.

Engineering Cocrystals of PoorlyWater-Soluble Drugs to Enhance Dissolution in Aqueous Medium.

Biopharmaceutics Classification System (BCS) Class II and IV drugs suffer from poor aqueous solubility and hence low bioavailability. Most of these drugs are hydrophobic and cannot be developed into a pharmaceutical formulation due to their poor aqueous solubility. One of the ways to enhance the aqueous solubility of poorlywater-soluble drugs is to use the principles of crystal engineering to formulate cocrystals of these molecules with water-soluble molecules (which are generally called coformers). Many researchers have shown that the cocrystals significantly enhance the aqueous solubility of poorly water-soluble drugs. In this review, we present a consolidated account of reports available in the literature related to the cocrystallization of poorly water-soluble drugs. The current practice to formulate new drug cocrystals with enhanced solubility involves a lot of empiricism. Therefore, in this work, attempts have been made to understand a general framework involved in successful (and unsuccessful) cocrystallization events which can yield different solid forms such as cocrystals, cocrystal polymorphs, cocrystal hydrates/solvates, salts, coamorphous solids, eutectics and solid solutions. The rationale behind screening suitable coformers for cocrystallization has been explained based on the rules of five i.e., hydrogen bonding, halogen bonding (and in general non-covalent bonding), length of carbon chain, molecular recognition points and coformer aqueous solubility. Different techniques to screen coformers for effective cocrystallization and methods to synthesize cocrystals have been discussed. Recent advances in technologies for continuous and solvent-free production of cocrystals have also been discussed. Furthermore, mechanisms involved in solubilization of these solid forms and the parameters influencing dissolution and stability of specific solid forms have been discussed. Overall, this review provides a consolidated account of the rationale for design of cocrystals, past efforts, recent developments and future perspectives for cocrystallization research which will be extremely useful for researchers working in pharmaceutical formulation development.

Stabilization benefits of single and multi-layer self-nanoemulsifying pellets: A poorly-water soluble model drug with hydrolytic susceptibility

Solidified self-nanoemulsifying drug delivery systems (SNEDDS) offer strong option to enhance both drug aqueous solubility and stability. The current study was designed to evaluate the potential stabilization benefits of solidifying cinnarizine (CN) liquid SNEDDS into single and multi-layer self-nanoemulsifying pellets (SL-SNEP and ML-SNEP, respectively). The selected formulations were enrolled into accelerated, intermediate and long-term stability studies. The chemical stability was assessed based on the % of intact CN remaining in formulation. The physical stability was assessed by monitoring the in-vitro dissolution and physical appearance of the formulations. The degradation pathway of CN within lipid-based formulation was proposed to involve a hydroxylation reaction of CN molecule. The chemical stability study revealed significant CN degradation in liquid SNEDDS, SL-SNEP and ML-SNEP (lacking moisture-sealing) within all the storage conditions. In contrast, the moisture sealed ML-SNEP showed significant enhancement of CN chemical stability within the formulation. In particular, ML-SNEP coated with Kollicoat Smartseal 30D showed superior CN stabilization and no significant decrease in dissolution efficiency, at all the storage conditions. The observed stability enhancement is owing to the complete isolation between CN and SNEDDS layer as well as the effective moisture protection provided by Kollicoat Smartseal 30D. Hence, the degradation problem could be eradicated completely. The incorporation of silicon dioxide had an important role in the inhibition of pellet agglomeration upon storage. Accordingly, ML-SNEP coated with Kollicoat Smartseal 30D and/or silicon dioxide could be an excellent dosage form that combine dual enhancement of CN solubilization and stabilization.

Formulation and Evaluation of Solid Dispersion and Inclusion Complex of Poorly Aqueous Soluble Diacerein

The present study was focused on a poorly aqueous soluble drug (diacerein); basic structured anthracene molecule possesses defensive activity against osteoarthritis. The problem with the diacerein is its poor bioavailability (35%) which is due to its poor dissolution profile. The present study efforts to improve the dissolution profile using solubility enhancement techniques. The objective of the study was to improve the solubility of poorly soluble drug diacerein by solid dispersion technique and inclusion complex using the most compatible carriers and technique for the formulation. The prepared solid dispersion and inclusion complex were evaluated for physiochemical characteristics and dissolution efficacy. Thesolid dispersion and inclusion complex were formulated using kneading method with PVP K30 (screened to be the best among different carriers) and β-cyclodextrin respectively. The prepared formulations were characterized by FTIR, SEM, DSC and XRPD. The prepared solid dispersion and inclusion complex were then compressed into conventional tablets which were then coated with acid resistant polymer.

FORMULATION DEVELOPMENT, CHARACTERIZATION, AND IN VITRO-IN VIVO STUDY OF ANTIHYPERLIPIDEMIC DRUG ROSUVASTATIN CALCIUM - SOLID LIPID NANOPARTICLES

Objective: The aim of this study was to formulate and optimize solid lipid nanoparticles (SLNs) for the enhancement of solubility and bioavailability of the poorly aqueous soluble drug rosuvastatin calcium.Methods: SLNs were prepared by slight modification of solvent emulsification-diffusion technique and analyzed for particle size, zeta potential, drug entrapment efficiency, in vitro drug release, stability, and pharmacokinetic studies. Rosuvastatin calcium SLNs were formulated using stearic acid as main lipid, poloxamer 407 as surfactant, and Tween 80 as cosurfactant.Results: All parameters were found to be in an acceptable range. Optimized formulation OR2 SLNs have shown mean particle size 115.49±2.97 nm with polydispersity index value of 0.456, zeta potential - 18.40 mV, 60.34% drug loading, and 97.16% drug entrapment efficiency. In vitro drug release was found to be 88.70±3.59% after 12 h with sustained release and was fitted with Higuchi model with a very high correlation coefficient (R2=0.9905). Transmission electron microscopy confirms that the SLNs of selected optimized formulation are circular in shape. Differential scanning calorimetry and X-ray diffraction confirm the formation of amorphous product. 1H nuclear magnetic resonance studies confirm the intermolecular hydrogen bonding between drug and lipid. Pharmacokinetic studies showed an optimized formulation OR2 SLNs enhanced bioavailability with 4.44-fold as compare to plain drug suspension. Optimized formulation OR2 SLNs have shown good stability at 25±2°C and 60±5°C relative humidity for 180 days.Conclusion: Thus, the current study can be useful for the successful development of optimized SLNs and able to enhance the bioavailability of poorly soluble drug rosuvastatin calcium.

Mixed surfactant (altering chain length and head group) aggregates as an effective carrier for tuberculosis drug

Surface properties and aggregation behavior of cationic-cationic and cationic-non-ionic mixed surfactant systems viz. Dodecylethyldimethylammonium bromide (DDAB) with a series of double chain cationic surfactants (DiDDAB, DMDTAB, and DODAB) and non-ionic surfactants (Brij 96, Tyloxapol and Tween 80) were analysed using surface tension and transmission electron microscopy (TEM). The effect of chain length of cationic surfactant and hydrophilic-lypophilic balance (HLB) prominently observed in critical aggregation (cac) value. The aqueous solubility of anti-tuberculosis drug: rifampicin (RIF) was comparatively studied by UV–vis spectroscopy in presence of formulated micelles and vesicles. RIF was significantly solubilised in aqueous medium using all the formulated aggregates. RIF is very unstable in basic medium (above pH-7) and in oxidizing media. Therefore, stability at pH-13 as well as in strong oxidising environment was monitored using UV–vis spectroscopy. To trace the locus of the drug encapsulation in the micelles/vesicles, fluorescence spectroscopy and TEM studies were carried out. Both the techniques stemmed in complimentary results and confirmed that, RIF is majorly populated at polar medium in cationic-cationic vesicles and favour to reside at hydrophobic medium of the nonionic-cationic micelles.

Formulation and Evaluation of Fast Dissolving Tablet Containing Vilazodone Nanocrystals for Solubility and Dissolution Enhancement Using Soluplus: In vitro-In vivo Study

Orally disintegrating tablets : formulation, preparation techniques and evaluationPriyanka Nagar, Kusum Singh, Iti Chauhan, Madhu Verma, Mohd Yasir,Azad Khan, Rajat Sharma, Nandini Gupta

Nanoemulsion-Based Transdermal Drug Delivery System for the Treatment of Tuberculosis.

The nanoemulsion based carriers are the most suitable delivery systems for poorly soluble drugs to improve the drugs solubility, permeation of drugs and ultimately increase bioavailability by transdermal therapeutic system. The nanoemulsion for poorly soluble drugs is admirable and offered several advantages over others drug delivery. For nanoemulsions formulation, they have to deliver the energetic element at the specific organ with nominal uneasiness. Because of the prevention of hepatic first pass uptake transdermal course excel usual crest and trough plasma shape that usually comfort the administration. The antitubercular drugs relate to the formulation of Poly DL-Lactide-Co-Glycolide nanoparticles having an active substance encapsulated within and that the encapsulated substances are stable with respect to each other. The present study aimed to explore the challenges and methods in order to increase the solubility of poorly aqueous soluble drug for improved bioavailability alongwith relative study of toxicity problems related to anti-tubercular drug.

Multi-Layer Self-Nanoemulsifying Pellets: an Innovative Drug Delivery System for the Poorly Water-Soluble Drug Cinnarizine.

Beside their solubility limitations, some poorly water-soluble drugs undergo extensive degradation in aqueous and/or lipid-based formulations. Multi-layer self-nanoemulsifying pellets (ML-SNEP) introduce an innovative delivery system based on isolating the drug from the self-nanoemulsifying layer to enhance drug aqueous solubility and minimize degradation. In the current study, various batches of cinnarizine (CN) ML-SNEP were prepared using fluid bed coating and involved a drug-free self-nanoemulsifying layer, protective layer, drug layer, moisture-sealing layer, and/or an anti-adherent layer. Each layer was optimized based on coating outcomes such as coating recovery and mono-pellets%. The optimized ML-SNEP were characterized using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD), in vitro dissolution, and stability studies. The optimized ML-SNEP were free-flowing, well separated with high coating recovery. SEM showed multiple well-defined coating layers. The acidic polyvinylpyrrolidone:CN (4:1) solution presented excellent drug-layering outcomes. DSC and XRD confirmed CN transformation into amorphous state within the drug layer. The isolation between CN and self-nanoemulsifying layer did not adversely affect drug dissolution. CN was able to spontaneously migrate into the micelles arising from thedrug-free self-nanoemulsifying layer. ML-SNEP showed superior dissolution compared to Stugeron® tablets at pH 1.2 and 6.8. Particularly, on shifting to pH 6.8, ML-SNEP maintained > 84% CN in solution while Stugeron® tablets showed significant CN precipitation leaving only 7% CN in solution. Furthermore, ML-SNEP (comprising Kollicoat® Smartseal 30D) showed robust stability and maintained > 97% intact CN within the accelerated storage conditions. Accordingly, ML-SNEP offer a novel delivery system that combines both enhanced solubilization and stabilization of unstable poorly soluble drugs.

Excipient selection and aerodynamic characterization of nebulized lipid-based nanoemulsion loaded with docetaxel for lung cancer treatment.

Docetaxel has demonstrated extraordinary anticancer effects on lung cancer. However, lack of optimal bioavailability due to poor solubility and high toxicity at its therapeutic dose has hampered the clinical use of this anticancer drug. Development of nanoemulsion formulation along with biocompatible excipients aimed for pulmonary delivery is a potential strategy to deliver this poorly aqueous soluble drug with improved bioavailability and biocompatibility. In this work, screening and selection of pharmaceutically acceptable excipients at their minimal optimal concentration have been conducted. The selected nanoemulsion formulations were prepared using high-energy emulsification technique and subjected to physicochemical and aerodynamic characterizations. The formulated nanoemulsion had mean particle size and ζ-potential in the range of 90 to 110nm and - 30 to - 40mV respectively, indicating high colloidal stability. The pH, osmolality, and viscosity of the systems met the ideal requirement for pulmonary application. The DNE4 formulation exhibited slow drug release and excellent stability even under the influence of extreme environmental conditions. This was further confirmed by transmission electron microscopy as uniform spherical droplets in nanometer range were observed after storage at 45 ± 1°C for 3months indicating high thermal stability. The nebulized DNE4 exhibited desirable aerosolization properties for pulmonary delivery application and found to be more selective on human lung carcinoma cell (A549) than normal cell (MRC-5). Hence, these characteristics make the formulation a great candidate for the potential use as a carrier system for docetaxel in targeting lung cancer via pulmonary delivery.

Self-nanoemulsifying drug delivery system of nabumetone improved its oral bioavailability and anti-inflammatory effects in rat model

The present research work explored the prospective of self-nanoemulsifying drug delivery system (SNEDDS) to improve the oral bioavailability of NBT and its anti-inflammatory effect. Nabumetone (NBT) is a poorly aqueous soluble drug that demonstrates low bioavailability after oral administration. NBT-SNEDDS was prepared by using Capryol-90, Tween-80 and polyethylene glycol-400 (PEG-400) via pseudo-ternary phase diagram. Different components of SNEDDS were curtained and found an optimal ratio of 22: 16:4:58 for Capryol-90, Tween-80, PEG-400 and deionized water, respectively. The developed SNEDDS were characterized in terms of physicochemical, drug release (via dialysis membrane) studies. The pharmacokinetics and anti-inflammatory activity of the drug from optimized NBT-SNEDDS was compared with the suspension of marketed tablet in rats. A high oral bioavailability (3.02-times) of the drug was found from SNEDDS as compared to the suspension of marketed tablet. Remarkably, NBT-SNEDDS presented an increased anti-inflammatory efficacy when compared with orally administered commercial product of NBT. The results indicated that NBT-SNEDDS could be a potential carrier for an oral dosage form of NBT with enhanced relative bioavailability and therapeutic effects.

Fabrication of lecithin-gum tragacanth muco-adhesive hybrid nano-carrier system for in-vivo performance of Amphotericin B

Nano-carriers are excellent systems for improving bioavailability of poor aqueous soluble drugs. This study focuses fabrication of lecithin-gum tragacanth muco-adhesive hybrid NPs for enhancing Amphotericin B (AmpB) oral bioavailability. AmpB loaded lecithin NPs were synthesized through solvent diffusion method. Green synthesis of stable muco-adhesive gum tragacanth (GT) gold NPs was confirmed through UV–vis spectrophotometer and FT-IR. AmpB loaded lecithin NPs hybrid with GT gold NPs were characterized for shape, size, polydispersity index (PDI), zeta potential, drug entrapment efficiency and drug-excepients interactions using atomic force microscope (AFM), zetasizer, UV–vis spectrophotometer and FT-IR respectively. In-vivo bioavailability of AmpB loaded in NPs was investigated in rabbits. AmpB loaded muco-adhesive NPs were found polydispersed with 358.3 ± 1.78 nm mean size and −19.9 ± 0.51 mV zeta potential. They entrapped 78.91 ± 2.44% AmpB and enhanced its oral bioavailability in animals. Results reveal the hybrid NPs as efficient carriers for enhancing AmpB oral bioavailability in controlled manner.

FORMULATION AND EVALUATION OF SOLID DISPERSION OF TADALAFIL

Tadalafil is used for the treatment of the erectile dysfunction (ED) and pulmonary arterial hypertension. It is having low aqueous solubility thus it shows poor bioavailability of about 28% by after oral administration. To improve its solubility and dissolution profile solid dispersions (SDPs) of Tadalafil was prepared by physical mixing and solvent evaporation method using polyvinyl pyrollidone-K30 (PVP-30) as a hydrophilic polymeric carrier in different proportions with respect to drug (drug to polymer ratio 1:1 to 1:5). Drug and polymer compatibility studies were performed using FTIR study. The best suitable ratio and method was selected on the basis of enhanced aqueous solubility of drugs. Further selected SDPs were evaluated for various parameters like DSC analysis, percentage yield, percent drug content, saturation solubility, percent drug dissolution and stability studies. FTIR study indicated no incompatibility between Tadalafil and PVP-K30. SDPs prepared with drug to polymer ratio 1:3 and solvent evaporation method was found to be best as they shown significant increased (up to 10 fold) in aqueous solubility in comparison with that of others. DSC study also suggested the depression in the crystalline nature of Tadalafil. Selected SDPs exhibited good stability up to 3 months at 25 ± 2°C /60 ± 5% RH. Based on the results it can be concluded that, SDPs shown remarkable increase in the aqueous solubility and dissolution of Tadalafil and it may improve oral bioavailability of drug as compared with plain drug.

FORMULATION AND EVALUATION OF SOLID DISPERSION OF TADALAFIL

Tadalafil is used for the treatment of the erectile dysfunction (ED) and pulmonary arterial hypertension. It is having low aqueous solubility thus it shows poor bioavailability of about 28% by after oral administration. To improve its solubility and dissolution profile solid dispersions (SDPs) of Tadalafil was prepared by physical mixing and solvent evaporation method using polyvinyl pyrollidone-K30 (PVP-30) as a hydrophilic polymeric carrier in different proportions with respect to drug (drug to polymer ratio 1:1 to 1:5). Drug and polymer compatibility studies were performed using FTIR study. The best suitable ratio and method was selected on the basis of enhanced aqueous solubility of drugs. Further selected SDPs were evaluated for various parameters like DSC analysis, percentage yield, percent drug content, saturation solubility, percent drug dissolution and stability studies. FTIR study indicated no incompatibility between Tadalafil and PVP-K30. SDPs prepared with drug to polymer ratio 1:3 and solvent evaporation method was found to be best as they shown significant increased (up to 10 fold) in aqueous solubility in comparison with that of others. DSC study also suggested the depression in the crystalline nature of Tadalafil. Selected SDPs exhibited good stability up to 3 months at 25 ± 2°C /60 ± 5% RH. Based on the results it can be concluded that, SDPs shown remarkable increase in the aqueous solubility and dissolution of Tadalafil and it may improve oral bioavailability of drug as compared with plain drug.

Solubilization and Enhancement of Ex Vivo Vaginal Delivery of Progesterone Using Solid Dispersions, Inclusion Complexes and Micellar Solubilization.

Progesterone (PG), a natural female sex hormone is used clinically in menopausal hormone replacement therapy and to control reproductive functions. Its very limited aqueous solubility results in reduced oral bioavailability and low patient compliance when administered in high doses. The aim of this study was to enhance PG aqueous solubility and vaginal delivery using solid dispersion, inclusion complex and micellar solubilization techniques. PG solid dispersions and inclusion complexes were prepared by solvent evaporation method using different polymers, such as cyclodextrins, polyvinyl pyrrolidone (PVP), poly (ethylene glycol) 6000, Pluronic® F-127 and Pluronic® F-68. PG was also incorporated into polymeric micelles of Pluronic® F-127, Pluronic® F- 68, Brij®35 and Myrj®52. The prepared solid dispersions, inclusion complexes and micelles were characterized using different techniques. Drug permeability across rabbit vaginal mucosa was also studied. Dissolution studies of PG solid dispersions showed that the highest drug dissolution rate was achieved at PG/polymer weight ratio of 5:5. Further, complete drug dissolution was obtained for PG/Pluronic® F-127 solid dispersion after 15 min compared to 42% dissolution for the drug alone. Brij®35 micelles had a drug loading capacity ~15%, which increased the drug aqueous solubility by more than 20 folds. PG permeability coefficients through rabbit vaginal mucosa for PG/Brij®35 micelles and PG/Pluronic® F-127 micelles were ~ two times higher than that of the drug alone. These results confirm that Brij®35 and Pluronic® F-127 micelles are promising carriers to overcome PG shortcomings through enhancing its aqueous solubility and vaginal permeability.

Lipids and Surfactants: The Inside Story of Lipid-Based Drug Delivery Systems.

In the bioavailability enhancement of poorly aqueous soluble drugs, self-emulsifying/microemulsifying drug delivery systems (SEDDS/SMEDDS) are isotropic mixtures of oils, surfactants, solvents, and cosolvents/surfactants that have gained immense popularity because of their self-emulsification ability. This characteristic relies on some critical parameters such as surfactant concentration, oil-to-surfactant ratio, polarity of the emulsion, droplet size and charge, which are acquired from an amalgamation of appropriate excipients. The fabrication of this combination is of utmost importance for formulation scientists. Hence, to explore the potential of such a delivery system, standardized guidelines for excipients must be developed to address bioavailability issues. In the present review, we summarize the approaches to selecting the most suitable lipid(s)-based drug delivery system, including characterization, especially for oral delivery, of both physicochemical and biopharmaceutical aspects and properties of assorted excipients as well as the related patent reports.

Formulation and Evaluation of Pioglitazone HCl Fast Dissolving Tablet using Solid Dispersion

Pioglitazone HCL is a BCS class-II (poorly water soluble) drug and its absorption is dissolution rate limited. The solubility and the dissolution rate of the drug was enhanced by using the solid dispersion technique. The main purpose of this investigation was to increase the solubility and dissolution rate of pioglitazone HCL by the preparation of its solid dispersion with PEG-6000 using solvent evaporation methods. FT-IR spectra revealed no chemical incompatibility between drug and PEG-6000. The result obtained show that the dissolution profile of pioglitazone HCL solid dispersion was considerably improved. The dissolution profile solid dispersion formulation SD1 contains (1: 1) (drug: polymer) formulation SD2 (1: 2) & formulation SD3 (1: 3) was found to be 97.83±0.09, 94.03±0.09, 91.26±0.03 respectively. Based on the above dissolution data SD1 is found to be best as a solid dispersion for fast dissolving tablet. Based on the result solid dispersion technique can be an acceptable method for improving the dissolution profile of poorly aqueous soluble drug.