Liquid Self-emulsifying Drug Delivery System Research Articles

African Breadfruit Seed Oil as Lipid Phase of Self-Emulsifying Drug Delivery System for Improved Gastrointestinal Fluid Solubility of Ibuprofen: Design and Evaluation

Introduction: Rain forest vegetations all over the world produce large quantity of economically important seed oils which, in most developing countries are utilized only as food condiments but hardly employed in pharmaceutical formulations.
 Objectives: The purpose of this work was to formulate ibuprofen-loaded self-emulsifying drug delivery system for the enhancement of the gastrointestinal fluid solubility of this poorly water soluble drug.
 Methods: The breadfruit seed oil was extracted by the soxhlet extraction technique and characterized for various physicochemical properties including acid, iodine, peroxide, saponification values and organoleptic properties.  The super saturation solubility process, water titration studies and pseudo ternary phase diagrams were used to select and quantify the components of the emulsion systems. The liquid self-emulsifying drug delivery systems were converted to solid forms by adsorption onto a blend of miceocrystalline cellulose and Aerosil-200 powders. The resulting wet mass was dried and processed for encapsulation.
 Results: The percentage yield of the oil from the extraction process was 20.68 % while the acid, iodine, and saponification values were, 4.12 ± 1.24, 21.91 ± 0.88, and 302.45 ± 1.22 respectively. The ibuprofen exhibited higher solubility in the hydrolysed oil than in the crude form. Fourier transform infrared analysis did not reveal existence of component incompatibility. The optimized liquid and solid emulsions exhibited standard characteristics that were compatible to previous literature reports. The formulations also exhibited superior drug release properties over two control samples.
 Conclusion: It was concluded that Breadfruit seed oil has the potential to function as the lipid component of ibuprofen-loaded self-emulsifying drug delivery system formulated to enhance the aqueous solubility of the drug.

Formulation and statistical optimization of clozapine solid self emulsification system for improving the dissolution properties

Clozapine is an atypical antipsychotic drug that exhibits low bioavailability (>27%) due to poor solubility and higher hepatic metabolism. The present investigation was aimed to prepare a solid self-emulsifying drug delivery system (S-SEDDS) of clozapine to improve its dissolution properties. Various long-chained natural dietary oils, surfactants, and cosurfactants were screened to evaluate their drug solubilization ability and emulsification efficiency which was measured in terms of % transmittance of the formed system. A ternary phase diagram was generated to identify compositions that were able to form emulsions with the required globule size. The simplex lattice design was used to understand the effect of change in the composition of excipients on important product characteristics. The regression analysis suggested a significant effect of the change in the proportion of composition on selected response variables. The Liquid-SEDDS (L-SEDDS) were mixed with solid carriers (aerosil-200 and MCC) to form S-SEDDS. The results of Differential Scanning Calorimetry (DSC) and Powder X-Ray Diffraction (PXRD) studies indicated the complete transformation of the crystalline drug into the amorphous or molecular level dispersed state for the S-SEDDS prepared using aerosil-200 as a carrier. The results of in-vitro dissolution studies proved significant improvement in the dissolution of the drug from the S-SEDDS compared to the pure drug.

Twin Screw Melt Granulation: A Single Step Approach for Developing Self-Emulsifying Drug Delivery System for Lipophilic Drugs.

The current research aims to improve the solubility of the poorly soluble drug, i.e., ibuprofen, by developing self-emulsifying drug delivery systems (SEDDS) utilizing a twin screw melt granulation (TSMG) approach. Gelucire® 44/14, Gelucire® 48/16, and Transcutol® HP were screened as suitable excipients for developing the SEDDS formulations. Initially, liquid SEDDS (L-SEDDS) were developed with oil concentrations between 20-50% w/w and surfactant to co-surfactant ratios of 2:1, 4:1, 6:1. The stable formulations of L-SEDDS were transformed into solid SEDDS (S-SEDDS) using a suitable adsorbent carrier and compressed into tablets (T-SEDDS). The S-SEDDS has improved flow, drug release profiles, and permeability compared to pure drugs. The existence of the drug in an amorphous state was confirmed by differential scanning calorimetry (DSC) and powder X-ray diffraction analysis (PXRD). The formulations with 20% w/w and 30% w/w of oil concentration and a 4:1 ratio of surfactant to co-surfactant have resulted in a stable homogeneous emulsion with a globule size of 14.67 ± 0.23 nm and 18.54 ± 0.55 nm. The compressed tablets were found stable after six months of storage at accelerated and long-term conditions. This shows the suitability of the TSMG approach as a single-step continuous manufacturing process for developing S-SEDDS formulations.

Improvement of dissolution profile of eplerenone with solidified self-emulsifying drug delivery systems (S-SEDDS)

Context Eplerenone is a member of antihypertensives used individually or in combination with other medicines. Eplerenone exhibits poor solubility and is considered a class II drug. Objective Increasing the solubility of eplerenone by using both liquid and solid self-emulsifying drug delivery systems as an alternative to its marketed tablet product. Methods Solubility studies of eplerenone were done with different oils, surfactants, and co-surfactants to determine which one has the highest solubility for eplerenone and determine the preference in the formulations of liquid self-emulsifying drug delivery system. The solidification process was carried out with the adsorption to solid carrier method. Optimal ratios of components were specified with the pseudo-ternary phase diagram technique. Self-emulsifying drug delivery system formulations were characterized in terms of chemical interaction, droplet size/distribution, crystallization behaviors, and rheological evaluation. In vitro drug release studies were conducted and compared to pure drugs and marketed products. Results The solubility screening results showed high solubility of EPL in triacetin (11.99 mg/mL) as oil, Kolliphor®EL (≈ 2.65 mg/mL), and Tween80 (≈ 1.91 mg/mL) as surfactant and polyethylene glycol 200 (PEG200) (≈ 8.50 mg/mL), dimethyl sulfoxide (≈ 7.57 mg/mL), TranscutolP (≈ 6.03 mg/mL) as co-surfactant, respectively. Rheology studies revealed that liquid self-emulsifying drug delivery formulations exhibited non-Newtonian pseudoplastic flow. Conclusion Solid self-emulsifying drug delivery systems prepared with Aerosil and Neusilin have shown tremendous improvement in terms of eplerenone dissolution by releasing the entire dose with boosted effect within 5 and 30 min respectively compared to the marketed product and pure eplerenone (p < 0.05).

Fabrication and Evaluation of Solid Self Emulsifying Drug Delivery System of Dolutegravir sodium by using Adsorption to Solid Carrier Techniques

The objective of this work was to design and characterize liquid and solid self-emulsifying drug delivery systems (SEDDS) for poorly soluble Dolutegravir Sodium. To optimize the composition of liquid Dolutegravir Sodium-SEDDS, solubility tests, pseudoternary phase diagrams, emulsification studies and other in vitro examinations (thermodynamic stability, droplet size and zeta potential analysis) were performed. The central composite design was employed to optimize the formulation variables, Capmul MCM (oil), Tween 80 (surfactant) and Propylene glycol (co-surfactant). Liquid self-emulsifying drug delivery system was appraised for determination of self emulsifying time, globule size and drug release. TEM study confirmed the uniform oil globules of the optimized liquid formulation. The optimized liquid formulation was formulated into free-flowing powder (S-SEDDS) by adsorption on the materials like Aerosil 200, Neusilin US2 and compressed into tablets. The solid state characterization of S-SEDDS powder was performed by using DSC, PXRD and SEM to investigate the physical nature of the drug. Further, the accelerated stability studies for 6 months revealed that S-SEDDS of Dolutegravir Sodium was found to be stable without any significant change in physico-chemical properties. S-SEDDS of Dolutegravir Sodium with improved dissolution profile was successfully prepared by using Neusilin US2 as an adsorbent carrier as compared to marketed sample.

Effects of Formulation and Manufacturing Process on Drug Release from Solid Self-emulsifying Drug Delivery Systems Prepared by High Shear Mixing.

This study sought to investigate the influence of formulation and process factors of the high shear mixing (HSM) on the properties of solid self-emulsifying drug delivery systems (S-SEDDS) containing the model drug carvedilol (CAR). Firstly, liquid SEDDS (L-SEDDS) were prepared by mixing castor oil with different proportions of surfactant (Solutol or Kolliphor RH40) and cosolvent (Transcutol or PEG400). A miscible L-SEDDS with high drug solubility (124.3mg/g) was selected and gave rise to 10% (m/m) CAR loaded-emulsion with reduced particle size. Then, a factorial experimental design involving five component's concentration and two process factors was used to study the solidification of the selected L-SEDDS by HSM. CAR content, diffractometric profile, and in vitro dissolution were determined. Morphological and flow analyses were also performed. Porous and spherical particles with mean sizes ranging from 160 to 210µm were obtained. Particle size was not affected by any formulation factor studied. Powder flowability, in turn, was influenced by L-SEDDS and crospovidone concentration. CAR in vitro dissolution from S-SEDDS was significantly increased compared to the drug as supplied and was equal (pH 1.2) or lower (pH 6.8) than that determined for L-SEDDS. Colloidal silicon dioxide decreased drug dissolution, whereas an increase in water-soluble diluent lactose and L-SEDDS concentration increased CAR dissolution. The proper selection of liquid and solid constituents proved to be crucial to developing an S-SEDDS by HSM. Indeed, the results obtained here using experimental design contribute to the production of S-SEDDS using an industrially viable process.

A Review on Formulation and Development of Solid Self-Nano Emulsifying Drug Delivery Systems

This article describes current strategies to enhance aqueous solubility and dissolution rate of poor soluble drugs. Most drugs in the market are lipophilic with low or poor water solubility. There are various methods to enhance solubility: co-solvency, particle size reduction, salt formation and Self Nanoemulsifying drug delivery systems, SEDDS is a novel approach to enhance solubility, dissolution rate and bioavailability of drugs. The study involves formulation and evaluation of solid self-Nano emulsifying drug delivery system (S-SNEDDS) to enhance aqueous solubility and dissolution rate. Oral route is the most convenient route for non-invasive administration. S-SNEDDS has more advantages when compared to the liquid self-emulsifying drug delivery system. Excipients were selected depends upon the drug compatibility oils, surfactants and co surfactants were selected to formulate Liquid SNEDDS these formulated liquid self-nano emulsifying drug delivery system converted into solid by the help of porous carriers, Melted binder or with the help of drying process. Conversion process of liquid to solid involves various techniques; they are spray drying; freeze drying and fluid bed coating technique; extrusion, melting granulation technique. Liquid SNEDDS has a high ability to improve dissolution and solubility of drugs but it also has disadvantages like incompatibility, decreased drug loading, shorter shelf life, ease of manufacturing and ability to deliver peptides that are prone to enzymatic hydrolysis.&#x0D;  

Insights into Novel Excipients of Self-Emulsifying Drug Delivery Systems and Their Significance: An Updated Review.

Self-emulsifying drug delivery system (SEDDS), a category of lipid-based technology, has gained interest in the recent years for enhancement of solubility and bioavailability of poorly water-soluble drugs. With the progress of research in this field, novel excipients have been developed with enhanced properties. But excipient selection is the key hurdle in the formulation of SEDDS. The objective of this review is to summarize different types of oils, surfactants, co-surfactants which are the key components of liquid SEDDS (L-SEDDS), various carriers utilized in the conversion of L-SEDDS to solid SEDDS (S-SEDDS), their description, properties, grades, and applications in pharmacy. This article provides an overview of solidification techniques to transform L-SEDDS to S-SEDDS which are more stable and have better patience compliance. This review presents numerous literature reports on various excipients used and the discussion on how these excipients affect the final results.

Solidification of self-emulsifying drug delivery systems (SEDDS): Impact on storage stability of a therapeutic protein

Four solidification methods for self-emulsifying drug delivery systems (SEDDS) were compared to evaluate the impact of solidification on storage stability of an incorporated protein.Papain was loaded in SEDDS via hydrophobic ion pairing (HIP). Liquid SEDDS (l-SEDDS) were either solidified by adsorption to solid excipients such as magnesium-aluminometasilicate via wet granulation (ssilica-SEDDS) and carbohydrates via lyophilisation (scarbo-SEDDS) or by incorporation of high-melting PEG-surfactants (sPEG-SEDDS) and triglycerides (soil-SEDDS) in SEDDS preconcentrates. L- and s-SEDDS were compared regarding intrinsic emulsion properties, solid-state form of papain, enzyme stability and activity during storage.HIP with deoxycholate showed a precipitation efficiency of 82% and papain maintained 90% of its initial activity. Incorporated papain was present in an amorphous state, confirming a molecular dispersion in all preconcentrates. In comparison to l-SEDDS each solidification method investigated improved the storage stability of incorporated papain. Neither precipitation nor phase separation was observed for s-SEDDS. sPEG-SEDDS demonstrated with 87.8% the highest enzymatic activity and displayed according to the following rank order: sPEG-SEDDS > soil-SEDDS > ssilica-SEDDS > scarbo-SEDDS > l-SEDDS the highest remaining papain activity after 30 days of storage. This work clearly demonstrates that solidified SEDDS can provide a significantly improved storage stability for therapeutic proteins compared to corresponding liquid formulations.

A Rundown Through Various Methods Used in the Formulation of Solid Self-Emulsifying Drug Delivery Systems (S-SEDDS).

The most common route of the drug administration is oral route despite the fact that most drugs have low oral aqueous solubility and bioavailability especially for BCS class II and class IV drugs. Many methods have been developed in recent years to overcome the poor solubility and oral bioavailability which includes self-emulsifying drug delivery systems (SEDDS) as one of the approaches. Not only for hydrophobic drugs, but also for hydrophilic compounds with low permeability, bioavailability can be enhanced by self nanoemulsifying drug delivery systems. Recently, a lot of focus and attention has been put in the conversion of liquid SEDDS (L-SEDDS) to solid SEDDS (S-SEDDS) to overcome the limitations of liquid formulations related to their physical and chemical stability, portability, accurate dosing, and limited choices of dosage forms. This article aims to review the formulation components used in SEDDS, various approaches used in the conversion of L-SEDDS to S-SEDDS, their applications, merits, and demerits.

Self-emulsifying drug delivery systems with atorvastatin adsorbed on solid carriers: formulation and in vitro drug release studies

Two novel self-emulsifying drug delivery systems (SEDDS) with atorvastatin calcium, an anti-hyperlipidemic drug, were obtained and adsorbed on different solid inorganic carriers. In order to determine the parameters affecting the drug release process, different physicochemical analyses were performed. Liquid SEDDS were investigated for water solubilization capacity, viscosity and surface tension. In the case of solid materials, differential scanning calorimetry and scanning electron microscopy were conducted in order to check the samples for the presence of drug crystals. The interactions between the components of the materials were analyzed with inverse gas chromatography and Flory-Huggins parameters were calculated. The drug release experiments performed for all investigated formulations revealed that after the initial quick release the drug concentration in the dissolution medium decreased slightly which might be related to the crystallization process. However, the level of the released active ingredient was maintained at 80% for most formulations. It was also shown that the results of drug dissolution studies were independent of the measured physicochemical parameters, even though some clear differences have been observed between the analyzed materials.

Preparation and evaluation of Vinpocetine self-emulsifying pH gradient release pellets

The main objective of this study was to develop a pH gradient release pellet with self-emulsifying drug delivery system (SEDDS), which could not only improve the oral bioavailability of Vinpocetine (VIN), a poor soluble drug, but reduce the fluctuation of plasma concentration. First, the liquid VIN SEDDS formulation was prepared. Then the self-emulsifying pH gradient release pellets were prepared by extrusion spheronization technique, and formulation consisted by the liquid SEDDS, absorbent (colloidal silicon dioxide), penetration enhancer (sodium chloride), microcrystalline cellulose, ethyl alcohol, and three coating materials (HPMC, Eudragit L30D55, Eudragit FS30D) were eventually selected. Three kinds of coated pellets were mixed in capsules with the mass ratio of 1:1:1. The release curves of capsules were investigated in vitro under the simulated gastrointestinal conditions. In addition, the oral bioavailability and pharmacokinetics of VIN self-emulsifying pH gradient release pellets, commercial tablets and liquid VIN SEDDS were evaluated in Beagle dogs. The oral bioavailability of self-emulsifying pH gradient release pellets was about 149.8% of commercial VIN tablets, and it was about 86% of liquid VIN SEDDS, but there were no significant difference between liquid SEDDS and self-emulsifying pH gradient release pellets. In conclusion, the self-emulsifying pH gradient release pellets could significantly enhance the absorption of VIN and effectively achieve a pH gradient release. And the self-emulsifying pH gradient release pellet was a promising method to improve bioavailability of insoluble drugs.

Formulation and characterization of self emulsifing pellets of carvedilol

The purpose of present study was aimed at developing self emulsifying drug delivery system in liquid and then in pellet form that would result in improved solubility, dissolution and permeability of the poorly water soluble drug carvedilol. Pellets were prepared using extrusion-spheronization technique incorporating liquid SEDDS (carvedilol, capmul MCM EP, cremophore EL, tween 20, propylene glycol), adsorbents ( and crospovidone), microcrystalline cellulose and binder (povidone K-30). Ternary phase diagram was constructed to identify different oil-surfactant-cosurfactant mixtures according to the proportion of each point in it. The optimal CAR-SEDDS pellets showed a quicker redispersion with a droplet size of the reconstituted microemulsion being 160.47 nm, which was almost unchanged after solidification. SEM analysis confirmed good spherical appearance of solid pellets; DSC and XRD analysis confirmed that there was no crystalline carvedilol in the pellets. Pellets were then capable of transferring lipophilic compounds into the aqueous phase and significantly enhancing its release with respect to pure drug.

Design and evaluation of solid self-emulsifying drug delivery system of rosuvastatin calcium

Background: The work has been undertaken with an objective to prepare a self-emulsifying drug delivery system (SEDDS) of rosuvastatin calcium (ROS) with the least amount of surfactant which could enhance its solubility and oral bioavailability. Materials and Methods: Spectrophotometric method was used to estimate the solubility of the drug in various oils, surfactant and co-surfactant. The phase behavior and most efficient self-emulsifying region were identified by constructing pseudo ternary phase diagram. The solid-SEDDS (S-SEDDS) was prepared using an adsorbent consequently the prepared S-SEDDS were filled up in hard gelatin capsule which were evaluated for various physicochemical parameters. Results: The composition of optimized formulation consisted of 10 mg of ROS, capmul MCM (oil), cremophor ELP (surfactant) and propylene glycol (co-surfactant). The optimized formulation showed negative zeta potential (−22.11 mv), optimal particle size (10.59 nm) and demonstrated excellent self-emulsifying ability with a maximum solubilizing capability. The S-SEDDS formulations were prepared from the optimized liquid SEDDS, which revealed maximum release rate (97.7%) among all the prepared S-SEDDS formulation and marketed formulation. Conclusion: It was concluded that S-SEDDS prepared from liquid SEDDS can be a promising novel approach to enhance the solubility and drug release of ROS, which in turn also develops a stable formulation, least drugs leakage and precipitation than the liquid SEDDS. Key words: Adsorbent, bioavailability, drug release, rosuvastatin calcium, self-emulsifying drug delivery system, solubility

Taste-masked orodispersible tablets of cyclosporine self-nanoemulsion lyophilized with dry silica

The aim of the current study was to investigate the effects of formulation parameters on the disintegration, water absorption and dissolution characteristics of cyclosporine A (CyA) loaded self-emulsifying drug delivery system (SEDDS) in an orodispersible compacts. Its taste masking efficiency was also attempted using an electronic tongue. ODTs were prepared by freeze-drying liquid SEDDS and synthetic amorphous silica suspension followed by direct compression. The influences of the compression forces and super-disintegrant were evaluated to optimize tablet characteristics. The liquid SEDDS was characterized by vesicular size of 48.5 nm, polydispersity index of 0.95, turbidity of 40.7 NTU and rapid CyA dissolution and emulsification rate. The results of micrometric studies demonstrated an acceptable flow, hardness and friability to indicate good mechanical strength of ODTs. The interaction and Pareto charts demonstrated a greater effect of low compression force to increase the porosity and facilitate the disintegration rather than the deformation action of the super-disintegrant. Super-disintegrant level was the most important factor affecting the dissolution parameter followed by the compression force then their interaction effect. Moreover, as indicated by Euclidean distance values and discrimination indices, the unpalatable taste and aversion taste of CyA to stimuli were masked in its optimized SEDDS incorporated ODTs.

Formulation and in vitro characterization of a novel solid lipid-based drug delivery system.

The liquid self-emulsifying drug delivery system (L-SEDDS), commonly used to deliver effective but poorly water-soluble oleanolic acid (OA), has many limitations such as high manufacturing costs, few choices of dosage forms, risk of leakage from hard gelatin capsules, low stability, limited portability, incompatibility with capsule materials, and relatively restricted storage conditions. Thus the main purpose of our study was to develop a promising solid lipid-based drug delivery system (S-SEDDS) for OA. The S-SEDDS, prepared from wet granulation with an optimized L-SEDDS formulation and mannitol, was characterized by particle size analysis, scanning electron microscopy, differential scanning calorimetry, and X-ray powder diffraction. Finally, the solubility of the OA-loaded S-SEDDS was compared with that of OA powder in the dissolution assay. Our new S-SEDDS for OA was developed from the optimum L-SEDDS with ethyl oleate (oil phase), Labrasol (surfactant), and Transcutol P (cosurfactant) at a volume ratio of 15:71:14 with 1.5% w/v OA and mannitol. The dissolution of OA was improved by 60% compared with that of the pure OA powder. All the problems associated with the L-SEDDS were resolved. The methodologies we developed for OA delivery could also be utilized for the delivery of other drugs with the S-SEDDS.

Formulation Strategies to Improve the Bioavailability of Poorly Absorbed Drugs with Special Emphasis on Self-Emulsifying Systems

Poorly water-soluble drug candidates are becoming more prevalent. It has been estimated that approximately 60–70% of the drug molecules are insufficiently soluble in aqueous media and/or have very low permeability to allow for their adequate and reproducible absorption from the gastrointestinal tract (GIT) following oral administration. Formulation scientists have to adopt various strategies to enhance their absorption. Lipidic formulations are found to be a promising approach to combat the challenges. In this review article, potential advantages and drawbacks of various conventional techniques and the newer approaches specifically the self-emulsifying systems are discussed. Various components of the self-emulsifying systems and their selection criteria are critically reviewed. The attempts of various scientists to transform the liquid self-emulsifying drug delivery systems (SEDDS) to solid-SEDDS by adsorption, spray drying, lyophilization, melt granulation, extrusion, and so forth to formulate various dosage forms like self emulsifying capsules, tablets, controlled release pellets, beads, microspheres, nanoparticles, suppositories, implants, and so forth have also been included. Formulation of SEDDS is a potential strategy to deliver new drug molecules with enhanced bioavailability mostly exhibiting poor aqueous solubility. The self-emulsifying system offers various advantages over other drug delivery systems having potential to solve various problems associated with drugs of all the classes of biopharmaceutical classification system (BCS).

Preparation and in vitro evaluation of rutin nanostructured liquisolid delivery system

Poor aqueous solubility of chemical entities presents a major challenge to modern drug delivery, because of their low bioavailability. Our aim was to prepare and evaluate a suitable solid self-emulsifying drug delivery system (SSEDDS) as a potential carrier for rutin. After screening of various vehicles (surfactants, co-surfactants and oils) and selection of those having the better drug solubilizing power, liquid SEDDS were formulated. Prepared formulations were evaluated for self-emulsifying ability and phase diagrams were constructed to optimize the systems. System (S6), prepared from Triton/Acconon/Labrafac, attained highest drug solubilization capacity, hence, was selected for the preparation of SSEDDS by adsorption on different nano-structured carriers (Neusilin®, Fujicalin® and F-melt®) in different ratios. S6 had a very small particle size of 4.849±0.001nm and a high percentage transmittance of 99.31±0.16%. SSEDDS showing good flow properties as well as reasonable drug loading capacity were selected for in vitro drug release studies. The SSEDDS (SS4) composed of Neusilin® US2: S6 (1:2) attained the best drug release properties and was subjected to further characterization (SEM, FTIR and XRD). Conclusion: The optimized liquisolid dosage form of rutin provided good flowability as well as fast drug release properties and, therefore, can be suitable for oral delivery system.

Preparation of Solid Self-Emulsifying Drug Delivery System of Manidipine Hydrochloride

The ability of self-emulsifying drug delivery system (SEDDS), which is a mixture of oils, surfactants and co-surfactants, to improve dissolution rate of a poorly water-soluble drug, manidipine hydrochloride (MDP), was evaluated in this study. Liquid form of SEDDS containing caprylic/capric glyceride, polyoxyl 35 castor oil, and diethylene glycol monoethyl ether at a weight ratio of 1:1:8 was converted to solid SEDDS by adsorption on to different solid carriers, i.e., Aerosil® 200 and Sylysia® 320. The results demonstrated that the solid carrier of at least 50% (w/w) was required to adsorb liquid SEDDS containing MDP. The results from powder X-ray diffraction, differential scanning colorimetry and scanning electron microscopy showed that MDP in solid SEDDS formulations was in amorphous form while a crystalline form was observed only in MDP raw material and its physical mixture. The in vitro dissolution of MDP from solid SEDDS using Sylysia® 320 was higher than that using Aerosil® 200 as a solid carrier. In summary, the solid SEDDS could be used as a carrier to improve the dissolution of MDP, a poorly water-soluble drug.

Development and characterization of liquid and solid self-emulsifying drug delivery system of fexofenadine

Fexofenadine, the active metabolite of terfenadine, a well known and effective H1 receptor antagonist, is administered by the oral route. The objective of present investigation was to develop and characterize a liquid self-emulsifying drug delivery system (SEDDS) and a solid SEDDS by using bioenhancer excipients like Tween 80 and Labrasol which are known for their inhibiting action on CYP450 and P-glycoprotein pump. Solubility of fexofenadine was determined in various vehicles, including oils, surfactants and co-solvents. Various evaluation parameters (emulsification study, particle size, poly-dispersibility index, % drug release, etc.) were carried out to find out optimized liquid SEDDS formulation. Optimized liquid formulations were converted in solid SEDDS by simple and convenient physical adsorption technique. Solid SEDDS was characterized by X-ray diffraction (XRD), differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and Fourier transport infra-red spectroscopy. The optimized liquid SEDDS formulation contained 29 % Captex 200P/Capmul MCM C8 EP as oil, 47 % Labrasol/Tween 80 as a surfactant and 24 % Ethanol as a co-solvent. The optimized liquid and solid SEDDS showed higher drug release than pure API powder. DSC and XRD results of solid SEDDS confirmed that the drug presented in the formulation was in an amorphous state. The prepared liquid SEDDS and solid SEDDS containing bio-enhancer excipients increased the in vitro dissolution rate of fexofenadine compared to pure drug and has potential to increase bioavailability by blocking Pgp efflux pump and CYP450 hepatic metabolism.