Solid Self-emulsifying Delivery System Research Articles

Encapsulation of tuna oil by liquid and solid self‐emulsifying delivery system: in vitro digestion and oxidative stability assessment

SummaryTuna oil, one of the main sources of omega‐3 polyunsaturated fatty acids (omega‐3 or n‐3 PUFAs), is known to have limited bioavailability due to its hydrophobicity. Moreover, the main n‐3 PUFAs found in tuna oil, that is docosahexaenoic acid (DHA) and eicosapentaenoic acid (EPA) are prone to oxidation. To overcome these drawbacks, tuna oil encapsulation via liquid (LSEDS) and solid self‐emulsifying delivery system (SSEDS) was developed. Different LSEDS formulations were prepared and evaluated in terms of tuna oil droplet size and dispersibility. Accordingly, the formulation with small droplets size and narrow size distribution was selected and further developed into SSEDS by spray drying process. SSEDS was thereafter characterised concerning production yield, moisture content, size, size distribution and morphology. Furthermore, the in vitro simulated gastrointestinal model of LSEDS and SSEDS was carried out. The results showed that after intestinal digestion stage, 87% and 72% of DHA were released from LSEDS and SSEDS, respectively. Therefore, these formulations of LSEDS and SSEDS were proven their ability to enhance the bioaccessibility of DHA. Moreover, the oxidative stability of LSEDS and SSEDS formulation was investigated and compared to pure tuna oil using non‐isothermal differential scanning calorimetry (DSC) analysis under oxygen. The results showed that both LSEDS and SSEDS formulations exhibited a high oxidative resistance with a higher energy needed to induce tuna oil oxidation than pure tuna oil. The chemical and thermal stability given by LSEDS and SSEDS may be efficiently applied in food area to enhance the techno‐functional properties of hydrophobic compounds.

Comparative Study of Powder Carriers Physical and Structural Properties.

High specific surface area (SSA), porous structure, and suitable technological characteristics (flow, compressibility) predetermine powder carriers to be used in pharmaceutical technology, especially in the formulation of liquisolid systems (LSS) and solid self-emulsifying delivery systems (s-SEDDS). Besides widely used microcrystalline cellulose, other promising materials include magnesium aluminometasilicates, mesoporous silicates, and silica aerogels. Clay minerals with laminar or fibrous internal structures also provide suitable properties for liquid drug incorporation. This work aimed at a comparison of 14 carriers’ main properties. Cellulose derivatives, silica, silicates, and clay minerals were evaluated for flow properties, shear cell experiments, SSA, hygroscopicity, pH, particle size, and SEM. The most promising materials were magnesium aluminometasilicates, specifically Neusilin® US2, due to its proper flow, large SSA, etc. Innovative materials such as FujiSil® or Syloid® XDP 3050 were for their properties evaluated as suitable. The obtained data can help choose a suitable carrier for formulations where the liquid phase is incorporated into the solid dosage form. All measurements were conducted by the same methodology and under the same conditions, allowing a seamless comparison of property evaluation between carriers, for which available company or scientific sources do not qualify due to different measurements, conditions, instrumentation, etc.

LIPID BASED SOLID SELF-EMULSIFYING DELIVERY SYSTEM OF PITAVASTATIN CALCIUM: DEVELOPMENT AND CHARACTERIZATION

Solid self-emulsifying delivery system containing pitavastatin calcium was developed using oil and hydrophilic surfactants. Pitavastatin calcium has low solubility and low bioavailability; hence, it was meaningful to improve solubility and dissolution properties by using suitable formulation component and process. Based on preliminary study, oleic acid, Tween 20 and PEG 400 were utilized for development of self-emulsifying system. Microemulsion region was identified by pseudo-ternary phase diagrams. The liquid system: adsorbent (Aerosil 200) at a ratio of 2:1 was employed for spray drying. The system was evaluated for emulsification time, percent drug content, in-vitro dissolution. The other analytical techniques used for characterization were FTIR, DSC, SEM, particle size, zeta potential and XRD. The optimized formulation had particle size of 172.2 nm and the drug content found was 96.38%. It also had shown 95.98% drug release at the end of 1 hr which was more when compared to pure drug. It was observed that increase in surfactant concentration decreases dispersion time and particle size with concomitant increase in amount of drug released. The XRD diffractogram confirmed the conversion of drug from crystalline to amorphous form. The spray dried particles had smoother surface. The DSC thermogram showed no melting endotherm in the system indicating well dispersed drug with amorphous nature.

Cover Caption

May Online Cover: A novel method to create a solid emulsion delivery system, from Feature Article “Solid Self‐Emulsifying Delivery System (S‐SEDS) of Dihydromyricetin: A New Way for Preparing Functional Food” by Dantong Wang, Yudi Ma, Qiang Wang, Juan Huang, Rui Sun, and Qiang Xia. p. 936.

A novel solid self-emulsifying delivery system (SEDS) for the encapsulation of linseed oil and quercetin: Preparation and evaluation

The aim of current research was to develop a solid self-emulsifying delivery system (SEDS) to enhance the delivery of linseed oil and quercetin. The pseudo ternary phase diagram was constructed to optimize the suitable liquid formulation. Liquid absorption on solid absorbent carrier was used to convert liquid into solid self-emulsifying lipid formulation by simple physical mixture. The solid carrier of Aerosil 300 showed highest adsorption capacity. Besides, the solid SEDS prepared with liquid formulation/Aerosil 300 ratio of 2:1 had good flow properties. FTIR indicated that linseed oil and quercetin were encapsulated in Aerosil 300. XRD study suggested that the crystalline structure of quercetin transformed to molecularly dissolved state in solid SEDS. In vitro digestion and release experiments showed that after solid adsorption, linseed oil and quercetin exhibited delayed release patterns. The accelerated oxidation study revealed that non aqueous system was more beneficial to the storage of linseed oil, and Aerosil 300 had no effect on the oxidation stability of linseed oil. Hence, solid SEDS is an attractive candidate for the encapsulation of functional oil and flavonoids for use in food industry.

Spray-Dried Solid Self-Emulsifying Delivery System of Ketoprofen: Development and Its Characterization

Ketoprofen is classified as BCS class II drug with low aqueous solubility, short half-life (2–2.5 h), and low oral bioavailability and also causes gastric irritation. The systems intended for oral administration were prepared by using soybean oil, Cremophor EL, and Maisine 35-1 and its adsorption on Aerosil 200. The spray-dried product demonstrated high process yield (52.2–68.3%) with good loading capacity (83.13–93.69%) and significant drug release compared to pure drug. The smooth spherical particles produced had no interaction with the excipients as demonstrated by scanning electron microscopy (SEM) and Fourier transform infrared (FTIR). Differential scanning calorimetry (DSC) indicated the complete miscibility of the drug with excipients and X-ray diffraction (XRD) demonstrated the transformation from crystalline to amorphous form.