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).

/pdf/formulation-strategies-to-improve-the-bioavailability-of-2bplkm215z.pdf

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

Oral route still remains the favorite route of drug administration in many diseases and till today it is the first way investigated in the development of new dosage forms. The major problem in oral drug formulations is low and erratic bioavailability, which mainly results from poor aqueous solubility. This may lead to high inter- and intra subject variability, lack of dose proportionality and therapeutic failure. It is estimated that 40% of active substances are poorly soluble in water. The improvement of bio-availability of drugs with such properties presents one of the greatest challenges in drug formulations. Various technological strategies are reported in the literature including micronization, solid dispersions or cyclodextrines complex formation and different technologies of drug delivery systems. Among various approach selfemulsifying drug delivery system has gained more attention due to enhanced oral bio-availability enabling reduction in dose, more consistent temporal profiles of drug absorption, selective targeting of drug(s) toward specific absorption window in GIT, and protection of drug(s) from the hostile environment in gut.

Self Emulsifying Drug Delivery System: A Review

Formulating poly(lactide-co-glycolide) particles for plasmid DNA delivery

Self-microemulsifying drug-delivery system (SMEDDS) can be defined as an isotropic system containing lipid and surfactant as well as cosurfactant that develop an emulsion in the aqueous fluid after slight agitation. Nearly half of the newly synthesized chemical molecules show less solubility in the aqueous phase, which is the major concern to the efficient delivery of drug molecules and hence decrease the bioavailability of these entities. In addition, SMEDDSs are considered as a prominent platform in resolving poor bioavailability of hydrophobic drugs through oral delivery. However, traditional self-emulsifying systems that are being developed using a liquid phase may exhibit few disadvantages such as in vivo precipitation of bioactive molecules, product handling problems, and restricted lymphatic transport. Moreover, these limitations restrict their prominent applications. In this context the addition of distinct polymeric precipitation inhibitors may facilitate the keeping of the drug in supersaturation state. Furthermore, solid-SMEDDS assist in combating both handling of liquid as well as stability-related issues. In addition the incorporation of medium-chain triglycerides along with antioxidants may also reduce oxidation-related issues of some unsaturated fatty acids. This chapter details in-depth report on distinct kinds of SMEDDS-based formulations via various route, dosage forms, composition, characterization, and their applications.

Self-microemulsifying drug-delivery system: ongoing challenges and future ahead

Lipophilic drugs can be solublized to increase the bioavailability by using several methods as microemulsion, nanosuspension, liposome, solid lipid nanoparticles (SLN), self e mulsifying drug delivery system (SEDDS), complexation with cyclodextrin etc. SEDDS has received particular attention as a means of enhancing the oral bioavailability of poorly absorbed drugs. SEDDS are liquid to semisolid in nature, but it has drawbacks as formulation development, quality control, stability etc. These liquid SEDDS can be converted into solid dosage form w ithout affecting drug release property. After administering the drug gets released and self emulsify in the GI tract.

/pdf/newer-approches-to-self-emulsifying-drug-delivery-system-tu0jct969y.pdf

Newer approches to self emulsifying drug delivery system

In this study, we constructed a novel drug delivery system for realizing the combination of gene therapy and chemotherapy by co-loading 5-FU and antisense EGFR (epidermal growth factor receptor) plasmids in biodegradable PLGA/O-CMC (O-carboxmethyl-chitosan) nanoparticles. This novel kind of nanoparticle was characterized by dynamic light scattering for size, size distribution and zeta potential, and scanning electron microscopy (SEM) and transmission electronic microscopy (TEM) for morphological properties and structures. Drug encapsulation efficiency and drug release kinetics under in vitro conditions were also measured. At the same time, the MTT assay, the TUNEL technique and immunohistochemical staining were used to investigate the antitumor activity of these multi-functional nanoparticles on human glioma cells. It was concluded that the 5-FU and plasmid encapsulation efficiencies were as high as 94.5% and 95.7%, and the 5-FU release activity from nanoparticles could be sustained for as long as three weeks. Both the MTT assay and the TUNEL method illustrated that these multi-functional nanoparticles had cytotoxicities as high as 93.5% and could induce apoptosis in most glioma cells. Immunohistochemical staining proved that plasmids on the surface of nanoparticles could transfect gliomas cells, verified by a decline in the expression level of EGFR protein by the glioma cells. Therefore, this novel delivery system for drugs and genes provides another therapeutic pathway for cancer and needs further research.

Preparation and Evaluation of 5-FU/PLGA/Gene Nanoparticles

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Preparation and Evaluation of 5-FU/PLGA/Gene Nanoparticles