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Self-emulsifying and self-microemulsifying formulations for the oral administration of taxoids

TL;DR: The present invention relates to novel formulations of taxoids for oral administration that are self-emulsifying and self-microemulsify formulations for the oral administration of taxoid formulations.
Abstract: Self-emulsifying and self-microemulsifying formulations for the oral administration of taxoids. The present invention relates to novel formulations of taxoids for oral administration.
Citations
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Journal ArticleDOI
TL;DR: The SEDDS offers the benefit of a protective effect against the hostile environment in the gut, and the unique fabrication techniques provide specific strategy to overcome the low bioavailability and poor solubility problems.
Abstract: Introduction: Oral administration of a drug is the most common, ideal and preferred route of administration. The main problem of oral drug formulations is their low bioavailability arises from poor aqueous solubility of drug. Aqueous solubility of lipophilic drugs can be improved by various techniques like salt formation, complexation, addition of co-solvent etc. but self-emulsifying drug-delivery system (SEDDS) is getting more attention for increasing the solubility of such drugs. The SEDDS is an isotropic mixture of drug, lipids, and emulsifiers, usually with one or more hydrophilic co-solvents/co-emulsifiers. This system is having ability to generate oil-in-water (o/w) emulsions or microemulsions upon gentle agitation followed by dilution with aqueous phase. The SEDDSs are relatively newer, lipid-based technological innovations possessing unparalleled potential in improving oral bioavailability of poorly water-soluble drugs.Areas covered: This review provides updated information regarding the types of SEDDS, their preparation techniques, drug delivery and related recent patents along with marketed formulations.Expert opinion: The SEDDS has been explored for improving bioavailability, rising intra-subject heterogeneity, and increasing solubility. SEDDS offers the benefit of a protective effect against the hostile environment in the gut. The unique fabrication techniques provide specific strategy to overcome the low bioavailability and poor solubility problems.

29 citations

Book ChapterDOI
25 Oct 2019
TL;DR: The present literature gives exhaustive information on the formulation design and characterization of self-microemulsifying systems, which are proved as highly useful technological innovations to vanquish low oral bioavailability problem with hydrophobic drugs.
Abstract: Oral route is preferred for drug administration; however according to the recent scenario 40% of new drug candidates have poor water solubility and low bioavailability. One of the biggest challenges in drug delivery science is to improve low oral bioavailability problem which is associated with the hydrophobic drugs due to their unprecedented potential as a drug deliver with the broad range of application. Self-emulsifying systems have been proved as highly useful technological innovations to vanquish such bioavailability problem by virtue of their diminutive globule size, higher solubilization tendency for hydrophobic drugs, robust formulation advantages, and easy to scale up. Self-microemulsifying systems are isotropic mixers of oil, surfactant, drug and co-emulsifier or solubilizer, which spontaneously form transparent micro-emulsions with oil droplets ranging between 100 and 250 nm. Micro emulsified drug can be easily absorbed through the lymphatic pathway and it bypasses the hepatic first-pass effect. Self-microemulsifying system is a thermodynamically stable system and overcomes the drawback of layering of emulsions after sitting for a long period of time. The present literature gives exhaustive information on the formulation design and characterization of self-microemulsifying systems.

4 citations

References
More filters
Journal ArticleDOI
TL;DR: The SEDDS offers the benefit of a protective effect against the hostile environment in the gut, and the unique fabrication techniques provide specific strategy to overcome the low bioavailability and poor solubility problems.
Abstract: Introduction: Oral administration of a drug is the most common, ideal and preferred route of administration. The main problem of oral drug formulations is their low bioavailability arises from poor aqueous solubility of drug. Aqueous solubility of lipophilic drugs can be improved by various techniques like salt formation, complexation, addition of co-solvent etc. but self-emulsifying drug-delivery system (SEDDS) is getting more attention for increasing the solubility of such drugs. The SEDDS is an isotropic mixture of drug, lipids, and emulsifiers, usually with one or more hydrophilic co-solvents/co-emulsifiers. This system is having ability to generate oil-in-water (o/w) emulsions or microemulsions upon gentle agitation followed by dilution with aqueous phase. The SEDDSs are relatively newer, lipid-based technological innovations possessing unparalleled potential in improving oral bioavailability of poorly water-soluble drugs.Areas covered: This review provides updated information regarding the types of SEDDS, their preparation techniques, drug delivery and related recent patents along with marketed formulations.Expert opinion: The SEDDS has been explored for improving bioavailability, rising intra-subject heterogeneity, and increasing solubility. SEDDS offers the benefit of a protective effect against the hostile environment in the gut. The unique fabrication techniques provide specific strategy to overcome the low bioavailability and poor solubility problems.

29 citations

Book ChapterDOI
25 Oct 2019
TL;DR: The present literature gives exhaustive information on the formulation design and characterization of self-microemulsifying systems, which are proved as highly useful technological innovations to vanquish low oral bioavailability problem with hydrophobic drugs.
Abstract: Oral route is preferred for drug administration; however according to the recent scenario 40% of new drug candidates have poor water solubility and low bioavailability. One of the biggest challenges in drug delivery science is to improve low oral bioavailability problem which is associated with the hydrophobic drugs due to their unprecedented potential as a drug deliver with the broad range of application. Self-emulsifying systems have been proved as highly useful technological innovations to vanquish such bioavailability problem by virtue of their diminutive globule size, higher solubilization tendency for hydrophobic drugs, robust formulation advantages, and easy to scale up. Self-microemulsifying systems are isotropic mixers of oil, surfactant, drug and co-emulsifier or solubilizer, which spontaneously form transparent micro-emulsions with oil droplets ranging between 100 and 250 nm. Micro emulsified drug can be easily absorbed through the lymphatic pathway and it bypasses the hepatic first-pass effect. Self-microemulsifying system is a thermodynamically stable system and overcomes the drawback of layering of emulsions after sitting for a long period of time. The present literature gives exhaustive information on the formulation design and characterization of self-microemulsifying systems.

4 citations