Online citations, reference lists, and bibliographies.
← Back to Search

Formulation Strategies To Improve The Bioavailability Of Poorly Absorbed Drugs With Special Emphasis On Self-Emulsifying Systems

S. Gupta, Rajesh Kesarla, Abdelwahab Omri
Published 2013 · Medicine

Cite This
Download PDF
Analyze on Scholarcy
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).
This paper references
In vitro and in vivo evaluation of an amylobarbitone/hydroxypropyl-beta-cyclodextrin complex prepared by a freeze-drying method.
M. Fathy (2000)
Enhancement of the stability of BCNU using self-emulsifying drug delivery systems (SEDDS) and in vitro antitumor activity of self-emulsified BCNU-loaded PLGA wafer.
Gang Soo Chae (2005)
Charge-dependent interaction of self-emulsifying oil formulations with Caco-2 cells monolayers: binding, effects on barrier function and cytotoxicity.
T. Gershanik (2000)
Cryoprotection of emulsions in freeze-drying : freezing process analysis
J. Bamba (1995)
Solid dispersion of poorly water-soluble drugs: early promises, subsequent problems, and recent breakthroughs.
A. T. Serajuddin (1999)
Development and bioavailability assessment of ramipril nanoemulsion formulation.
S. Shafiq (2007)
Identification and molecular interpretation of the effects of drug incorporation on the self-emulsification process using spectroscopic, micropolarimetric and microscopic measurements.
A Mercuri (2012)
Excipient effects on in vitro cytotoxicity of a novel paclitaxel self-emulsifying drug delivery system.
Neslihan Gursoy (2003)
Oral lipid-based formulations : enhancing the bioavailability of poorly water-soluable drugs
D. Hauss (2007)
Enhancement of griseofulvin release from liquisolid compacts.
C. M. Hentzschel (2012)
Oral bioavailability of silymarin phytocomplex formulated as self-emulsifying pellets.
T. Iosio (2011)
In vitro and in vivo evaluation of an amylobarbitone/hydroxypropyl--cyclo-dextrin complex prepared by a freeze-drying method
M Fathy (2000)
Hot Melt Extrusion with BASF Pharma Polymers—Extrusion Compendium, Pharma Ingredients and Services
K Kolter (2012)
의약품의 Solid Lipid Nanoparticle의 제조 및 용출특성
유혜종 (1996)
Study of the preparation of sustained-release microspheres containing zedoary turmeric oil by the emulsion-solvent-diffusion method and evaluation of the self-emulsification and bioavailability of the oil.
Jian You (2006)
Design and optimization of a new self-nanoemulsifying drug delivery system.
L. Wang (2009)
Formulation of a self-emulsifying system for oral delivery of simvastatin: In vitro and in vivo evaluation
P. Patil (2007)
Preparation and evaluation of self-nanoemulsifying tablets of carvedilol,”AAPSPharmSciTech
E. A. Mahmoud (2009)
Modification of physicochemical characteristics of active pharmaceutical ingredients and application of supersaturatable dosage forms for improving bioavailability of poorly absorbed drugs.
K. Kawakami (2012)
Medium-chain versus long-chain triacylglycerol emulsion hydrolysis by lipoprotein lipase and hepatic lipase: implications for the mechanisms of lipase action.
R. Deckelbaum (1990)
Oral self emulsifying powder of lercanidipine hydrochloride: Formulation and evaluation
Venkata Raman Kallakunta (2012)
A new solid self-microemulsifying formulation prepared by spray-drying to improve the oral bioavailability of poorly water soluble drugs.
T. Yi (2008)
Self-emulsifying pellets in a lab-scale high shear mixer: Formulation and production design
Erica Franceschinis (2011)
Design and evaluation of self-nanoemulsifying drug delivery systems (SNEDDS) for cefpodoxime proxetil.
A. Date (2007)
Preparation and evaluation of 5-FU/PLGA/gene nanoparticles,”Key EngineeringMaterials
H. Yunxia (2005)
A Review on Micronization Techniques
Jalay T. Joshi (2011)
Enhancement of the oral bioavailability of cinnarizine in oleic acid in beagle dogs.
T. Tokumura (1987)
Enhanced oral bioavailability of dexibuprofen by a novel solid self-emulsifying drug delivery system (SEDDS).
P. Balakrishnan (2009)
Self-nanoemulsifying drug delivery systems of tamoxifen citrate: design and optimization.
Y. Elnaggar (2009)
Floating Alginate Beads as Carriers for Self-Emulsifying System Containing Tetrahydrocurcumin
Supatsa Sriraksa (2012)
A Novel Nanoparticle Formulation for Sustained Paclitaxel Delivery
W. Trickler (2008)
An investigation into the physico-chemical properties of self-emulsifying systems using low frequency dielectric spectroscopy, surface tension measurements and particle size analysis
D. Craig (1993)
Self-double-emulsifying drug delivery system (SDEDDS): a new way for oral delivery of drugs with high solubility and low permeability.
X. Qi (2011)
Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and 'self-microemulsifying' drug delivery systems.
C. Pouton (2000)
Enhancement of dissolution of glyburide by solid dispersion and lyophilization techniques
G. Betageri (1995)
Solubilizing Excipients in Oral and Injectable Formulations
R. Strickley (2004)
Enhancement of Naringenin Bioavailability by Complexation with Hydroxypropoyl-β-Cyclodextrin
Maria Shulman (2011)
Enhancement of the Dissolution and Permeation Rates of Meloxicam by Formation of Its Freeze-dried Solid Dispersions in Polyvinylpyrrolidone K-30
M. El-Badry (2006)
Optimized nanoemulsifying systems with enhanced bioavailability of carvedilol.
B. Singh (2013)
C. Solans (2005)
Self-nanoemulsifying drug delivery system for adefovir dipivoxil: Design, characterization, in vitro and ex vivo evaluation
S. Gupta (2011)
Enhanced absorption of indomethacin after oral or rectal administration of a self-emulsifying system containing indomethacin to rats.
J. Kim (2000)
Development and characterization of solid lipid nanoparticles for enhancement of oral bioavailability of Raloxifene
B. Patel (2012)
Intestinal permeation enhancers.
B. Aungst (2000)
Gryczke, Hot Melt Extrusion with BASF Pharma Polymers—Extrusion Compendium
K. Kolter (2012)
Oral Lipid-Based Formulations: Enhancing the Bioavailability of Poorly Water-Soluble Drugs
J. Dressman (2007)
Enhanced bioavailability of nano-sized chitosan-atorvastatin conjugate after oral administration to rats.
M. Anwar (2011)
Melt extrusion-based dosage forms: Excipients and processing conditions for pharmaceutical formulations
G. Verreck (2004)
Proposal of stability categories for nano-dispersions obtained from pharmaceutical self-emulsifying formulations.
Andreas Niederquell (2013)
Supersaturated Self-Nanoemulsifying Drug Delivery Systems (Super-SNEDDS) Enhance the Bioavailability of the Poorly Water-Soluble Drug Simvastatin in Dogs
N. Thomas (2012)
In vitro evaluation of drug release from self micro-emulsifying drug delivery systems using a biodegradable homolipid from Capra hircus.
A. Attama (2005)
Self-emulsifying drug delivery systems (SEDDS) of coenzyme Q10: formulation development and bioavailability assessment.
T. R. Kommuru (2001)
Effect of formulation variables on preparation and evaluation of gelled self-emulsifying drug delivery system (SEDDS) of ketoprofen
P. Patil (2008)
Entropy-induced dispersion of bulk liquids
H. Reiss (1975)
Preparation and Evaluation of 5-FU/PLGA/Gene Nanoparticles
Y. Hu (2005)
Self-emulsifying systems for oral delivery of drugs
C. W. Pouton (1987)
Development of docetaxel-loaded solid self-nanoemulsifying drug delivery system (SNEDDS) for enhanced chemotherapeutic effect.
Youn Gee Seo (2013)
Nanosizing: a formulation approach for poorly-water-soluble compounds.
E. Merisko-Liversidge (2003)
Amorphous drug delivery systems: molecular aspects, design, and performance.
A. Kaushal (2004)
Intestinal Lymphatic Transport of Halofantrine Occurs After Oral Administration of a Unit-Dose Lipid-Based Formulation to Fasted Dogs
Shui-Mei Khoo (2004)
Solid lipid nanoparticles
W. Mehnert (2012)
Formulation and production of rapidly disintegrating tablets by lyophilisation using hydrochlorothiazide as a model drug.
S. Corveleyn (1997)
Enhanced bioavailability and retinal accumulation of lutein from self-emulsifying phospholipid suspension (SEPS).
S. K. S. Shanmugam (2011)
Selfnanoemulsifying drug delivery systems of tamoxifen citrate: design and optimization
Y.S.R. Elnaggar (2009)
In vitro and in vivo evaluation of an amylobarbitone/hydroxypropyl-í µí»½-cyclo-dextrin complex prepared by a freeze-drying method
M Fathy (2000)
Preparation and characterization of emulsifiable glasses: Oil-in-water and water-in-oil-in-water emulsions
S. Myers (1992)
Oral solid gentamicin preparation using emulsifier and adsorbent.
Y. Ito (2005)
Preparation and characterization of a self-emulsifying pellet formulation.
Ahmed Abdalla (2007)
Solid dispersions: revival with greater possibilities and applications in oral drug delivery.
S. Sethia (2003)
Intestinal Permeability Enhancement: Efficacy, Acute Local Toxicity, and Reversibility
E. S. Swenson (2004)
Lipid Microemulsions for Improving Drug Dissolution and Oral Absorption: Physical and Biopharmaceutical Aspects
P. Constantinides (2004)
Preparation and in vitro characterization of a eutectic based semisolid self-nanoemulsified drug delivery system (SNEDDS) of ubiquinone: mechanism and progress of emulsion formation.
S. Nazzal (2002)
Formulation of poorly water-soluble drugs for oral administration: physicochemical and physiological issues and the lipid formulation classification system.
C. Pouton (2006)
Identification and molecular interpretation of the effects of drug incorporation on the self - emulsification process using spectroscopic , micropo - larimetric andmicroscopic measurements
P. S. Belton
Self-emulsification of vegetable oil-nonionic surfactant mixtures: a proposed mechanism of action
M. Wakerly (1986)
Lipid-based delivery systems for improving the bioavailability and lymphatic transport of a poorly water-soluble LTB4 inhibitor.
D. Hauss (1998)
Preparation and evaluation of self-microemulsifying drug delivery system of oridonin.
Ping Zhang (2008)
Comparison of solid self-microemulsifying drug delivery system (solid SMEDDS) prepared with hydrophilic and hydrophobic solid carrier.
Dong Hoon Oh (2011)
Identification and molecular interpretation of the effects of drug incorporation on the self - emulsification process using spectroscopic , micropo - larimetric andmicroscopic measurements
A. Mercuri (2012)
Identification and molecular interpretation of the effects of drug incorporation on the self-emulsification process using spectroscopic, micropolarimetric andmicroscopic measurements,”Molecular
A. Mercuri (2012)
Enhanced Intestinal Absorption of Cyclosporine in Rats Through the Reduction of Emulsion Droplet Size
B. Tarr (2004)
Lipophilic 1-β-d-arabinofuranosyl cytosine derivatives in liposomal formulations for oral and parenteral antileukemic therapy in the murine L1210 leukemia model
R. Schwendener (2005)
Formulation and Antitumor Activity Evaluation of Nanocrystalline Suspensions of Poorly Soluble Anticancer Drugs
E. Merisko-Liversidge (2004)
Classification of orally administered drugs on the World Health Organization Model list of Essential Medicines according to the biopharmaceutics classification system.
Marc Lindenberg (2004)
Controlled drug release from pellets containing water-insoluble drugs dissolved in a self-emulsifying system.
M. Serratoni (2007)
Investigations of a Novel Self-Emulsifying Osmotic Pump Tablet Containing Carvedilol
L. Wei (2007)
Pouton, “Formulation of self-emulsifying drug delivery systems,”Advanced
C W. (1997)
Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs.
R. N. Gursoy (2004)
Lipid-based formulations for intestinal lymphatic delivery.
C. O'Driscoll (2002)
Self-Nanoemulsifying Drug Delivery System of Glimepiride: Design, Development, and Optimization
Sunny R Shah (2013)
An investigation into the mechanisms of self-emulsification using particle size analysis and low frequency dielectric spectroscopy
D. Craig (1995)
Porous polystyrene beads as carriers for self-emulsifying system containing loratadine
P. Patil (2008)
Self-emulsifying drug delivery systems: assessment of the efficiency of emulsification
C. Pouton (1985)
Effect of vehicle amphiphilicity on the dissolution and bioavailability of a poorly water-soluble drug from solid dispersions.
A. T. Serajuddin (1988)
Development of a supersaturable SEDDS (S-SEDDS) formulation of paclitaxel with improved oral bioavailability.
Ping Gao (2003)
Formulation of self-emulsifying drug delivery systems
C. Pouton (1997)
Preparation and Evaluation of Self-nanoemulsifying Tablets of Carvedilol
E. Mahmoud (2009)
Improvement of physicochemical properties of N-4472 part I formulation design by using self-microemulsifying system.
K. Itoh (2002)
Improvement of cefpodoxime proxetil oral absorption in rats by an oil-in-water submicron emulsion.
G. Nicolaos (2003)
Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings.
C. Lipinski (2001)
Drug-like properties and the causes of poor solubility and poor permeability.
C. Lipinski (2000)
Self-dispersing lipid formulations for improving oral absorption of lipophilic drugs.
T. Gershanik (2000)
Enhanced dissolution of celecoxib by supersaturating self-emulsifying drug delivery system (S-SEDDS) formulation
W. Song (2013)
Self-emulsifying drug delivery systems (SEDDS) with polyglycolyzed glycerides for improving in vitro dissolution and oral absorption of lipophilic drugs
N. Shah (1994)
Bioavailability of probucol from lipid and surfactant based formulations in minipigs: influence of droplet size and dietary state.
F. S. Nielsen (2008)
Self-Microemulsifiyng Suppository Formulation of β-Artemether
Dalapathi B Gugulothu (2010)
Self emulsification of vegetable oil-non-ionic surfactant mixtures
M. G. Wakerly (1986)
In vitro and in vivo evaluation of an amylobarbitone/hydroxypropyl-β- cyclo-dextrin complex prepared by a freeze-drying method
M. Fathy (2000)
Hot Melt Extrusion with BASF Pharma Polymers-Extrusion Compendium
K Kolter (2012)

This paper is referenced by
Formulation and Cytotoxic Characterization of Trigonella foenum Loaded Polymeric Nanoparticles
Bire Priyanka (2020)
Physiologically-based pharmacokinetic models: approaches for enabling personalized medicine
Clara Hartmanshenn (2016)
Variability in bioavailability of small molecular tyrosine kinase inhibitors.
M. Herbrink (2015)
Optimization of self-nanoemulsifying formulations for weakly basic lipophilic drugs: role of acidification and experimental design
A. Shahba (2016)
Development and evaluation of self-nanoemulsifying drug delivery systems for oral delivery of indomethacin
Basmah Nasser Abdullah Aldosari (2018)
Herbal Drug Use In Sickle Cell Disease Management; Trends And Perspectives In Sub-Saharan Africa.
M. P. Okoh (2018)
Dermal application of lactic acid based cream of a non pathogenic Kocuria marina (BMKO1) strain against Epidermophyton floccosum (MTCC 613) symptomatic excision mice model
S. S. Dash (2019)
Development of rectal self-emulsifying suspension of a moisture-labile water-soluble drug.
T. Kauss (2018)
Nicotinamide polymeric nanoemulsified systems: a quality-by-design case study for a sustained antimicrobial activity
Ahmed Samir Zidan (2016)
Novel tablet formulation of amorphous indomethacin using wet granulation with a high-speed mixer granulator combined with porous calcium silicate
Yumi Fujimoto (2016)
Microemulsions and Nanoemulsions as Carriers for Delivery of NSAIDs
Ljiljana Đekić (2017)
Encapsulation of bioactive compounds using nanoemulsions
D. H. Lohith Kumar (2017)
Micro-Nano formulation of bile-gut delivery: rheological, stability and cell survival, basal and maximum respiration studies
S. Wagle (2020)
Bioaccessibility and Antioxidant Activity of Calendula officinalis Supercritical Extract as Affected by in Vitro Codigestion with Olive Oil.
D. Martín (2016)
Design and Optimization of Self Nano-Emulsifying Drug Delivery System Containing a New Anti-inflammatory Agent Pentagamavunon-0 Ika
Yuni Astuti (2017)
Effect of centrifugation speed on the measured equilibrium solubility of poorly water-soluble compounds in viscous solvents
Xiaona Liu (2020)
Stabilizers used in nanocrystal based drug delivery systems
G. Shete (2014)
Formulation and characterisation of nanosuspension of herbal extracts for enhanced antiradical potential
N. Jahan (2016)
Palmitoylethanolamide sub-micronization using fast precipitation followed by supercritical fluids extraction
R. Campardelli (2017)
BRD4 PROTAC as a novel therapeutic approach for the treatment of vemurafenib resistant melanoma: Preformulation studies, formulation development and in vitro evaluation.
Drishti Rathod (2019)
Advances on the formulation of proteins using nanotechnologies
Irene Santalices (2017)
Bioavailability Enhancement of Poorly Water-Soluble Drugs via Nanocomposites: Formulation–Processing Aspects and Challenges
A. Bhakay (2018)
Iron Transport Tocopheryl Polyethylene Glycol Succinate in Animal Health and Diseases
Ajay Srivastava (2019)
Pharmacokinetics of Tetracycline and Tetracycline Loaded Nanoemulsion Formula in Rabbits
Aziza M.M. Amer (2020)
Impact of polymers on the aggregation of wet-milled itraconazole particles and their dissolution from spray-dried nanocomposites
Ecevit Bilgili (2018)
Chitosan-Based Drug Delivery Systems for Optimization of Photodynamic Therapy: a Review
G. Calixto (2019)
Preparation and characterization of sorafenib-loaded microprecipitated bulk powder for enhancing oral bioavailability.
Ju-Hwan Park (2020)
Recent Advances in Self-Emulsifying Drug-Delivery Systems for Oral Delivery of Cancer Chemotherapeutics
Ankit Saneja (2016)
Increased intestinal permeation and modulation of presystemic metabolism of resveratrol formulated into self-emulsifying drug delivery systems.
G. Mamadou (2017)
Synergistic antibacterial effects of herbal extracts and antibiotics on methicillin-resistant Staphylococcus aureus: A computational and experimental study
Chiu-Fai Kuok (2017)
Enhancement of zaleplon oral bioavailability using optimized self-nano emulsifying drug delivery systems and its effect on sleep quality among a sample of psychiatric patients
Maha K A Khalifa (2019)
Hollow pessary loaded with lawsone via self-microemulsifying drug delivery system for vaginal candidiasis
A. Pandit (2020)
See more
Semantic Scholar Logo Some data provided by SemanticScholar