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

Phospholipid Complex Enriched Micelles: A Novel Drug Delivery Approach For Promoting The Antidiabetic Effect Of Repaglinide

Ahmed Alaa Kassem, Sameh Hosam Abd El-Alim, M. Basha, A. Salama
Published 2017 · Medicine, Chemistry

Save to my Library
Download PDF
Analyze on Scholarcy
Share
Abstract To enhance the oral antidiabetic effect of repaglinide (RG), a newly emerging approach, based on the combination of phospholipid complexation and micelle techniques, was employed. Repaglinide‐phospholipid complex (RG‐PLC) was prepared by the solvent‐evaporation method then characterized using Differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT‐IR) and X‐ray powder diffraction (XPRD). The results revealed obvious disappearance of the characteristic peaks of the prepared RG‐PLCs confirming the formation of drug‐phospholipid complex. RG‐PLC enriched micelles (RG‐PLC‐Ms) were prepared by the solvent‐evaporation technique employing poloxamer 188 as surfactant. The prepared RG‐PLC‐Ms showed high drug encapsulation efficiencies (93.81–99.38%), with nanometric particle diameters (500.61–665.32 nm) of monodisperse distribution and high stability (Zeta potential < −29.8 mV). The in vitro release of RG from RG‐PLC‐Ms was pH‐dependant according to the release media. A higher release pattern was reported in pH = 1.2 compared to a more retarded release in pH = 6.8 owing to two different kinetics of drug release. Oral antidiabetic effect of two optimized RG‐PLC‐M formulations was evaluated in an alloxan‐induced diabetic rat model for 7‐day treatment protocol. The two investigated formulations depicted normal blood glucose, serum malondialdehyde and insulin levels as well as an improved lipid profile, at the end of daily oral treatment, in contrast to RG marketed tablets implying enhanced antidiabetic effect of the drug. Hence, phospholipid‐complex enriched micelles approach holds a promising potential for promoting the antidiabetic effect of RG.
This paper references
10.1166/JBN.2007.001
Dissolution Rates and Supersaturation Behavior of Amorphous Repaglinide Particles Produced by Controlled Precipitation
Prapasri Sinswat (2007)
10.1016/S2221-1691(12)60023-9
Antidiabetic effect of Merremia emarginata Burm. F. in streptozotocin induced diabetic rats.
G. R. Gandhi (2012)
10.1016/j.jphotobiol.2015.09.002
Rutin nanostructured lipid cosmeceutical preparation with sun protective potential.
R. Kamel (2015)
Protective effect of Al-hagi graecorum in alloxan- induced diabetic rats
Abeer A. A. Salama (2016)
10.1136/bmj.f1654
Coronary artery calcium score prediction of all cause mortality and cardiovascular events in people with type 2 diabetes: systematic review and meta-analysis
C. Kramer (2013)
10.1016/j.jpba.2015.05.017
Preparation and evaluation of kaempferol-phospholipid complex for pharmacokinetics and bioavailability in SD rats.
K. Zhang (2015)
10.1016/0378-5173(83)90064-9
Mechanisms of solute release from porous hydrophilic polymers
R. Korsmeyer (1983)
10.1248/YAKUSHI1947.117.12_1022
[Trial for transdermal administration of sulfonylureas].
Y. Takahashi (1997)
10.2165/11207600-000000000-00000
Repaglinide: a review of its use in type 2 diabetes mellitus.
L. Scott (2012)
10.1016/0378-5173(89)90306-2
A simple equation for the description of solute release. III. Coupling of diffusion and relaxation
N. Peppas (1989)
10.1016/j.ijpharm.2015.12.002
Influence of surfactants in self-microemulsifying formulations on enhancing oral bioavailability of oxyresveratrol: Studies in Caco-2 cells and in vivo.
Y. Sangsen (2016)
10.1007/s11095-006-9132-0
Micellar Nanocarriers: Pharmaceutical Perspectives
V. Torchilin (2006)
10.2147/IJN.S50557
Preparation and characterization of tetrandrine-phospholipid complex loaded lipid nanocapsules as potential oral carriers
Y. Zhao (2013)
10.1186/s40200-014-0119-9
Amelioration of lipid peroxidation in vivo and in vitro by Satureja khozestanica essential oil in alloxan-induced diabetic rats
H. Ahmadvand (2014)
10.3109/10717544.2012.752420
A study on ethosomes as mode for transdermal delivery of an antidiabetic drug
Siddhodhan S Bodade (2013)
10.1208/s12249-008-9057-5
Micellar Solubilization of Some Poorly Soluble Antidiabetic Drugs: A Technical Note
N. Seedher (2008)
10.1016/j.numecd.2010.10.016
The burden of hospitalization related to diabetes mellitus: a population-based study.
G. de Berardis (2012)
10.1016/J.IJPHARM.2006.01.011
Preparation, characterization and in vivo evaluation of formulation of repaglinide with hydroxypropyl-β-cyclodextrin.
Jun Liu (2006)
Synthesis , Characterization and Discovery Novel Anti-diabetic and Anti-hyperlipidemic Thiazolidinedione Derivatives
Ahmed A. El-Henawy (2015)
10.2174/1570163811310030005
Baicalein-phospholipid complex: a novel drug delivery technology for phytotherapeutics.
D. Rawat (2013)
10.1016/S0939-6411(98)00015-0
Preparation and characterization of nanoparticles containing an antihypertensive agent.
M. Leroueil-Le Verger (1998)
Phospholipid solubilization of both poorly water-soluble and poorly oil-soluble drug into oils using freeze-drying technology
L. Qin (2006)
10.1016/J.JPBA.2006.12.010
Method development and validation of repaglinide in human plasma by HPLC and its application in pharmacokinetic studies.
A. B. Ruzilawati (2007)
10.1021/jf305143k
Curcumin and genistein coloaded nanostructured lipid carriers: in vitro digestion and antiprostate cancer activity.
N. P. Aditya (2013)
10.1002/jps.22454
In vivo and cytotoxicity evaluation of repaglinide-loaded binary solid lipid nanoparticles after oral administration to rats.
M. K. Rawat (2011)
10.1208/s12249-013-9990-9
Design and Evaluation of Self-Nanoemulsifying Pellets of Repaglinide
N. Desai (2013)
10.1166/JBN.2013.1704
Micelles of TPGS modified apigenin phospholipid complex for oral administration: preparation, in vitro and in vivo evaluation.
W. L. Munyendo (2013)
10.1016/J.JOPR.2013.04.049
Preparation and characterization of repaglinide loaded ethylcellulose nanoparticles by solvent diffusion technique using high pressure homogenizer
A. Lokhande (2013)
10.1016/S2221-1691(13)60060-X
Bioavailability enhancers of herbal origin: an overview.
K. Kesarwani (2013)
10.1016/j.ijpharm.2015.07.075
Novel self-assembled nano-tubular mixed micelles of Pluronics P123, Pluronic F127 and phosphatidylcholine for oral delivery of nimodipine: In vitro characterization, ex vivo transport and in vivo pharmacokinetic studies.
E. B. Basalious (2015)
10.1016/J.AJPS.2014.06.004
A simple method to improve the dissolution of repaglinide and exploration of its mechanism
Zhaolu Zhu (2014)
10.1016/j.jconrel.2009.06.015
Hydrotropic oligomer-conjugated glycol chitosan as a carrier of paclitaxel: synthesis, characterization, and in vivo biodistribution.
G. Saravanakumar (2009)
10.1136/bmj.f165
Work stress and risk of cancer: meta-analysis of 5700 incident cancer events in 116 000 European men and women
K. Heikkilä (2013)
10.1016/j.diabet.2013.12.003
Metformin accumulation without hyperlactataemia and metformin-induced hyperlactataemia without metformin accumulation.
J. D. Lalau (2014)
10.1016/j.ijpharm.2015.04.024
Improve bile duct-targeted drug delivery and therapeutic efficacy for cholangiocarcinoma by cucurbitacin B loaded phospholipid complex modified with berberine hydrochloride.
L. Cheng (2015)
celles of TPGSmodi fi ed apigenin phospholipid complex for oral administration : preparation , in vitro and in vivo evaluation
X. Pan
10.1371/journal.pone.0084530
A New Strategy for Enhancing the Oral Bioavailability of Drugs with Poor Water-Solubility and Low Liposolubility Based on Phospholipid Complex and Supersaturated SEDDS
H. Zhou (2013)
10.1186/1472-6882-7-29
An experimental evaluation of the antidiabetic and antilipidemic properties of a standardized Momordica charantia fruit extract
Nafisa PC Fernandes (2007)
10.1016/j.jdiacomp.2009.09.007
Role of lipoic acid on insulin resistance and leptin in experimentally diabetic rats.
M. A. Kandeil (2011)
10.1155/2016/1635361
Comparative Study of the Antioxidant Effects of Metformin, Glibenclamide, and Repaglinide in Alloxan-Induced Diabetic Rats
Bonaventure Chukwunonso Obi (2016)
10.2174/156720110790396472
Development of repaglinide loaded solid lipid nanocarrier: selection of fabrication method.
M. K. Rawat (2010)
10.1186/s40199-015-0128-3
Repaglinide-loaded solid lipid nanoparticles: effect of using different surfactants/stabilizers on physicochemical properties of nanoparticles
H. Ebrahimi (2015)
10.1186/1472-6882-9-48
Evaluation of hypoglycemic and anti-hyperglycemic potential of Tridax procumbens (Linn.)
Hemant Pareek (2009)
10.1016/j.colsurfb.2010.07.029
Design and ocular tolerance of flurbiprofen loaded ultrasound-engineered NLC.
E. Gonzalez-Mira (2010)
10.1016/J.JCIS.2007.09.007
Self-assembly of β-casein and lysozyme
X. Pan (2007)
10.1016/j.jsps.2015.02.013
In-vitro and in-vivo evaluation of repaglinide loaded floating microspheres prepared from different viscosity grades of HPMC polymer
Megha Sharma (2015)
10.1016/J.JCONREL.2006.04.005
A novel calcium silicate based microspheres of repaglinide: in vivo investigations.
S. K. Jain (2006)
10.1016/J.JPBA.2006.01.056
Ionization, lipophilicity and solubility properties of repaglinide.
Z. Mandić (2006)
10.1155/2013/340315
Polymeric Micelles, a Promising Drug Delivery System to Enhance Bioavailability of Poorly Water-Soluble Drugs
W. Xu (2013)
10.3390/ijms11052056
Antioxidant Protective Effect of Glibenclamide and Metformin in Combination with Honey in Pancreas of Streptozotocin-Induced Diabetic Rats
O. O. Erejuwa (2010)
10.1016/J.JCONREL.2005.06.007
Calcium silicate based microspheres of repaglinide for gastroretentive floating drug delivery: preparation and in vitro characterization.
S. K. Jain (2005)
Alloxan stimulation and subsequent inhibition of insulin release from in situ perfused rat pancreas.
A. Kliber (1996)
10.1002/jps.22435
Studies on binary lipid matrix based solid lipid nanoparticles of repaglinide: in vitro and in vivo evaluation.
M. K. Rawat (2011)
10.1016/J.JCIS.2005.06.013
Concentration, temperature, and salt-induced micellization of a triblock copolymer Pluronic L64 in aqueous media.
J. Mata (2005)
10.1016/j.ijpharm.2014.11.059
Matrix tablets for sustained release of repaglinide: Preparation, pharmacokinetics and hypoglycemic activity in beagle dogs.
W. He (2015)
10.1208/s12249-014-0229-1
Bilayer Matrix Tablets for Prolonged Actions of Metformin Hydrochloride and Repaglinide
W. He (2014)
10.1016/j.ijpharm.2010.06.023
In vitro characterization and invivo toxicity study of repaglinide loaded poly (methyl methacrylate) nanoparticles.
U. M. Dhana Lekshmi (2010)
prove bile duct - targeted drug delivery and therapeutic ef fi cacy for cholangiocarcinoma by cucurbitacin B loaded phospholipid complex modi fi ed with berberine hydrochloride
B. Chukwunonso Obi (2016)
10.1016/J.IJPHARM.2006.09.025
Curcumin-phospholipid complex: Preparation, therapeutic evaluation and pharmacokinetic study in rats.
K. Maiti (2007)
10.1080/10717540701203034
Preparation and Characterization of Solid Lipid Nanoparticles Containing Silibinin
J. Zhang (2007)
10.1517/17425240902967607
Pharmacosomes: the lipid-based new drug delivery system
A. Semalty (2009)
10.1016/J.DIABRES.2004.09.018
Effects of repaglinide on oxidative stress in tissues of diabetic rabbits.
A. Gumieniczek (2005)
10.2147/IJN.S39526
A novel drug–phospholipid complex enriched with micelles: preparation and evaluation in vitro and in vivo
Hai-jian Xia (2013)
10.1111/dme.12269
Prevalence of Type 2 diabetes and pre‐diabetes among overweight or obese children in Tianjin, China
H. Zhu (2013)
Bioavailability of repaglinide, a novel antidiabetic agent, administered orally in tablet or solution form or intravenously in healthy male volunteers.
V. Hatorp (1998)
10.1016/S1262-3636(07)70192-1
Repaglinide has more beneficial effect on cardiovascular risk factors than glimepiride: data from meal-test study.
M. Rizzo (2005)
10.1016/j.ijpharm.2013.10.043
Novel rifampicin-phospholipid complex for tubercular therapy: synthesis, physicochemical characterization and in-vivo evaluation.
C. Singh (2014)
10.1186/1472-6882-5-14
Antihyperlipidemic and antiperoxidative effect of Diasulin, a polyherbal formulation in alloxan induced hyperglycemic rats
R. Saravanan (2005)
10.1208/s12249-012-9772-9
Design and Evaluation of a Novel Evodiamine-Phospholipid Complex for Improved Oral Bioavailability
Q. Tan (2012)
10.1016/j.ijpharm.2014.08.006
Application of phospholipid complex technique to improve the dissolution and pharmacokinetic of probucol by solvent-evaporation and co-grinding methods.
B. Guo (2014)
10.1111/j.1753-0407.2008.00001.x
Repaglinide‐loaded long‐circulating biodegradable nanoparticles: Rational approach for the management of type 2 diabetes mellitus
S. Jain (2009)
10.1016/j.ijpharm.2012.05.009
Huperzine A-phospholipid complex-loaded biodegradable thermosensitive polymer gel for controlled drug release.
X. Cai (2012)
10.1016/j.ijbiomac.2014.06.011
In vitro and in vivo evaluation of novel interpenetrated polymer network microparticles containing repaglinide.
R. Kulkarni (2014)
10.7326/0003-4819-131-4-199908170-00008
Pharmacologic Therapy for Type 2 Diabetes Mellitus
R. DeFronzo (1999)
10.2478/v10007-009-0023-x
Development and physicochemical evaluation of pharmacosomes of diclofenac
A. Semalty (2009)
10.1002/(SICI)1099-0461(2000)14:4<189::AID-JBT2>3.0.CO;2-V
Effects of new antioxidant compounds PNU‐104067F and PNU‐74389G on antioxidant defense in normal and diabetic rats
F. Rauscher (2000)
10.1046/J.0306-5251.2003.01862.X
CYP2C8 and CYP3A4 are the principal enzymes involved in the human in vitro biotransformation of the insulin secretagogue repaglinide.
Tanja Busk Bidstrup (2003)
10.1016/j.colsurfb.2013.05.020
Optimization and charaterization of repaglinide biodegradable polymeric nanoparticle loaded transdermal patchs: in vitro and in vivo studies.
V. Vijayan (2013)
10.1007/s40278-018-52936-y
Repaglinide
J. Balfour (1998)
10.1016/S0939-6411(02)00087-5
Atomic force microscopy imaging of novel type of polymeric colloidal nanostructures.
I. Montasser (2002)
10.1208/s12249-014-0267-8
Ultra Rapidly Dissolving Repaglinide Nanosized Crystals Prepared via Bottom-Up and Top-Down Approach: Influence of Food on Pharmacokinetics Behavior
Rahul Gadadare (2014)
LIPID PROFILE OF ALLOXAN-INDUCED DIABETIC WISTAR RATS TREATED WITH METHANOLIC EXTRACT OF ADANSONIA DIGITATA FRUIT PULP
Hauwa’u Yakubu Bako (2014)
10.1021/JF010697N
Antioxidant activity and phenolic compounds in selected herbs.
W. Zheng (2001)
Effect of repaglinide and gliclazide on glycaemic control, early-phase insulin secretion and lipid profiles in.
H. Zhang (2011)
Self-assembly of beta-casein and lysozyme.
X. Pan (2007)
10.1016/j.ijpharm.2014.10.038
Preparation, characterization and in vivo evaluation of formulation of repaglinide with hydroxypropyl-β-cyclodextrin.
M. Liu (2014)



This paper is referenced by
10.1016/j.ijbiomac.2020.03.172
Chitosan/calcium phosphate flower-like microparticles as carriers for drug delivery platform.
Chao Luo (2020)
10.1155/2020/1295492
Dunaliella salina Attenuates Diabetic Neuropathy Induced by STZ in Rats: Involvement of Thioredoxin
F. El-Baz (2020)
10.3233/BME-181029
Preparation, physicochemical characterization and pharmacokinetics of paeoniflorin-phospholipid complex.
Jiajia Qian (2019)
10.1080/00914037.2019.1706513
Novel pH/reduction responsive graphene oxide nanoparticles based hydrogel for targeted combination chemotherapy
T. Anirudhan (2019)
10.1016/j.ijbiomac.2018.12.072
Preparation and drug release property of tanshinone IIA loaded chitosan-montmorillonite microspheres.
C. Luo (2019)
10.1007/s10870-019-00811-7
Preparation, Characterization and Crystal Structures of a Key Intermediate, and a Significant Impurity, in the Synthesis of Repaglinide
Gui-Mei Tang (2019)
10.1016/j.actbio.2017.12.028
Redox-responsive polymeric micelles formed by conjugating gambogic acid with bioreducible poly(amido amine)s for the co-delivery of docetaxel and MMP-9 shRNA.
Yanan Kang (2018)
10.1016/j.ijpharm.2017.09.033
Reconstitutable spray dried ultra-fine dispersion as a robust platform for effective oral delivery of an antihyperlipidemic drug.
M. Basha (2017)
10.7324/japs.2018.81002
DOE , formulation , and optimization of Repaglinide nanostructured lipid carriers
Shady Swidan (2018)
NANOSTRUCTURED LIPID CARRIER: THE ADVANCED LIPID CARRIERS
Nikita Nandvikar (2019)
10.1080/10717544.2017.1334719
Engineering of a novel optimized platform for sublingual delivery with novel characterization tools: in vitro evaluation and in vivo pharmacokinetics study in human
N. Morsi (2017)
10.3390/cancers11060807
The Delivery Strategy of Paclitaxel Nanostructured Lipid Carrier Coated with Platelet Membrane
Ki-Hyun Bang (2019)
10.1016/J.JDDST.2018.12.014
A promising nystatin nanocapsular hydrogel as an antifungal polymeric carrier for the treatment of topical candidiasis
Mona M AbouSamra (2019)
10.1016/j.ijbiomac.2020.01.189
Encapsulation of phycocyanin by prebiotics and polysaccharides-based electrospun fibers and improved colon cancer prevention effects.
Y. Wen (2020)
10.1016/j.ijbiomac.2018.01.044
Chitosan nanoparticles/cellulose nanocrystals nanocomposites as a carrier system for the controlled release of repaglinide.
Wafaa S Abo-Elseoud (2018)
10.1016/j.ijbiomac.2020.06.058
Self- assembled lactoferrin-conjugated linoleic acid micelles as an orally active targeted nanoplatform for Alzheimer's disease.
Mona M. Agwa (2020)
10.1016/j.apsb.2018.09.009
Selenium-layered nanoparticles serving for oral delivery of phytomedicines with hypoglycemic activity to synergistically potentiate the antidiabetic effect
Wenji Deng (2019)
10.2174/1389450120666190307101642
Nanotechnology Advanced Strategies for the Management of Diabetes Mellitus.
A. M. Mohsen (2019)
10.1016/j.actbio.2018.09.049
Nanoparticulate-based drug delivery systems for small molecule anti-diabetic drugs: An emerging paradigm for effective therapy.
S. Uppal (2018)
10.1016/j.ijpharm.2017.07.060
Improved metabolic stability and therapeutic efficacy of a novel molecular gemcitabine phospholipid complex.
Chander Parkash Dora (2017)
10.1080/02652048.2019.1656294
Self-assembled micelles based on gambogenic acid-phospholipid complex for sustained-release drug delivery
Beilei Wang (2019)
10.1080/10717544.2019.1616236
Use of magnoflorine-phospholipid complex to permeate blood-brain barrier and treat depression in the CUMS animal model
B. Li (2019)
Semantic Scholar Logo Some data provided by SemanticScholar