Abstract：
PURPOSE:The present research work involves Quality by Design (QbD)-based fabrication of lipid nanoconstructs (LNC) of paliperidone (PPD) bearing superior biopharmaceutical attributes. METHODS:LNC of paliperidone was prepared by melt emulsification-probe sonication and high-pressure homogenization method followed by optimization using QbD approach. Preparing LNC by both these methods will give the benefit of identifying the best optimized formulation which will be further evaluated for in vitro studies. RESULTS:The best optimized formulation was obtained using melt emulsification-probe sonication technique with small particle size (86.35 nm), high entrapment efficiency (90.07 %), and high loading capacity (8.49 %). The drug release from LNC was found to be 5, 8, and 9-folds greater than drug suspension in pH 1.2, 6.8, and 7.4 respectively (p < 0.001). Stability studies of LNC in simulated gastric fluid pH 1.2 and fasted state simulated intestinal fluid depicted no alteration in particle size and polydispersity index of LNC but were found to increase in fed state simulated intestinal fluid. The drug permeability through rat intestine for LNC was found to be approximately 6-folds (p < 0.05) greater as compared to the drug suspension which was further confirmed by confocal microscopy. The in vitro lipolysis study presented significantly highest solubilization (p < 0.001) in the aqueous phase thereby anticipating higher in vivo absorption. CONCLUSION:Thus, it was concluded that LNC bears the knack of improving the solubilization and permeation potential of an otherwise hydrophobic drug, paliperidone."
journal_name
Chem Phys Lipidsjournal_title
Chemistry and physics of lipidsauthors
Rehman S,Nabi B,Baboota S,Ali Jdoi
10.1016/j.chemphyslip.2020.105005subject
Has Abstractpub_date
2021-01-01 00:00:00pages
105005eissn
0009-3084issn
1873-2941pii
S0009-3084(20)30136-5journal_volume
234pub_type
杂志文章abstract：:An investigation into the effect of alpha-tocopherol on phospholipid model membranes has been carried out by electron spin resonance (ESR) and saturation transfer ESR. The use of stearic acid and of perdeutero -di-t-butyl nitroxide spin probes has allowed us to monitor, in particular, the effect of alpha-tocopherol on...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/0009-3084(90)90129-f
更新日期：1990-03-01 00:00:00
abstract：:(1) An analysis has been conducted of the lipids present in three obligately anaerobic bacteria isolated from the ovine rumen belonging to the genus Butyrivibrio. Two of these organisms are rich in phospholipase (A1 + A2) activity, and appear to be different strains of the species fibrisolvens. (2) The only N-containi...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/0009-3084(76)90067-0
更新日期：1976-10-01 00:00:00
abstract：:The chemical syntheses of a number of C27 15-oxygenated sterols and their derivatives have been pursued to permit evaluation of their activity in the inhibition of sterol biosynthesis in animal cells in culture. Described herein are chemical syntheses of 3 alpha-benzoyloxy-5 alpha-cholest-8(14)-en-15-one, 5 alpha-chol...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/0009-3084(79)90111-7
更新日期：1979-11-01 00:00:00
abstract：:Human serum amyloid A (SAA) is a precursor protein of AA amyloidosis and a component of high-density lipoproteins (HDLs), thus it is essential to investigate the amyloid fibril formation of SAA under a lipid environment. We used synthetic fragment peptides corresponding to the N-terminal (residues 1-27) and central (r...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/j.chemphyslip.2016.11.004
更新日期：2017-01-01 00:00:00
abstract：:A new scheme for synthesis of saturated 1-O-alkyl-2-O-methyl-rac-glycerolipids is described. The reductive cleavage of 2-O-methyl-1,3-O,O-benzylideneglycerol with BH3.THF complex leads to 1-O-benzyl-2-O-methyl-rac-glycerol, which is a key in intermediate for the facile preparation of 1-O-alkyl-2-O-methyl-rac-glycerol ...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/0009-3084(91)90026-8
更新日期：1991-10-01 00:00:00
abstract：:In the present work, we obtained polymeric diacetylene liposomes that can associate N-Acetyl-l-Cysteine (NAC), a broad spectrum mucolytic. The reason for studying these formulations is that they could be applied in the future as NAC delivery systems, with a possible dose reduction but maintaining its effect. Liposomes...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/j.chemphyslip.2020.104936
更新日期：2020-09-01 00:00:00
abstract：:The effect of peptides on bilayer----non-bilayer phase transitions can be used as a tool to investigate the molecular aspects of peptide-lipid interactions. In this contribution the action on membranes of the peptide antibiotic gramicidin A and the bee venom component melittin are compared. Although the known structur...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章,评审
doi：10.1016/0009-3084(91)90084-o
更新日期：1991-03-01 00:00:00
abstract：:The properties of dipalmitoylphosphatidylcholine (DPPC):6-ketocholestanol bilayer at 50 mol% sterol were studied using the molecular dynamics simulation technique. Our simulations were performed at constant pressure and temperature on a nanosecond time scale. Data from this simulation were compared to the results of o...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/s0009-3084(01)00160-8
更新日期：2001-07-01 00:00:00
abstract：:We have studied the interaction of water with the lipid head group by gravimetrically measuring the lipid water adsorption and the lateral dc electrical conductivity increase resulting from this hydration. We have done this for dimyristoyl phosphatidylcholine (DMPC) having protonated or deuterated hydrocarbon chains. ...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/j.chemphyslip.2004.05.003
更新日期：2004-09-01 00:00:00
abstract：:The antioxidative and/or prooxidative activity of 4-methylcoumanrin (MC), 7-hydroxy-4-methylcoumarin (HMC) and 7,8-dihydroxy-4-methylcoumarin (DHMC), respectively, in the peroxidation of human low-density lipoprotein (LDL) has been studied. The peroxidation was initiated either thermally by water-soluble initiator 2,2...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/s0009-3084(99)00101-2
更新日期：1999-12-01 00:00:00
abstract：:The properties of cholesterol in bilayers of egg phosphatidylcholine (PC) were investigated directly by means of 2H-NMR of specifically-deuterated species (C3, C7, C26, C27). Quadrupole splittings were a measure of molecular ordering, and relaxation times T1 and T2e were indicators of rates of motion. The importance o...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/0009-3084(82)90072-x
更新日期：1982-12-01 00:00:00
abstract：:Temperature and pH effects were studied for stability, structural organization, fluidity and permeability of vesicles from a polar lipid methanol fraction isolated from the Aeropyrum pernix. We determined the permeability of C(25,25) liposomes using fluorescence intensity of released calcein. At pH 7.0 and 9.0, and fr...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/j.chemphyslip.2011.01.005
更新日期：2011-03-01 00:00:00
abstract：:A fluorescence spectroscopy global data analysis environment is described. Within this analysis environment, multidimensional fluorescence decay data (time and frequency domains) can be analyzed in terms of a wide variety of photophysical models. A generalized compartmental analysis structure is utilized, where one ca...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/0009-3084(89)90052-2
更新日期：1989-06-01 00:00:00
abstract：:Cannabinoid receptor agonists diminish responses to painful stimuli. Extensive evidence demonstrates that CB(1) cannabinoid receptor activation inhibits pain responses. Recently, the synthesis of CB(2) cannabinoid receptor-selective agonists has allowed testing whether CB(2) receptor activation inhibits pain. CB(2) re...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章,评审
doi：10.1016/s0009-3084(02)00155-x
更新日期：2002-12-31 00:00:00
abstract：:Cold atmospheric plasma (CAP) is an emerging source for the locally defined delivery of reactive species, and its clinical potential has been identified in the control of inflammatory processes, such as acute and chronic wounds, or cancerous lesions. Lipids, due to their localization and chemical structure as ideal ta...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/j.chemphyslip.2019.104786
更新日期：2020-01-01 00:00:00
abstract：:Human erythrocyte band 3 reconstituted into phospholipid vesicles has been used for studying the interaction of interdigitated lipid bilayer with an integral membrane protein. The interdigitated gel phase in DPPG/band 3 or DPPG/DMPC/band 3 systems was induced with polymyxin B (PMB) or Tris+. The phase transitions of t...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/0009-3084(94)90005-1
更新日期：1994-03-01 00:00:00
abstract：:Production of conjugated linoleic acids (CLA) using castor oil as starting material involves conversion of ricinoleic acid to methyl 12-mesyloxy-octadec-9-enoate (MMOE) followed by dehydration. This process usually uses 1,8-diazabicyclo-(5.4.0)-undec-7-ene (DBU) as an expensive dehydrating reagent. The present study r...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/s0009-3084(02)00052-x
更新日期：2002-10-01 00:00:00
abstract：:Characterization of phospholipids (PLs) and phytosterols were determined in Schisandra chinensis (S. chinensis) oil by UPLC-Q/TOF-MSE. The determination process was based on feature fragment information of components generated by the MSE detector. A total of 49 and 39 PLs were identified in S. chinensis oil under nega...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/j.chemphyslip.2019.03.003
更新日期：2019-07-01 00:00:00
abstract：:Understanding how stereochemistry affects interactions with cell membranes is important for effective drug development. Chirality has been shown to greatly effect pharmaceutical distribution and metabolism within the cell. However it has been thought that interactions with, and passive diffusion through, the membrane ...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/j.chemphyslip.2018.05.002
更新日期：2018-08-01 00:00:00
abstract：:Cholesterol has many functions, including those that affect biophysical properties of membranes, and is a precursor to hormone synthesis. These actions are governed by enzymatic pathways that modify the sterol nucleus or the isooctyl tail. The addition of oxygen to the cholesterol backbone produces its derivatives kno...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章,评审
doi：10.1016/j.chemphyslip.2011.06.006
更新日期：2011-09-01 00:00:00
abstract：:Age-related fluorescent and cross-linked proteins increase with lipid oxidation of tissues. The fluorophores and cross-links have been considered to be conjugated Schiff bases between amino groups of proteins and malonaldehyde. Our recent studies showed that the fluorophores produced in the in vitro reaction of protei...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章,评审
doi：10.1016/0009-3084(87)90054-5
更新日期：1987-07-01 00:00:00
abstract：:The application of fluorescence methodologies to obtain information about the extent, dynamics and topology of peptide interaction with binary phospholipid (mainly zwitterionic/anionic) mixtures is reviewed. First, general approaches based on peptide (tryptophan residues) fluorescence properties that give information ...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/s0009-3084(02)00180-9
更新日期：2003-01-01 00:00:00
abstract：:Delta(9)-Tetrahydrocannabinol (delta(9)-THC), the primary psychoactive constituent of marijuana (Cannabis sativa), is known to bind to two cannabinoid receptors: CB(1) receptors, located primarily in the brain, and CB(2) receptors, located primarily in the periphery. Recent research has suggested that other cannabinoi...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章,评审
doi：10.1016/s0009-3084(02)00146-9
更新日期：2002-12-31 00:00:00
abstract：:The apparent Mn2+ binding constant for L-alpha-dipalmitoylphosphatidylcholine (DPPC) bilayers dispersed in monovalent salt and MnCl2 dispersions was determined as a function temperature using electron paramagnetic resonance (ERP). Reproducibility in the data sets requires the use of a standard salt solution and dual c...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/0009-3084(88)90023-0
更新日期：1988-03-01 00:00:00
abstract：:High density lipoprotein (HDL) is prone to modification by the oxidizing and chlorinating agent hypochlorite anion (OCl-). Oxidation of apolipoprotein (apo) A-I, the major protein in HDL, reduces ABCA-1 mediated cholesterol efflux and other protective responses to HDL. The apoA-I mimetic peptide 4F has been shown to u...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/j.chemphyslip.2019.01.009
更新日期：2019-03-01 00:00:00
abstract：:Trehalose lipids are bacterial biosurfactants which present interesting physicochemical and biological properties. These glycolipids have a number of different commercial applications and there is an increasing interest in their use as therapeutic agents. The amphiphilic nature of trehalose lipids points to the membra...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/j.chemphyslip.2014.03.005
更新日期：2014-07-01 00:00:00
abstract：:The present work aim to develop pH responsive nanosystem comprising lumefantrine with calcium phosphate nanoparticles loaded lipidic cubosomes for the effective treatment of lung cancer. FTIR results showed that, compatibility nature of selected excipients for the synthesis of LF-CaP-Cs. The XRD results showed develop...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/j.chemphyslip.2019.03.016
更新日期：2019-11-01 00:00:00
abstract：:The diffusion of a lipid fluorescent analogue across tight junctions in MDCK-I cells was studied by FRAP measurements. Cells were labelled with C6-NBD-PC at the apical cell membrane. Transepithelial resistance of MDCK-I cells was found to be higher than 3000 omega x cm2, which indicates the presence of a very tight ep...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/0009-3084(94)90066-3
更新日期：1994-05-23 00:00:00
abstract：:The development of "molecular rulers" would allow one to quantitatively locate the penetration depth of intercalants within lipid bilayers. To this end, an attempt was made to correlate the (13)C NMR chemical shift of polarizable "reporter" carbons (e.g., carbonyls) of intercalants within DMPC liposomal bilayers - wit...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/j.chemphyslip.2014.07.007
更新日期：2014-12-01 00:00:00
abstract：:We consider the situation of integral membrane proteins in a lipid bilayer matrix where the size of the polar group of the protein is important in determining the lateral packing of the proteins. We represent the cross-section of the protein hydrophobic core as a hexagon moving on a lattice, and represent the projecti...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/0009-3084(88)90041-2
更新日期：1988-04-01 00:00:00
