scholarly journals Polar Lipid Fraction E from Sulfolobus acidocaldarius and Dipalmitoylphosphatidylcholine Can Form Stable yet Thermo-Sensitive Tetraether/Diester Hybrid Archaeosomes with Controlled Release Capability

2020 ◽  
Vol 21 (21) ◽  
pp. 8388
Author(s):  
Umme Ayesa ◽  
Parkson Lee-Gau Chong
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Polar Lipid ◽  
Sharp Increase ◽  
Serum Proteins ◽  
Release Kinetics ◽  
Lipid Fraction ◽  
Sulfolobus Acidocaldarius ◽  
Polar Lipid Fraction ◽  
Flip Flop

Archaeosomes have drawn increasing attention in recent years as novel nano-carriers for therapeutics. The main obstacle of using archaeosomes for therapeutics delivery has been the lack of an efficient method to trigger the release of entrapped content from the otherwise extremely stable structure. Our present study tackles this long-standing problem. We made hybrid archaeosomes composed of tetraether lipids, called the polar lipid fraction E (PLFE) isolated from the thermoacidophilic archaeon Sulfolobus acidocaldarius, and the synthetic diester lipid dipalmitoylphosphatidylcholine (DPPC). Differential polarized phase-modulation and steady-state fluorometry, confocal fluorescence microscopy, zeta potential (ZP) measurements, and biochemical assays were employed to characterize the physical properties and drug behaviors in PLFE/DPPC hybrid archaeosomes in the presence and absence of live cells. We found that PLFE lipids have an ordering effect on fluid DPPC liposomal membranes, which can slow down the release of entrapped drugs, while PLFE provides high negative charges on the outer surface of liposomes, which can increase vesicle stability against coalescence among liposomes or with cells. Furthermore, we found that the zeta potential in hybrid archaeosomes with 30 mol% PLFE and 70 mol% DPPC (designated as PLFE/DPPC(3:7) archaeosomes) undergoes an abrupt increase from −48 mV at 37 °C to −16 mV at 44 °C (termed the ZP transition), which we hypothesize results from DPPC domain melting and PLFE lipid ‘flip-flop’. The anticancer drug doxorubicin (DXO) can be readily incorporated into PLFE/DPPC(3:7) archaeosomes. The rate constant of DXO release from PLFE/DPPC(3:7) archaeosomes into Tris buffer exhibited a sharp increase (~2.5 times), when the temperature was raised from 37 to 42 °C, which is believed to result from the liposomal structural changes associated with the ZP transition. This thermo-induced sharp increase in drug release was not affected by serum proteins as a similar temperature dependence of drug release kinetics was observed in human blood serum. A 15-min pre-incubation of PLFE/DPPC(3:7) archaeosomal DXO with MCF-7 breast cancer cells at 42 °C caused a significant increase in the amount of DXO entering into the nuclei and a considerable increase in the cell’s cytotoxicity under the 37 °C growth temperature. Taken together, our data suggests that PLFE/DPPC(3:7) archaeosomes are stable yet potentially useful thermo-sensitive liposomes wherein the temperature range (from 37 to 42–44 °C) clinically used for mild hyperthermia treatment of tumors can be used to trigger drug release for medical interventions.

scholarly journals PREPARATION, PHYSICAL CHARACTERIZATION, AND PHARMACOKINETIC STUDY OF DOCETAXEL NANOCRYSTALS

2019 ◽  
pp. 238-244
Author(s):  
ARVIND GANNIMITTA ◽  
PRATHIMA SRINIVAS ◽  
VENKATESHWAR REDDY A ◽  
PEDIREDDI SOBHITA RANI
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Water Solubility ◽  
Release Kinetics ◽  
Tween 80 ◽  
Fickian Diffusion ◽  
Sustained Drug Release ◽  
Egg Lecithin

Objective: The main objective of this study was to prepare and evaluate the nanocrystal formulation of docetaxel. Methods: Docetaxel nanocrystals were formulated to improve the water solubility. Docetaxel nanocrystals were prepared by nanoprecipitation method using Tween 80, egg lecithin, and povidone C-12 as stabilizers and poly(lactic-co-glycolic acid) (PLGA) as polymer in acceptable limits. A total of 16 formulations were prepared by changing stabilizer and polymer ratios. The prepared nanocrystals were characterized by particle size, zeta potential, crystalline structure, surface morphology, assay, saturation solubility, and in vitro drug release. Results: Based on particle size, polydispersity index, and zeta potential data, four formulations were optimized. The formulation containing Tween 80 as stabilizer has shown lowest particle size and better drug release than the formulations containing egg lecithin and povidone C-12 as stabilizers. The formulation containing Tween 80 and PLGA has shown still lower sized particles than the Tween 80 alone and exhibited prolonged sustained drug release. The release kinetics of formulations containing Tween 80 and PLGA followed zero-order release kinetics and formulations containing egg lecithin and povidone C-12 followed Higuchi diffusion (non-Fickian). Conclusion: From the study, we concluded that as the type and concentration of stabilizer changed the size and shape of the crystals were also changed and the formulations showed sustained drug release with non-Fickian diffusion.

Analysis of polar lipid fraction of Pinus halepensis Mill. seeds from North Algeria

2013 ◽  
Vol 51 ◽  
pp. 116-122 ◽  
Author(s):  
Nabil Kadri ◽  
Bachra Khettal ◽  
Rachida Yahiaoui-zaidi ◽  
Veronique Barragan-Montero ◽  
Jean-Louis Montero
Keyword(s):  
Polar Lipid ◽  
Pinus Halepensis ◽  
Lipid Fraction ◽  
Polar Lipid Fraction ◽  
North Algeria

scholarly journals FABRICATION AND IN VITRO CHARACTERIZATION OF A NOVEL NANOSUSPENSION OF TELMISARTAN: A POORLY SOLUBLE DRUG PREPARED BY ANTISOLVENT PRECIPITATION TECHNIQUE USING 33 FACTORIAL DESIGN

2020 ◽  
pp. 286-294
Author(s):  
PRASANTA KUMAR MOHAPATRA ◽  
SIREESHA ◽  
VAIBHAV RATHORE ◽  
HARISH CHANDRA VERMA ◽  
BIBHUTI PRASAD RATH ◽  
...  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Dissolution Rate ◽  
Release Kinetics ◽  
Precipitation Method ◽  
Lauryl Sulfate ◽  
Poorly Soluble ◽  
Poorly Soluble Drug

Objective: The motivation behind the current examination was to build the solvency and dissolution rate of an antihypertensive drug telmisartan by the planning of nanosuspension by precipitation method at the research facility scale. We researched the nanoparticle manufacture of telmisartan employing a 33 factorial experimental configuration considering the impacts of nanosuspension on the physical, morphological, and dissolution properties of telmisartan. Methods: To get ready, nanosuspension particles of an ineffectively dissolvable drug are moreover of a drug solution to the anti-solvent leads to abrupt supersaturation and precipitation the making of nanoparticles. The nanosuspension particles of a poorly soluble drug loaded with urea and surfactants (sodium lauryl sulfate (SLS), poloxamer 188, Tween 80) have been prepared by a precipitation method. The nanosuspension particles were characterized for particle size, zeta potential, Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), in vitro drug release, and release kinetics. Results: The readily optimized batch nanosuspension particles evaluated and exhibited the particle size (750 nm), zeta potential (-24.33 mV), differential scanning calorimetry (DSC) drug exhibited a change in crystalline form to amorphous, in vitro dissolution (F12 was higher 95% within 5 min) and drug release kinetics. The formulation parameter of surfactant concentration is optimized. Conclusion: The formulation of the nanosuspension approach has been shown to substantial improvement in the dissolution rate, thereby enhancing the oral bioavailability with the future development of this technology.

scholarly journals FORMULATION AND EVALUATION OF ETHAMBUTOL POLYMERIC NANOPARTICLES

2020 ◽  
pp. 207-217
Author(s):  
MONOWAR HUSSAIN ◽  
ANUPAM SARMA ◽  
SHEIKH SOFIUR RAHMAN ◽  
ABDUL MATIN SIDDIQUE ◽  
TANUKU PAVANI EESWARI
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Polymeric Nanoparticles ◽  
Release Kinetics ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Compatibility Study ◽  
Bacterial Disease ◽  
Dose Frequency

Objective: Tuberculosis (TB) is an infectious bacterial disease caused by Mycobacterium tuberculosis which most commonly affects the lungs. TB has the highest mortality rate than any other infectious disease occurs worldwide. The main objective of the present investigation was to develop polymeric nanoparticles based drug delivery system to sustain the ethambutol (ETB) release by reducing the dose frequency. Methods: The Preformulation studies of drug ETB were done by physical characterization, melting point determination, and UV spectrophotometric analysis. The ETB loaded nanoparticles were prepared by double-emulsion (W/O/W) solvent evaporation/diffusion technique. The prepared polymeric nanoparticles were evaluated for particle size, polydispersity index, zeta potential, drug entrapment efficiency, drug loading, drug-polymer compatibility study, surface morphology, in vitro drug release, and release kinetics. Results: Based on the result obtained from the prepared formulations, F11 showed the best result and was selected as the optimized formulation. Optimized batch (F11) showed better entrapment efficiency (73.3%), good drug loading capacity (13.21%), optimum particle size (136.1 nm), and zeta potential (25.2 mV) with % cumulative drug release of 79.08% at the end of 24 h. Conclusion: These results attributed that developed polymeric nanoparticles could be effective in sustaining the ETB release over 24 h. Moreover, the developed nanoparticles could be an alternate method for ETB delivery with a prolonged drug release profile and a better therapeutic effect can be achieved for the treatment of tuberculosis.

Neutral lipids, phospholipids, and a betaine lipid of the snow mold fungus Microdochium nivale

1998 ◽  
Vol 44 (11) ◽  
pp. 1051-1059 ◽  
Author(s):  
Anita Istokovics ◽  
Naoki Morita ◽  
Kazuo Izumi ◽  
Tamotsu Hoshino ◽  
Isao Yumoto ◽  
...  
Keyword(s):  
Fatty Acids ◽  
Fatty Acid ◽  
Neutral Lipid ◽  
Polar Lipid ◽  
Lipid Fraction ◽  
Microdochium Nivale ◽  
Neutral Lipid Fraction ◽  
Polar Lipid Fraction ◽  
Snow Mold ◽  
Betaine Lipid

The hyphae of the snow mold Microdochium nivale contained lipids in a yield of about 10% w/w of the dry matter of hyphae. The total lipid was fractionated into neutral and polar lipid fractions. In the neutral lipid fraction, triacylglylcerol was the sole major component. As minor components, ergosterol, diacylglycerol, free fatty acid, and fatty acyl ergosterol were identified. The polar lipid fraction contained phospholipids, glycolipids, and a lipid containing neither phosphorus nor sugar. Phosphatidylethanolamine, phosphatidylcholine, phosphatidylglycerol, phosphatidylserine, and phosphatidic acid were identified as phospholipids. The polar lipid fraction included at least four kinds of glycolipids that have not been identified. A very unusual lipid in fungi, a betaine lipid, diacylglyceryltrimethylhomoserine, was identified by chemical and physicochemical analyses. The level of the neutral lipid fraction, which accounted for 60% of the total lipid in hyphae at the exponential phase, was significantly increased compared with that of the polar lipid fraction and constituted 80% of the total at the stationary phase. The neutral and polar lipids of Microdochium nivale contained 18:3 (9,12,15), 18:2 (9,12), 18:1 (9), and 16:0 as principal fatty acids. Among them, 18:2 (9,12) and 18:3 (9,12,15) were the major fatty acids of triacylglycerol, phosphatidylcholine, phosphatidylglycerol, and phosphatidylethanolamine, whereas in diacylglyceryltrimethylhomoserine, the major components were 16:0 and 18:3 (9,12,15).Key words: snow mold, phospholipids, betaine lipid, fatty acid, Microdochium nivale.

scholarly journals In Vitro Evaluation of a Peptide-Mesoporous Silica Nanoparticle Drug Release System against HIV-1

Inorganics ◽  
2020 ◽  
Vol 8 (7) ◽  
pp. 42 ◽  
Author(s):  
Katharina Braun ◽  
Christina M. Stürzel ◽  
Frank Kirchhoff ◽  
Mika Lindén
Keyword(s):  
Drug Release ◽  
Mesoporous Silica ◽  
Release Rate ◽  
Serum Proteins ◽  
Release Kinetics ◽  
Drug Loading ◽  
Active Form ◽  
Equilibrium Concentration ◽  
Hiv 1

It has been shown that the optimized VIR-576 derivative of the natural HIV-1 entry inhibitor targeting the viral gp41 fusion peptide is safe and effective in infected individuals. However, high doses of this peptide were required, and stability, as well as delivery, must be improved for clinical application. Here, we examined the loading and release of VIR-576 into/from mesoporous silica nanoparticles (MSNs) in vitro. We found that a moderately high peptide loading of 11.5 wt % could be achieved by adsorption from PBS buffer (pH 7.2), i.e., under mild, fully peptide-compatible conditions. The release rate of peptide into the same buffer was slow and the equilibrium concentration as indicated by the adsorption isotherm could not be reached even within 50 h at the particle concentrations studied. However, a faster release was observed at lower particle concentrations, indicating that partial particle dissolution had a positive influence on peptide release. To determine the antiviral activity of VIR-576-loaded MSNs, TZM-bl indicator cells were exposed to HIV-1 and the infection rates were followed as a function of time and VIR-576 concentration. The inhibitory activity observed for VIR-576 released from the MSNs was virtually identical to that of free VIR-576 at the 48 h time point, indicating that (a) VIR-576 was released in an active form from the MSNs, and (b) the release rate in the presence of serum proteins was clearly higher than that observed under protein-free conditions. These observations are discussed based on competitive peptide/protein adsorption, as well as potential influences of serum proteins on the dissolution-reprecipitation of silica under conditions where the total silica concentration is above the saturation level for dissolved silica. Our results highlight the need for studying drug release kinetics in the presence of serum proteins, in order to allow for a better extrapolation of in vitro data to in vivo conditions. Furthermore, due to the high peptide loadings that can be achieved using MSNs as carriers, such a formulation appears promising for local release applications. For systemic administration, however, peptides with a higher potency would be needed, due to their high molar masses limiting the drug loading in terms of moles per gram carrier.

Polar lipid fraction in soil: a kerogen-like matter

1991 ◽  
Vol 17 (3) ◽  
pp. 341-349 ◽  
Author(s):  
A. Amblès ◽  
J.C. Jacquesy ◽  
P. Jambu ◽  
J. Joffre ◽  
R. Maggi-Churin
Keyword(s):  
Polar Lipid ◽  
Lipid Fraction ◽  
Polar Lipid Fraction

scholarly journals Polar Lipid Fraction from Golden Oyster Mushrooms (Pleurotus citrinopileatus) Suppresses Colon Injuries from Inflammatory Stresses in vivo and in vitro

2020 ◽  
Vol 69 (7) ◽  
pp. 751-757
Author(s):  
Shinji Yamashita ◽  
Takuya Seino ◽  
Miho Inobe ◽  
Mirinthorn Jutanom ◽  
Satoshi Matsumoto ◽  
...  
Keyword(s):  
Polar Lipid ◽  
Lipid Fraction ◽  
Polar Lipid Fraction ◽  
Oyster Mushrooms ◽  
Pleurotus Citrinopileatus ◽  
Colon Injuries

scholarly journals Preparation and Characterization of Celecoxib Entrapped Guar Gum Nanoparticles Targeted for Oral Drug Delivery against Colon Cancer: An In-Vitro Study

2020 ◽  
Vol 10 (2-s) ◽  
pp. 14-21
Author(s):  
Deepika Chandel ◽  
Shivani Uppal ◽  
Surinder Kumar Mehta ◽  
Geeta Shukla
Keyword(s):  
Colorectal Cancer ◽  
Colon Cancer ◽  
Drug Release ◽  
Zeta Potential ◽  
Guar Gum ◽  
Oral Drug Delivery ◽  
Release Kinetics ◽  
Drug Loading ◽  
Oral Drug

The present study is an attempt to synthesize nanosized guar gum carriers encapsulating celecoxib as the chemopreventive agent for experimental colorectal cancer (CRC).  Guar gum nanoparticles without celecoxib (eGGNPs) and celecoxib loaded guar gum nanoparticles (cGGNPs) were prepared by oil-in-water emulsification and in situ polymer crosslinking method. Electron microscopy, zeta potential and fourier transform infrared spectra analysis was used to affirm the size, stability and morphology of the nanoparticles. In-vitro drug release was investigated using dialysis method. Further, the effect of nanoparticles (eGGNPs & cGGNPs) was evaluated on Caco 2 colon cancer cell lines. Spherical guar gum nanoparticles were obtained in the size range of 200±6nm with zeta potential of -32.1mV indicating good stability of the GGNPs with drug loading of 30±3.2%, and drug release following zero order kinetics. The eGGNPs had no effect on Caco2 cell viability whereas the cGGNPs showed time and concentration dependent growth inhibition of Caco 2 cells. These findings suggest the successful preparation of chemopreventive nanoparticles that can be targeted as the prophylactic agent for experimental colorectal cancer. Keywords: nanoparticles, guar gum, celecoxib, colorectal cancer, release kinetics, cytotoxicity

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