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1.
Chem Asian J ; : e202400284, 2024 Jul 02.
Artigo em Inglês | MEDLINE | ID: mdl-38953124

RESUMO

Dicarboxylate metallosurfactants (AASM), synthesized by mixing N-dodecyl aminomalonate, -aspartate and -glutamate with CaCl2, MnCl2 and CdCl2, were characterized by XRD, FTIR, and NMR spectroscopy. Layered structures, formed by metallosurfactants, were evidenced from differential scanning calorimetry and thermogravimetric analyses. Solvent-spread monolayer of AASM in combination with soyphosphatidylcholine (SPC) and cholesterol (CHOL) were studied using Langmuir surface balance. With increasing mole fraction of AASM mean molecular area increased and passed through maxima at ~60 mol% of AASMs, indicating molecular packing reorganization. Systems with 20 and 60 mol% AASM exhibited positive deviations from ideal behavior signifying repulsive interaction between the AASM and SPC, while synergistic interactions were established from the negative deviation at other combinations. Dynamic surface elasticity increased with increasing surface pressure signifying formation of rigid monolayer. Transition of monolayer from gaseous to liquid expanded to liquid condensed state was established by Brewster angle microscopic studies. Stability of the hybrid vesicles, formed by AASM+SPC+CHOL, was established by monitoring their size, zeta potential and polydispersity index values over 100 days. Size and spherical morphology of hybrid vesicles were confirmed by transmission electron microscopic studies. Biocompatibility of the hybrid vesicles were established by cytotoxicity studies revealing their possible applications in drug delivery and imaging.

2.
J Oleo Sci ; 73(4): 547-562, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38556288

RESUMO

Physicochemical investigations on the inclusion of anionic polyamidoaminesuccinamic acid dendrimer, generation 5 (PAMAM-SA, G5) with positively charged hybrid vesicles (HCV), prepared using soylecithin, ion pair amphiphile (IPA), cholesterol and dihexadecyldimethylammonium bromide, were investigated by dynamic light scattering, transmission electron/atomic force microscopy (TEM/AFM), differential scanning calorimetry, fluorescence spectroscopy and surface pressure-time isotherm studies. Adsorption of dendrimer onto vesicle surface and subsequent bilayer disruption strongly depends on the bilayer composition and dendrimer concentration. Change in the zeta potential value with increasing dendrimer concentration suggests the dendrimer-vesicle interaction to be electrostatic in nature. AFM studies also confirm the adsorption of dendrimer as well as hole formation in the bilayer. Impact of the inclusion of dendrimer into the bilayer were further investigated through differential scanning calorimetry by monitoring the chain melting temperature and enthalpy of the chain melting processes. Dendrimer at low concentration does not alter bilayer integrity, while hole formations are noted at higher dendrimer concentration. Fluorescence anisotropy studies confirm the adsorption and subsequent bilayer disruption due to dendrimer inclusion. Dendrimer induced vesicle disintegration kinetics conclusively illustrate the transformation of cationic bilayer to monolayer and thereby exposing the role of IPA. In vitro cytotoxicity studies on PAMAM-SA, G5 and HCVs mixtures against human breast cancer cell line suggest that dendrimer-liposome aggregates (dendriosomes) exhibit substantial anticancer activities with insignificant side effects. It is expected that the dendriosomes may have application to host and deliver anticancer drug in the field of targeted drug delivery.


Assuntos
Dendrímeros , Humanos , Dendrímeros/química , Bicamadas Lipídicas/química , Lipossomos , Sistemas de Liberação de Medicamentos , Adsorção
3.
Chem Phys Lipids ; 258: 105364, 2024 01.
Artigo em Inglês | MEDLINE | ID: mdl-38040405

RESUMO

Interactions between a zwitterionic phospholipid, 1, 2-dipalmitoyl-sn-glycero-3-phosphatidylcholine (DPPC) and four anionic phospholipids dihexadecyl phosphate (DHP), 1, 2-dimyristoyl-sn-glycero-3-phosphoglycerol (DMPG), 1, 2-dipalmitoyl-sn-glycero-3-phosphate (DPP) and 1, 2-dipalmitoyl-sn-glycero-3-phospho ethanol (DPPEth) in combination with an additional amount of 30 mol% cholesterol were separately investigated at air-buffer interface through surface pressure (π) - area (A) measurements. π-A isotherm derived parameters revealed maximum negative deviation from ideality for the mixtures comprising 30 mol% anionic lipids. Besides the film functionality, structural changes of the monomolecular films at different surface pressures in the absence and presence of polyamidoamine (PAMAM, generation 4), a cationic dendrimer, were visualised through Brewster angle microscopy and fluorescence microscopic studies. Fluidity/rigidity of monolayers were assessed by surface dilatational rheology studies. Effect of PAMAM on the formation of adsorbed monolayer, due to bilayer disintegration of liposomes (DPPC:anionic lipids= 7:3 M/M, and 30 mol% cholesterol) were monitored by surface pressure (π) - time (t) isotherms. Bilayer disintegration kinetics were dependent on lipid head group and chain length, besides dendrimer concentration. Such studies are considered to be an in vitro cell membrane model where the alteration of molecular orientation play important roles in understanding the nature of interaction between the dendrimer and cell membrane. Liposome-dendrimer aggregates were nontoxic to breast cancer cell line as well as in doxorubicin treated MDA-MB-468 cell line suggesting their potential as drug delivery systems.


Assuntos
Dendrímeros , Fosfolipídeos/química , Lipossomos/química , 1,2-Dipalmitoilfosfatidilcolina/química , Microscopia de Fluorescência , Colesterol/química , Propriedades de Superfície
4.
Environ Monit Assess ; 195(1): 39, 2022 Oct 27.
Artigo em Inglês | MEDLINE | ID: mdl-36301348

RESUMO

Groundwater contamination becomes an alarming threat to the provision of ecosystem services and natural resources. A very high level of groundwater contamination has been observed in the northeastern states particularly in North Tripura district. Therefore, the present study considered the region as a case study to evaluate the hydrogeochemical facies, heavy metal pollution and irrigation indices, and their impact on human health. For the investigation, we have collected a total of 35 groundwater samples from North Tripura district. Hydrogeochemical facies through Piper plot reflect Ca2+-Mg2+-HCO3- and Na+-HCO3- as dominant water types. Gibbs plot identifies the dominance of rock-water interaction process in groundwater hydrochemistry. Geochemical plots indicate the dominance of silicate weathering, ion exchange and carbonate dissolution processes in groundwater mineralisation. The order of trace metal contaminations follows Fe > As > Zn > Mn > Cu > Pb. Results of heavy metal indices suggest above 80% samples are at high risk due to high Fe contamination. The risk of the heavy metal indices is associated with rising elevation in southern part of North Tripura. Findings of health risk assessment study imply that children face much carcinogenic and non-carcinogenic risks than adults because of unsafe levels of Fe and As. Multivariate statistical tools are applied to unravel interrelationships among all ions and trace metals as well as probable hydrogeochemical processes in groundwater. Results of Wilcox and USSL plots suggest 77% samples meet irrigation suitability criteria. Besides, the analysis suggests a better insight to identify hydrogeochemical processes controlling groundwater chemistry and the suitability of groundwater for irrigation and drinking purposes. The study also suggests treatment and sustainable management of groundwater resources is compulsory to reduce trace metal contaminations before public use.


Assuntos
Água Subterrânea , Metais Pesados , Oligoelementos , Poluentes Químicos da Água , Criança , Adulto , Humanos , Qualidade da Água , Monitoramento Ambiental/métodos , Ecossistema , Fácies , Poluentes Químicos da Água/análise , Água Subterrânea/análise , Metais Pesados/análise , Oligoelementos/análise , Água/análise , Índia
5.
IEEE Trans Biomed Circuits Syst ; 14(6): 1323-1332, 2020 12.
Artigo em Inglês | MEDLINE | ID: mdl-33026985

RESUMO

Photoplethysmographic (PPG) measurements from ambulatory subjects may suffer from unreliability due to body movements and missing data segments due to loosening of sensor. This paper describes an on-device reliability assessment from PPG measurements using a stack denoising autoencoder (SDAE) and multilayer perceptron neural network (MLPNN). The missing segments were predicted by a personalized convolutional neural network (CNN) and long-short term memory (LSTM) model using a short history of the same channel data. Forty sets of volunteers' data, consisting of equal share of healthy and cardiovascular subjects were used for validation and testing. The PPG reliability assessment model (PRAM) achieved over 95% accuracy for correctly identifying acceptable PPG beats out of total 5000 using expert annotated data. Disagreement with experts' annotation was nearly 3.5%. The missing segment prediction model (MSPM) achieved a root mean square error (RMSE) of 0.22, and mean absolute error (MAE) of 0.11 for 40 missing beats prediction using only four beat history from the same channel PPG. The two models were integrated in a standalone device based on quad-core ARM Cortex-A53, 1.2 GHz, with 1 GB RAM, with 130 MB memory requirement and latency ∼0.35 s per beat prediction with a 30 s frame. The present method also provides improved performance with published works on PPG quality assessment and missing data prediction using two public datasets, CinC and MIMIC-II under PhysioNet.


Assuntos
Redes Neurais de Computação , Fotopletismografia , Adulto , Idoso , Idoso de 80 Anos ou mais , Humanos , Pessoa de Meia-Idade , Fotopletismografia/instrumentação , Fotopletismografia/métodos , Reprodutibilidade dos Testes , Processamento de Sinais Assistido por Computador , Adulto Jovem
6.
Pharm Res ; 35(10): 198, 2018 Aug 27.
Artigo em Inglês | MEDLINE | ID: mdl-30151753

RESUMO

PURPOSE: Orcinol glucoside (OG) - loaded nanostructured lipid carrier (NLC), coated with polyethylene glycol-25/55-stearate (PEG-25/55-SA), were explored for delivering OG to improve in vitro cytotoxicity against gastrointestinal tract (GIT), colon and hepatoma carcinoma cell lines. It is being expected that the PEGylated formulations would possess the sustainability in withstanding the adverse physiological extremities like the most significant metabolic activities and phase I / II enzymatic activities in the intestines. METHODS: NLCs were prepared using tristearin, oleic acid and PEG-25/55-stearate by hot homogenization-ultrasonic dispersion; characterized by DLS, TEM, SEM, AFM, entrapment efficiency and drug loading capacity studies. RESULTS: NLC diameter ranged from 160 to 230 nm with negative zeta potential of -8 to -20 mV. TEM/SEM and AFM studies suggest spherical and smooth surface morphologies. Differential scanning calorimetry studies reveal the loss of crystallinity when OG was incorporated into the NLC. NLCs showed initial burst release, followed by sustained release of OG. PEG-NLC exhibited superior anticancer activity against GIT and also in hepatoma cancer cell lines. CONCLUSIONS: This is the first report demonstrating a practical approach for possible oral delivery of OG in GIT and targeting hepatoma cancer, warranting further in vivo studies for superior management of GIT cancer.


Assuntos
Portadores de Fármacos/química , Glucosídeos/química , Lipídeos/química , Nanoestruturas/química , Resorcinóis/química , Animais , Antineoplásicos/administração & dosagem , Antineoplásicos/química , Linhagem Celular Tumoral , Neoplasias do Colo , Composição de Medicamentos/métodos , Liberação Controlada de Fármacos , Glucosídeos/administração & dosagem , Humanos , Neoplasias Hepáticas , Camundongos , Ácidos Oleicos/química , Tamanho da Partícula , Polietilenoglicóis/química , Resorcinóis/administração & dosagem , Solubilidade , Neoplasias Gástricas , Triglicerídeos/química , Ondas Ultrassônicas
7.
ACS Omega ; 3(9): 12235-12245, 2018 Sep 30.
Artigo em Inglês | MEDLINE | ID: mdl-31459298

RESUMO

Interaction between negatively charged liposomes and cationic polyamidoamine dendrimers of different generations was investigated through size, zeta potential, turbidity, electron microscopy, atomic force microscopy, fluorescence spectroscopy, and calorimetric studies. Liposomes with the binary combination of 1,2-dipalmitoyl-sn-glycero-3-phosphatidylcholine (DPPC) + dihexadecyl phosphate, DPPC + 1,2-dimyristoyl-sn-glycero-3-phosphoglycerol, DPPC + 1,2-dipalmitoyl-sn-glycero-3-phosphate, and DPPC + 1,2-dipalmitoyl-sn-glycero-3-phosphoethanol were stable up to 60 days. The electrostatic nature of dendrimer-lipid bilayer interaction was evidenced through charge neutralization and subsequent reversal upon added dendrimer to liposome. Dendrimer-liposome interaction depended on its generation (5 > 4 > 3) in addition to the charge, head groups, and hydrocarbon chain length of lipids. Fluorescence anisotropy and differential scanning calorimetry studies suggest the fluidization of the bilayer, although the surface rigidity was enhanced by the added dendrimers. Thermodynamic parameters of the interaction processes were evaluated by isothermal titration and differential scanning calorimetric studies. The binding processes were exothermic in nature. The enthalpy of transition of the chain melting of lipids decreased systematically with increasing dendrimer concentration and generation. Dendrimer-liposome aggregates were nontoxic to healthy human blood cell, suggesting the potential of such aggregates as drug delivery systems.

8.
J Phys Chem B ; 120(41): 10744-10756, 2016 Oct 20.
Artigo em Inglês | MEDLINE | ID: mdl-27659807

RESUMO

Cystine-based gemini surfactants with dodecyl, tetradecyl, hexadecyl, and octadecyl hydrocarbon chains were synthesized, and their interactions with unsaturated (soy phosphatidylcholine, SPC)/saturated (hydrogenated SPC, HSPC) soy phosphatidylcholines in the forms of a monolayer and a model liposome were estimated for different combinations of the components in the mixed systems. Studies of Langmuir monolayers at the air-aqueous buffer interface revealed condensation of the monomolecular films with the addition of surfactants. The effect of surfactants decreased according to the following order: octadecyl > hexadecyl > tetradecyl > dodecyl homologs. The nonideal mixing between the components was estimated using the deviation of the experimental molecular area from the ideal area per molecule. The excess molecular area increased with the increase in the surfactant chain length and phospholipid saturation. The 50 mol % mixture of cystine derivatives and phospholipids formed thermodynamically stable monolayers. The surfactants increased the rigidity of SPC monolayers and decreased that of HSPC monolayers, as observed by the studies of surface dialational rheology. The film structure at the air-water interface could differentiate the SPC- and HSPC-comprising systems through the formation of organized regions, especially at a higher surface pressure. The constriction of surfactant/phospholipid hybrid vesicles was observed with an increase in the length of surfactant hydrocarbon chains. The negative zeta potential of vesicles took the highest values and did not change with time for 20 and 50 mol % surfactant. The spherical shape of the vesicles was confirmed by transmission electron microscopy. Differential scanning calorimetry revealed an increase in fluidity of HSPC bilayers and rigidity of SPS bilayers under the influence of surfactants. These effects were confirmed by fluorescence spectroscopy. All of the vesicle formulations were found to be nontoxic from the 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl-tetrazolium bromide assay, suggesting their potential as a novel membranous system for the delivery of drugs, genetic materials, vaccines, and other therapeutic agents.

9.
Langmuir ; 32(38): 9816-25, 2016 09 27.
Artigo em Inglês | MEDLINE | ID: mdl-27588340

RESUMO

The impact of saturation and unsaturation in the fatty acyl hydrocarbon chain on the physicochemical properties of nanostructured lipid carriers (NLCs) was investigated to develop novel delivery systems loaded with an anticancer drug, ursolic acid (UA). Aqueous NLC dispersions were prepared by a high-pressure homogenization-ultrasonication technique with Tween 80 as a stabilizer. Mutual miscibility of the components at the air-water interface was assessed by surface pressure-area measurements, where attractive interactions were recorded between the lipid mixtures and UA, irrespective of the extent of saturation or unsaturation in fatty acyl chains. NLCs were characterized by combined dynamic light scattering, transmission electron microscopy (TEM), atomic force microscopy (AFM), differential scanning calorimetry, drug encapsulation efficiency, drug payload, in vitro drug release, and in vitro cytotoxicity studies. The saturated lipid-based NLCs were larger than unsaturated lipids. TEM and AFM images revealed the spherical and smooth surface morphology of NLCs. The encapsulation efficiency and drug payload were higher for unsaturated lipid blends. In vitro release studies indicate that the nature of the lipid matrix affects both the rate and release pattern. All UA-loaded formulations exhibited superior anticancer activity compared to that of free UA against human leukemic cell line K562 and melanoma cell line B16.


Assuntos
Antineoplásicos/farmacologia , Lipídeos/química , Nanoestruturas , Triterpenos/química , Varredura Diferencial de Calorimetria , Linhagem Celular Tumoral , Humanos , Ácido Ursólico
10.
J Oleo Sci ; 65(5): 399-411, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27150333

RESUMO

The physicochemical properties of large unilamellar vesicles (LUVs) were assessed with respect to lipid composition, pH, time, and temperature by monitoring their size, zeta potential, drug payload, and thermal behavior. A conventional thin film hydration technique was employed to prepare liposomes from soy phosphatidylcholine (SPC), dipalmitoylphosphatidylcholine (DPPC), dipalmitoylphosphatidylglycerol (DPPG), and a 7:3 (M/M) mixture of DPPC+DPPG along with 30 mole% cholesterol in each combination. While the size of liposomes depended on lipid composition, pH and temperature, the zeta potential was found to be independent of the pH of the medium, although it varied with liposome type. Spherical morphology and bilayer were observed by electron microscopy. The phase transition temperature increased with decreasing pH. Membrane micro-viscosity showed the highest value for SPC, and membrane rigidity increased with increasing pH. The entrapment efficiency of liposomes with reference to curcumin was as follows: DPPC>DPPC+DPPG>DPPG>SPC. Sustained release of curcumin was observed for all liposomes. Curcumin-loaded liposomes exhibited substantial antibacterial activity against the gram-positive bacteria Bacillus amyloliquefaciens. Additional studies are needed to improve the understanding of the effect of formulation variables on the physicochemical stability of liposomes.


Assuntos
Antibacterianos/farmacologia , Bacillus amyloliquefaciens/efeitos dos fármacos , Curcumina/farmacologia , Lipídeos/química , Lipossomos/química , Temperatura , Antibacterianos/química , Físico-Química , Curcumina/química , Portadores de Fármacos/química , Concentração de Íons de Hidrogênio , Testes de Sensibilidade Microbiana , Tamanho da Partícula , Propriedades de Superfície
11.
J Oleo Sci ; 65(5): 419-30, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27150334

RESUMO

Mutual miscibility of soylecithin, tristearin, fatty acids (FAs), and curcumin was assessed by means of surface pressure-area isotherms at the air-solution interface in order to formulate modified solid lipid nanoparticles (SLN). Appearance of minima in the excess area (Aex) and changes in free energy of mixing (∆G(0)ex) were recorded for systems with 20 mole% FAs. Modified SLNs, promising as topical drug delivery systems, were formulated using the lipids in combination with curcumin, stabilized by an aqueous Tween 60 solution. Optimal formulations were assessed by judiciously varying the FA chain length and composition. Physicochemical properties of SLNs were studied such as the size, zeta potential (by dynamic light scattering), morphology (by freeze fracture transmission electron microscopy), and thermal behavior (by differential scanning calorimetry). The size and zeta potential of the formulations were in the range 300-500 nm and -10 to -20 mV, respectively. Absorption and emission spectroscopic analyses supported the dynamic light scattering and differential scanning calorimetry data and confirmed localization of curcumin to the palisade layer of SLNs. These nanoparticles showed a sustained release of incorporated curcumin. Curcumin-loaded SLNs were effective against a gram-positive bacterial species, Bacillus amyloliquefaciens. Our results on the physicochemical properties of curcumin-loaded SLNs, the sustained release, and on antibacterial activity suggest that SLNs are promising delivery agents for topical drugs.


Assuntos
Antibacterianos/farmacologia , Bacillus amyloliquefaciens/efeitos dos fármacos , Curcumina/farmacologia , Ácidos Graxos/química , Lipídeos/química , Nanopartículas/química , Polissorbatos/química , Antibacterianos/química , Varredura Diferencial de Calorimetria , Curcumina/química , Portadores de Fármacos/química , Testes de Sensibilidade Microbiana , Soluções , Termodinâmica
12.
J Phys Chem B ; 119(11): 4251-62, 2015 Mar 19.
Artigo em Inglês | MEDLINE | ID: mdl-25715819

RESUMO

Ion-pair amphiphiles (IPAs) are neoteric pseudo-double-tailed compounds with potential as a novel substitute of phospholipid. IPA, synthesized by stoichiometric/equimolar mixing of aqueous solution of hexadecyltrimethylammonium bromide (HTMAB) and sodium dodecyl sulfate (SDS), was used as a potential substituent of naturally occurring phospholipid, soylecithin (SLC). Vesicles were prepared using SLC and IPA in different ratios along with cholesterol. The impact of IPA on SLC was examined by way of surface pressure (π)-area (A) measurements. Associated thermodynamic parameters were evaluated; interfacial miscibility between the components was found to depend on SLC/IPA ratio. Solution behavior of the bilayers, in the form of vesicles, was investigated by monitoring the hydrodynamic diameter, zeta potential, and polydispersity index over a period of 100 days. Size and morphology of the vesicles were also investigated by electron microscopic studies. Systems comprising 20 and 40 mol % IPA exhibited anomalous behavior. Thermal behavior of the vesicles, as scrutinized by differential scanning calorimetry, was correlated with the hydrocarbon chain as well as the headgroup packing. Entrapment efficiency (EE) of the vesicles toward the cationic dye methylene blue (MB) was also evaluated. Vesicles were smart enough to entrap the dye, and the efficiency was found to vary with IPA concentration. EE was found to be well above 80% for some stable dispersions. Such formulations thus could be considered to have potential as novel drug delivery systems.


Assuntos
Materiais Biomiméticos/química , Interações Hidrofóbicas e Hidrofílicas , Membranas Artificiais , Ar , Soluções Tampão , Colesterol/química , Portadores de Fármacos/química , Hidrodinâmica , Concentração de Íons de Hidrogênio , Lecitinas/química , Azul de Metileno/química , Modelos Moleculares , Conformação Molecular , Pressão , Glycine max/química
13.
J Oleo Sci ; 63(11): 1185-93, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-25341498

RESUMO

Studies on the interaction of different generation poly (amido amine) (PAMAM) dendrimers (2G, 4G and 6G) and liposomes of different compositions were carried out by a combined turbidity, dynamic light scattering and atomic force microscopic measurements. Liposomes comprising soy lecithin (SLC, negative surface charge), 1, 2-palmitoyl-sn-glycero-3-phosphatidylcholine (DPPC, mildly positive surface charge), 1,2-dipalmitoyl-sn-glycero-3-phospho-(1'-rac-glycerol (DPPG, negatively charged) and a biologically simulated mixture of DPPC + DPPG (7:3, M/M, negatively charged) were used as model bilayers. 30 wt% cholesterol was used in each combination as it is known to control the fluidity of membrane bilayers. Silica was used as a negatively charged hard sphere model with an aim to compare the results. Both the turbidity and hydrodynamic diameter values of all the liposomes, except DPPC, passed through maxima upon the progressive addition of PAMAM; the effect was insignificant in case of DPPC. Formation of dendriosome, a complex formed between dendrimer and liposome, resulted in the charge reversal of the negatively charged liposomes. Interaction between PAMAM and liposome was found to be governed by electrostatic as well as hydrogen bonding. Generation dependent PAMAM activity followed the order: 6G >4G>2G in terms of overall dendrimer concentration. However, interestingly, the order was reverse when PAMAM activity was considered in terms of total end group concentrations. AFM studies reveal the rupture of bilayer structure upon addition of dendrimer.


Assuntos
Aminas/química , Fenômenos Químicos , Dendrímeros/química , Bicamadas Lipídicas/química , Lipossomos , Colesterol , Hidrodinâmica , Ligação de Hidrogênio , Fluidez de Membrana , Dióxido de Silício , Eletricidade Estática , Propriedades de Superfície
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