scholarly journals Microneedle-Assisted Percutaneous Delivery of Paeoniflorin-Loaded Ethosomes

Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3371 ◽  
Author(s):  
Yahua Cui ◽  
Yujia Mo ◽  
Qi Zhang ◽  
Wanwan Tian ◽  
Yutao Xue ◽  
...  
Keyword(s):  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Topical Administration ◽  
Water Soluble ◽  
Orthogonal Experimental Design ◽  
Therapeutic Effects ◽  
Transdermal Drug Delivery System ◽  
Water Soluble Drug ◽  
Transmission Electron ◽  
Main Component

Paeoniflorin, the main component of total glucosides of paeony (TGP), shows good therapeutic effects in arthritis, but has low bioavailability when administered orally. Avoiding such a deficiency for topical administration would expand its clinical application. This study aimed to avoid these limitations by using nanotechnology (ethosomes) and a physical approach (microneedles). Paeoniflorin-loaded ethosomal formulation (TGP-E) was optimized and evaluated in terms of entrapment efficiency (EE), particle size (PS), zeta potential (ZP), polydispersity index (PDI) and morphology. TGP-E was prepared by the hot injection method and optimized by single-factor tests and an orthogonal experimental design. The optimized paeoniflorin-loaded ethosomes had EE of 27.82 ± 1.56%, PS of 137.9 ± 7.57 nm with PDI of 0.120 ± 0.005, ZP of −0.74 ± 0.43 mV. Ethosomes showed a nearly spherical shape under the transmission electron microscope (TEM). The optimal microneedle-assisted (MN-assisted) conditions were obtained at a microneedle length of 500 μm, a pressure of 3 N and an action time of 3 min. The cumulative penetration amounts (Qn) of TGP solution transdermal (ST) and MN-assisted TGP solution transdermal (MST) were 24.42 ± 8.35 μg/cm2 and 548.11 ± 10.49 μg/cm2, respectively. Qn of TGP-E transdermal (PT) and MN-assisted TGP-E transdermal (MPT) were 54.97 ± 4.72 μg/cm2 and 307.17 ± 26.36 μg/cm2, respectively. These findings indicate that use of ethosomes and microneedles can both enhance the penetration ofpaeoniflorin, but for the water-soluble drug, there is no obvious synergism between nanotechnology and microneedles for enhancing penetration in a transdermal drug delivery system.

scholarly journals Solubility Enhancement of Ibuprofen by Adsorption onto Spherical Porous Calcium Silicate

Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 767
Author(s):  
Yayoi Kawano ◽  
Shiyang Chen ◽  
Takehisa Hanawa
Keyword(s):  
Calcium Silicate ◽  
Spherical Shape ◽  
Water Soluble ◽  
Dissolution Behavior ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Dsc Measurements ◽  
Water Soluble Drug ◽  
Main Component ◽  
Poorly Water Soluble Drug

The solubility of a drug is higher when it is in an amorphous form than when it is in a crystalline form. To enhance the solubility of ibuprofen (IBU), a poorly water-soluble drug, we attempted to adsorb IBU onto spherical porous calcium silicate (Florite® PS300, PS300) in two ways: the evaporation (EV) and sealed heating (SH) methods. The crystallinity of the samples was evaluated using powder X-ray diffraction analysis (PXRD) and differential scanning calorimetry (DSC). The molecular interaction between IBU and PS300 was evaluated with FTIR. In addition, the dissolution behavior of IBU in the samples was assessed by the dissolution test. Based on the results of the PXRD and DSC measurements, both methods allowed adsorption of IBU onto PS300, and IBU was amorphized. Based on the FTIR observations, in the SH or EV mixtures containing 10% and 30% IBU, respectively, it seemed that the IBU molecules intermolecularly interacted with calcium molecules as the main component of PS300. Improvement in the solubility of IBU was observed with both methods; however, the dissolution rate of IBU from samples prepared via SH was higher than that from EV, or of IBU crystals. Collectively, our findings indicate that the petal-like structure of PS300, which has a spherical shape and good flowability, is an effective tool for adsorbing IBU onto PS300 via SH.

scholarly journals Preparation, characterization and scale-up of sesamol loaded solid lipid nanoparticles

2012 ◽  
Vol 2 (1) ◽  
pp. 8 ◽  
Author(s):  
Vandita Kakkar ◽  
Indu Pal Kaur
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Scale Up ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Solid Lipid ◽  
Transmission Electron ◽  
The Brain

Sesamol loaded solid lipid nanoparticles (SSLNs) were prepared with the aim of minimizing its distribution to tissues and achieving its targeting to the brain. Three scale-up batches (100x1 L) of S-SLNs were prepared using a microemulsification technique and all parameters were statistically compared with the small batch (1x;10 mL). S-SLNs with a particle size of less than 106 nm with a spherical shape (transmission electron microscopy) were successfully prepared with a total drug content and entrapment efficiency of 94.26±2.71% and 72.57±5.20%, respectively. Differential scanning calorimetry and infrared spectroscopy confirmed the formation of lipidic nanoparticles while powder X-ray diffraction revealed their amorphous profile. S-SLNs were found to be stable for three months at 5±3°C in accordance with International Conference on Harmonisation guidelines. The SLN preparation process was successfully scaled-up to a 100x batch on a laboratory scale. The procedure was easy to perform and allowed reproducible SLN dispersions to be obtained.

scholarly journals FORMULATION AND CHARACTERIZATION OF GASTRORETENTIVE FLOATING MICROBALLOONS OF POORLY WATER-SOLUBLE DRUG DIACEREIN

2021 ◽  
Vol 15 (5) ◽  
pp. 8-12
Author(s):  
Kajal Tomer ◽  
Dilip Kumar Gupta
Keyword(s):  
Particle Size ◽  
Entrapment Efficiency ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Diffusion Method ◽  
Acrylic Polymer ◽  
Water Soluble Drug ◽  
Technological Advances ◽  
S 100

The drug can be released in a controlled manner using a gastro retentive dosage type. The main focus on the novel technological advances in the floating drug delivery method for gastric retention. The preparation of diacerein micro balloon is done by solvent diffusion method, using acrylic polymer like Eudragit S 100 and HPMC K4 M. The various evaluation of the prepared floating microsphere like its % yield, drug entrapment efficiency, particle size in-vitro dissolution, buoyancy, was studied. The floating microsphere was found to be spherical and range from 85 μm - 192 μm. Whereas the buoyancy in gastric mucosa between the range 30.5% -49.5%. The % yield and % entrapment efficiency were found under the range 61% - 82% and 45.1–84.1% respectively. The microsphere showed favorable in-vitro dissolution 76.8 to 94.45. The optimized formulation was found based on evaluation of floating micro-balloons, Formulation (M3E3) showed the best result as particle size 192 μm, DDE 84.1%, in vitro drug release 94.5%, and in vitro buoyancy 49.5%. all the formulations showed controlled release up to 24 hours.

scholarly journals Nanoencapsulation of Nimodipine in Novel Biocompatible Poly(propylene-co-butylene succinate) Aliphatic Copolyesters for Sustained Release

2009 ◽  
Vol 2009 ◽  
pp. 1-11 ◽  
Author(s):  
Sofia Papadimitriou ◽  
George Z. Papageorgiou ◽  
Feras I. Kanaze ◽  
Manolis Georgarakis ◽  
Dimitrios N. Bikiaris
Keyword(s):  
Chemical Interaction ◽  
Spherical Shape ◽  
Water Soluble ◽  
Degree Of Crystallinity ◽  
Butylene Succinate ◽  
Melt Polycondensation ◽  
Water Soluble Drug ◽  
The Matrix ◽  
Model Drug ◽  
Poly Propylene

Biocompatible poly(propylene-co-butylene succinate) (PPBSu) copolyesters, containing up to 50 mol% butylene succinate units, were synthesized by the two-stage melt polycondensation method (esterification and polycondensation). The copolymers were fully characterized and biocompatibility studies were also performed. They were proved to be biocompatible and they were used as polymer matrices for the preparation of drug loaded nanoparticles. Nimodipine was selected as a model hydrophobic poorly water soluble drug. From the results obtained by dynamic light scattering (DLS) and scanning electron microscopy (SEM), drug loaded copolymer nanoparticles were found to exhibit a spherical shape and their mean diameter appeared in the range of 180–200 nm. Fourier Transformation-Infrared Spectroscopy (FTIR) spectra indicated that no chemical interaction between the drug and the matrix could be justified, while Wide-Angle X-Ray Diffraction (WAXD) patterns proved a low degree of crystallinity of Nimodipine in the nanoparticles. The release behavior of the model drug from nanoparticles was also investigated in order to identify modifications and find out any possible correlation between the chemical composition of the polymer matrix and the drug release rates.

scholarly journals Method Development Technologies for Clopidogrel Bisulphate by Improving Solubility and Bioavailability

2021 ◽  
Vol 6 (02) ◽  
pp. 15-21
Author(s):  
Deevan Paul A. ◽  
Avilala Neelima ◽  
Chitra Prasanthi ◽  
Navyaja Kota
Keyword(s):  
Drug Release ◽  
Method Development ◽  
Physical Nature ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Adenosine Diphosphate ◽  
Water Soluble ◽  
Irreversible Inhibitor ◽  
Water Soluble Drug ◽  
Drug Entrapment Efficiency

Clopidogrel bisulphate (CB) is a crystalline, poorly water-soluble drug of bioavailability less than 50%. The drug is an irreversible inhibitor of the P2Y12 adenosine diphosphate receptor found on the membranes of platelet cells. The present work was performed using different polymers such as Polyvinylpyrrolidone (PVP) K-30 and polyvinyl alcohol with varied surfactants such as Tween 80 in comparison by using superdisintegrants like Sodium Starch Glycolate (SSG) and Microcrystalline Cellulose (MCC). By performing the particle size distribution, the size ranges from 232.6 nm to 995.6 nm and the polydispersity index ranges from 0.11 to 0.96, these ranges indicating the good physical nature of nanoparticles. The drug entrapment efficiency (DEE) of clopidogrel bisulphate nanoparticles was found to be in the range of 30.10% to 94.4%. From the study, it was found that F2 formulation containing PVP K-30 and L-arginine has given the best release in 80mins and the maximum cumulative drug release was 96.8% in comparison with other formulation, and the dissolution studies were performed for the seven formulations of prepared clopidogrel bisulphate granules among which F5 formulation containing crospovidone has given maximum drug release of 91.6% within 80mins. Here we state that the method development technologies improve the solubility and bioavailability studies by producing the nanoparticles.

Fabrication and characterization of nanostructured lipid carrier system for effective delivery of poorly water-soluble drug quetiapine fumarate

2021 ◽  
pp. 6235-6244
Author(s):  
Deepak Patil ◽  
Seema Pattewar ◽  
Sarvesh Palival ◽  
Gargi Patil ◽  
Swapnil Sharma
Keyword(s):  
Entrapment Efficiency ◽  
Water Soluble ◽  
Nanostructured Lipid Carrier ◽  
Quetiapine Fumarate ◽  
Water Soluble Drug ◽  
Effective Delivery ◽  
Capmul Mcm ◽  
Central Composite ◽  
Poorly Water Soluble Drug

The aim of present study is to investigate the potential of nanostructured lipid carriers (NLCs) in improving the oral bioavailability of quetiapine fumarate, a second-generation antipsychotic drug. Quetiapine Fumarate (QF) loaded NLC were prepared by hot homogenization followed by an ultrasonication method. Response surface methodology - central composite design (CCD) was used to systemically examine the influence of concentration of capmul MCM EP, concentration of poloxamer 188 and concentration of egg lecithin on particle size (PS) and % entrapment efficiency (% EE) and to optimize the NLC formulation. The CCD consists of three factored design with five levels, plus and minus alpha (axial points), plus and minus 1 (factorial points) and the centre point. A mathematical relationship between variables was created by using Design Expert software Version 12. The statistical evaluations revealed that three independent variables were the important factors that affected the PS and % EE of QF loaded NLC. The best fitted mathematical model was linear and quadratic for PS and % EE respectively. The optimized formulations found with 218.1±0.14nm of PS and 93±0.16% of % EE. Results illustrated the superiority of developed QF loaded NLC formulation as a stable drug delivery system, providing better bioavailability with the possibility of better treatment for psychological disorders.

scholarly journals FORMULATION, OPTIMIZATION, AND IN VITRO EVALUATION OF POLYMERIC NANOSUSPENSION OF FLURBIPROFEN

2019 ◽  
pp. 183-191
Author(s):  
PANKAJ JADHAV ◽  
ADHIKRAO YADAV
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Hydroxypropyl Methylcellulose ◽  
Entrapment Efficiency ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Dissolution Profile ◽  
Scanning Calorimetry ◽  
Transmission Electron

Objective: At present, more than 40% of drugs are poorly water-soluble that leads to reduced bioavailability. The objective of the present investigation was to overcome the issue of poor aqueous solubility of drug; therefore, stable flurbiprofen (FBF) nanosuspensions were developed by nanoprecipitation method. Materials and Methods: Based on particle size, zeta potential, and entrapment efficiency, the polymeric system of hydroxypropyl methylcellulose E15 and poloxamer 188 was used effectively. The prepared formulations were evaluated for Fourier transform infrared spectroscopy, transmission electron microscopy, differential scanning calorimetry, powder X-ray diffraction, saturation solubility, entrapment efficiency, particle size, zeta potential, dissolution profile, and stability. Results: The resultant FBF nanosuspensions depicted particles in size range of 200–400 nm and were physically stable. After nanonization, the crystallinity of FBF was slightly reduced in the presence of excipients. The aqueous solubility and dissolution rate of all FBF nanosuspensions were significantly increased as compared with FBF powder. Conclusion: This investigation demonstrated that nanoprecipitation is a promising method to develop stable polymeric nanosuspension of FBF with significant increase in its aqueous solubility.

Properties of Amorphous Silica Entrapped Isoniazid Drug Delivery System

2011 ◽  
Vol 364 ◽  
pp. 134-138 ◽  
Author(s):  
Azwana Ab Wab Hajarul ◽  
Dyana Zakaria Nor ◽  
Azlan Abdul Aziz ◽  
Abdul Razak Khairunisak
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Synthesis Temperature ◽  
Stability Study ◽  
Water Soluble ◽  
Organic Precursor ◽  
Synthesis Parameters ◽  
Water Soluble Drug ◽  
Transmission Electron

This work describes the properties of silica drug delivery system (DDS) produced using micelles entrapment approach. Isoniazid, which is a water soluble drug for tuberculosis was used in the system. The effects of synthesis parameters were systematically studied such as synthesis temperature (38-70°C), amount of butanol co-solvent (6-18 ml), and amount of Si organic precursor (2-8 ml). From transmission electron microscope (TEM) images, the size of DDS could be tuned from 21-104 nm by changing the reaction temperature. The increase of butanol co-solvent enlarged the size of DDS in the range of 40-94 nm. A similar trend was observed for DDS with increasing organic Si precursor whereby the particle size could be tuned from 40-132 nm. However, at high organic Si precursor of > 2 ml, a bimodal structure of DDS was observed. Stability study in biological media at 37°C of selected sample showed that the produced DDS had acceptable degree of agglomeration.

scholarly journals Fabrication and Evaluation of Quercetin Nanoemulsion: A Delivery System with Improved Bioavailability and Therapeutic Efficacy in Diabetes Mellitus

2022 ◽  
Vol 15 (1) ◽  
pp. 70
Author(s):  
Manohar Mahadev ◽  
Hittanahalli S. Nandini ◽  
Ramith Ramu ◽  
Devegowda V. Gowda ◽  
Zainab M. Almarhoon ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Droplet Size ◽  
Tissue Injury ◽  
Ethyl Oleate ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Morphological Characterization ◽  
Tween 20 ◽  
Box Behnken Design ◽  
Transmission Electron

The current study was intended to fabricate and evaluate ultrasonically assisted quercetin nanoemulsion (Que-NE) for improved bioavailability and therapeutic effectiveness against diabetes mellitus in rats. Ethyl oleate, Tween 20, and Labrasol were chosen as oil, surfactant, and cosurfactant, respectively. Box–Behnken design (BBD) was employed to study the influence of process variables such as % surfactant and cosurfactant mixture (Smix) (5 to 7%), % amplitude (20–30%) and sonication time (2.5–7.5 min) on droplet size, polydispersibility index (PDI), and % entrapment efficiency (%EE) were studied. The optimization predicted that 9% Smix at 25% amplitude for 2.5 min would produce Que-NE with a droplet size of 125.51 nm, 0.215 PDI, and 87.04% EE. Moreover, the optimized Que-NE exhibited appreciable droplet size and PDI when stored at 5, 30, and 40 °C for 45 days. Also, the morphological characterization by transmission electron microscope (TEM) indicated the spherical shape of the optimized nanoemulsion. Furthermore, the Que-NE compared to pure quercetin exhibited superior release and enhanced oral bioavailability. The streptozocin-induced antidiabetic study in rats revealed that the Que-NE had remarkable protective and therapeutic properties in managing body weight, blood glucose level, lipid profile, and tissue injury markers, alongside the structure of pancreatic β-cells and hepatocytes being protected. Thus, the developed Que-NE could be of potential use as a substitute strategy for diabetes.

Preparation and In Vivo Characterization of Niosomal Carriers of the Antidiabetic Drug Repaglinide

2015 ◽  
Vol 8 (1) ◽  
pp. 2756-2767 ◽  
Author(s):  
Shrishti Namdev ◽  
Kishore Gujar ◽  
Satish Mandlik ◽  
Preeti Jamkar
Keyword(s):  
Particle Size ◽  
Factorial Design ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Therapeutic Effects ◽  
Drug Release Profile ◽  
Independent Variables ◽  
Span 60

The objective of this study is to prepare and characterise repaglinide niosomes using the Factorial Design strategy.Repaglinide is a potent second-generation oral hypoglycemic agent and has short half-life of 1 hour and oral bioavailability of 50%. Preparing Niosomal drugdelivery of repaglinide may increase its bioavailability which would lead to better therapeutic effects, reduce the frequency of dosing from twice a day to once a day and decrease side effects. The preliminary study was carried out for selection of surfactant and method of preparation based on least particle size and highest entrapment efficiency. For niosome preparation, organic solvent injection method was selected and span 60, cholesterol were selected as variable. A32 factorial design was used to optimize the effect of amounts of span 60(X1) and cholesterol (X2) which were the independent variables. Particle size (Y1) and entrapment efficiency (Y2) were the dependent variables. Relation between the dependent and independent variables were drawn out from the mathematical equations and response surface plots.Statistical analysis was performed using ANOVA which was found to be significant and quadratic equation was obtained by MLRA. The particle size was found to be in range of 144-497 nm and entrapment efficiency between 54-88%. Scanning electron microscopy indicated the spherical shape of the niosomes and formation of vesicle. Zeta potential analysis showed negatively charged surface with value of-36.7 mV. In vitro drug release profile showed that drug released fast initially followed by a slow release. In vivo pharmacokinetic study revealed that the niosomal preparation showed significant decrease in blood glucose level when compared to free repaglinide. The developed niosomal system also has potential of maintaining therapeutic level of RPG for longer period of time.Thus,the niosomes could be promising carriers for delivery ofrepaglinide with increased 

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