scholarly journals POLYMERIC NANOPARTICLES FOR IMPROVED BIOAVAILABILITY OF CILNIDIPINE

2017 ◽  
Vol 9 (4) ◽  
pp. 129 ◽  
Author(s):  
Rohit Mishra ◽  
Showkat R. Mir ◽  
Saima Amin
Keyword(s):  
Particle Size ◽  
Glycolic Acid ◽  
Antihypertensive Effect ◽  
Polymeric Nanoparticles ◽  
Relative Bioavailability ◽  
Diffusion Method ◽  
The Novel ◽  
Hypertensive Rats ◽  
Treatment Of Hypertension ◽  
Emulsification Solvent Evaporation

Objective: In the present study, we aimed to optimize, characterize and evaluate poly lactic-glycolic acid nanoparticles of cilnidipine for improved permeation across the gastrointestinal tract.Methods: Poly lactic-glycolic acid-cilnidipine (PLGA-CIL) nanoparticles were prepared by an emulsification solvent evaporation/diffusion method using polyvinyl alcohol (PVA) as a surfactant. The prepared nanoparticles were successfully characterized for particle size, shape, drug release and pharmacological effect.Results: Polymeric nanoparticles of cilnidipine at a dose of 10 mg had a small particle size of 272 nm with smooth morphology. Nearly 81% of the drug was encapsulated in the polymeric structure and showed 18.99±0.59% of release at pH 1.2 within 3h, however, at pH 6.8 the release was 80.89±1.59%. The formulation had a better antihypertensive effect on methylprednisolone-induced hypertensive rats. The relative bioavailability of the nanoparticles was found to be 2.44 and 2.94 fold higher than the tablet and drug suspension respectively.Conclusion: The results demonstrated that the novel delivery system offers an effective strategy for treatment of hypertension.

scholarly journals Translating the fabrication of protein-loaded poly(lactic-co-glycolic acid) nanoparticles from bench to scale-independent production using microfluidics

2020 ◽  
Vol 10 (3) ◽  
pp. 582-593 ◽  
Author(s):  
Carla B. Roces ◽  
Dennis Christensen ◽  
Yvonne Perrie
Keyword(s):  
Particle Size ◽  
Glycolic Acid ◽  
Polymeric Nanoparticles ◽  
Physicochemical Characteristics ◽  
European Medicines Agency ◽  
Protein Encapsulation ◽  
Human Use ◽  
Rate Ratios ◽  
The Impact ◽  
Process Controls

AbstractIn the formulation of nanoparticles, poly(lactic-co-glycolic acid) (PLGA) is commonly employed due to its Food and Drug Administration and European Medicines Agency approval for human use, its ability to encapsulate a variety of moieties, its biocompatibility and biodegradability and its ability to offer a range of controlled release profiles. Common methods for the production of PLGA particles often adopt harsh solvents, surfactants/stabilisers and in general are multi-step and time-consuming processes. This limits the translation of these drug delivery systems from bench to bedside. To address this, we have applied microfluidic processes to develop a scale-independent platform for the manufacture, purification and monitoring of nanoparticles. Thereby, the influence of various microfluidic parameters on the physicochemical characteristics of the empty and the protein-loaded PLGA particles was evaluated in combination with the copolymer employed (PLGA 85:15, 75:25 or 50:50) and the type of protein loaded. Using this rapid production process, emulsifying/stabilising agents (such as polyvinyl alcohol) are not required. We also incorporate in-line purification systems and at-line particle size monitoring. Our results demonstrate the microfluidic control parameters that can be adopted to control particle size and the impact of PLGA copolymer type on the characteristics of the produced particles. With these nanoparticles, protein encapsulation efficiency varies from 8 to 50% and is controlled by the copolymer of choice and the production parameters employed; higher flow rates, combined with medium flow rate ratios (3:1), should be adopted to promote higher protein loading (% wt/wt). In conclusion, herein, we outline the process controls for the fabrication of PLGA polymeric nanoparticles incorporating proteins in a rapid and scalable manufacturing process.

scholarly journals FORMULATION AND EVALUATION OF ISORHAMNETIN LOADED POLY LACTIC-CO-GLYCOLIC ACID NANOPARTICLES

2017 ◽  
Vol 10 (11) ◽  
pp. 177
Author(s):  
Kandakumar Settu ◽  
Manju Vaiyapuri
Keyword(s):  
Particle Size ◽  
Glycolic Acid ◽  
Polymeric Nanoparticles ◽  
Double Emulsion ◽  
Spherical Shape ◽  
Particle Size Analysis ◽  
Size Analysis ◽  
Characteristic Variety ◽  
Sem Image ◽  
Flexible Technology

  Objective: The aim of the present study was formulation and evaluation of isorhamnetin loaded poly lactic-co-glycolic acid (PLGA) polymeric nanoparticles (NPs).Methods: The present study was designed to incorporate the isorhamnetin in PLGA formulation by double emulsion solvent evaporation method, which offers a dynamic and flexible technology for enhancing drug solubility due to their biphasic characteristic, variety in design, composition and assembly. Synthesized isorhamnetin-PLGA NPs were characterized by Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), and particle size analyzer. We tested the efficacy of isorhamnetin-PLGA NPs in HepG2 cell lines.Results: From the FTIR result, we concluded that -C-N-, -C=C-, N-H, C-N, N-O, O-H, and C-H are the functional groups present in isorhamnetin-PLGA NPs, SEM image shows spherical shape of particles. The particle size analysis result shows 255-342 nm range of particles. Isorhamnetin-PLGA NPs significantly enhanced (p<0.05) the antiproliferative effect when compared to the plain drug.Conclusion: This study concluded that the newly formulated NP drug delivery systems of isorhamnetin provided an insight into the therapeutic effectiveness of the designed formulation for the treatment of chemotherapy.

Evaluation of the Enhanced Oral Effect of Omapatrilat-Monolein Nanoparticles Prepared by the Emulsification-Diffusion Method

2006 ◽  
Vol 6 (9) ◽  
pp. 3134-3138 ◽  
Author(s):  
D. Tamayo-Esquivel ◽  
A. Ganem-Quintanar ◽  
A. L. Martínez ◽  
M. Navarrete-Rodríguez ◽  
S. Rodríguez-Romo ◽  
...  
Keyword(s):  
Mixed Micelles ◽  
Antihypertensive Effect ◽  
High Surface ◽  
High Surface Area ◽  
Diffusion Method ◽  
Hypertensive Rats ◽  
Adhesive Properties ◽  
Spontaneously Hypertensive ◽  
Molecular Dispersion ◽  
Interesting System

In the present study, the emulsification-diffusion method was optimized in order to obtain omapatrilat/monolein-nanoparticles (omapatrilat/MO-nanoparticles). The antihypertensive effect of omapatrilat/MO-nanoparticles in spontaneously hypertensive rats (SHR) after oral administration was evaluated. The results indicated that the variables involved in the process did not have an influence on particle size, and that the former is directly determined by the amphiphilic properties of MO. When SHR were orally treated with omapatrilat/MO-nanoparticles, blood pressure was significantly reduced and completely normalized after three days. This effect was markedly higher than that observed with omapatrilat suspensions. The effect of omapatrilat/MO-nanoparticles can be attributed to: (i) The molecular dispersion of the drug into the lipophilic domain of monolein's bicontinuous phase; (ii) the adhesive properties of the nanodispersion on the gastrointestinal mucosa; (iii) the high surface area of the dispersion; (iv) the intraluminal interaction between MO, the mixed micelles arising from the digestive process, and omapatrilat; and (v) the well-known absorption-promoting properties of lipids, and in particular, of MO. MO-nanoparticles can be an interesting system to increase the oral bioavailability of drugs.

Formulation and Evaluation of Mefloquine Hydrochloride Nanoparticles

2014 ◽  
Vol 7 (1) ◽  
pp. 2377-2386
Author(s):  
Dilip Kumar Gupta ◽  
B K Razdan ◽  
Meenakshi Bajpai
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Taste Masking ◽  
Diffusion Method ◽  
Drug Entrapment Efficiency ◽  
Resistant Strains ◽  
Vitro Release

The present study deals with the formulation and evaluation of mefloquine hydrochloride nanoparticles. Mefloquine is a blood schizonticidal quinoline compound, which is indicated for the treatment of mild-to-moderate acute malarial infections caused by mefloquine-susceptible multi-resistant strains of P. falciparum and P. vivax. The purpose of the present work is to minimize the dosing frequency, taste masking toxicity and to improve the therapeutic efficacy by formulating mefloquine HCl nanoparticles. Mefloquine nanoparticles were formulated by emulsion diffusion method using polymer poly(ε-caprolactone) with six different formulations. Nanoparticles were characterized by determining its particle size, polydispersity index, drug entrapment efficiency, drug content, particle morphological character and drug release. The particle size ranged between 100 nm to 240 nm. Drug entrapment efficacy was >95%. The in-vitro release of nanoparticles were carried out which exhibited a sustained release of mefloquine HCl from nanoparticles up to 24 hrs. The results showed that nanoparticles can be a promising drug delivery system for sustained release of mefloquine HCl.

Preparation, Characterization and In-vitro release of Piroxicam-loaded Solid Lipid Nanoparticles

2010 ◽  
Vol 3 (3) ◽  
pp. 1136-1146
Author(s):  
V K Verma ◽  
Ram A
Keyword(s):  
Electron Microscopy ◽  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Diffusion Method ◽  
Solid Lipid ◽  
Vitro Release

 Solid lipid nanoparticles (SLNs) of piroxicam where produced by solvent emulsification diffusion method in a solvent saturated system. The SLNs where composed of tripamitin lipid, polyvinyl alcohol (PVAL) stabilizer, and solvent ethyl acetate. All the formulation were subjected to particle size analysis, zeta potential, drug entrapment efficiency, percent drug loading determination and in-vitro release studies. The SLNs formed were nano-size range with maximum entrapment efficiency. Formulation with 435nm in particle size and 85% drug entrapment was subjected to scanning electron microscopy (SEM) and transmission electron microscopy (TEM) for surface morphology, differential scanning calorimetry (DSC) for thermal analysis and short term stability studies. SEM and TEM confirm that the SLNs are nanometric size and circular in shape. The drug release behavior from SLNs suspension exhibited biphasic pattern with an initial burst and prolong release over 24 h. 

Ruta montana evokes antihypertensive activity through increase of prosta-glandins release in L-NAME-induced hypertensive rats

2020 ◽  
Vol 20 ◽  
Author(s):  
El-Ouady Fadwa ◽  
Mohamed Eddouks
Keyword(s):  
Blood Pressure ◽  
Heart Rate ◽  
Aqueous Extract ◽  
Antihypertensive Effect ◽  
Antihypertensive Activity ◽  
Computer Assisted ◽  
Hypertensive Rats ◽  
Vasorelaxant Effect ◽  
Vasorelaxant Activity ◽  
Ruta Montana

Aims: The aim of the study was to investigate experimentally the antihypertensive effect of Ruta Montana. Background: Ruta montana L. is traditionally used in Moroccan herbal medicine to treat hypertension. This study aimed to evaluate experimentally the hypotensive and vasoactive properties of this plant. Objective: The objective of the study was to evaluate the effect of the aqueous extract of Ruta Montana on blood pressure parameters in LNAME-induced hypertensive rats and to determine the vasorelaxant activity of this aqueous extract. Methods: The antihypertensive effect of the aqueous extract obtained from Ruta montana aerial parts (RMAPAE) (200 mg/kg) was evaluated in normal and anesthetized hypertensive rats. Blood pressure parameters (systolic blood pressure (SBP), mean blood pressure (MBP) and diastolic blood pressure (DBP)) and heart rate were measured using a tail-cuff and a computer-assisted monitoring device. The acute and chronic effect of RMAPAE was recorded during 6 hours for the acute experiment and during 7 days for the sub-chronic test. In the other set, the vasorelaxant effect of RMAPAE on the contractile response was undertaken in isolated thoracic aorta. Results: The results indicated that RMAPAE extract significantly decreased SBP, MBP, DBP and heart rate in L-NAMEinduced hypertensive rats. Furthermore, RMAPAE was demonstrated to induce a dose dependent relaxation in the aorta precontracted with Epinephrine or KCl. More interestingly, this vasorelaxant activity of RMAPAE seems to be probably mediated through the prostaglandins pathway. Conclusion: The present study illustrates the beneficial action of Ruta montana on hypertension and supports then its use as an antihypertensive agent.

The possible regulatory mechanisms of aqueous, ethyl acetate and nhexane fractions of the Ribes khorassanicum extract on acute hypertension in rats

2020 ◽  
Vol 20 ◽  
Author(s):  
Reza Mohebbati ◽  
Yasamin Kamkar-De ◽  
Mohammad Naser Shafei
Keyword(s):  
Ethyl Acetate ◽  
Antihypertensive Effect ◽  
Cardiovascular Responses ◽  
Regulatory Mechanisms ◽  
Hypertensive Rats ◽  
Control Groups ◽  
Acute Hypertension ◽  
The North ◽  
Significant Difference ◽  
And Control

Objective: Our previous studies showed the antihypertensive effect of Ribes khorassanicum (R. khorassanicum), a medicinal herb growing in the North Khorasan Province of Iran. For further evaluation, the present study investigated the effect of n-hexane (HX), ethyl acetate (EA), and aqueous (AQ) fractions of hydroalcoholic R. khorassanicum extract on cardiovascular responses in angiotensin II (AngII) and NG-nitro-L-arginine methyl ester (L-NAME) hypertensive rats. Methods: Wistar rats were randomly divided into 11 groups (n=5): 1) control, 2) AngII (50 ng/kg, i.v), 3) AngII + losartan (10 mg/kg, i.p), 4) L-NAME (10 mg/kg, i.v), 5) L-NAME+ sodium nitroprusside (SNP) (50 mg/kg, i.p), 6,7,8) one dose of each fraction of R. khorassanicum (AQ/EA/HX (50 mg/kg, i.p)) +AngII, and 9,10,11) one dose of each fraction of R. khorassanicum (AQ/EA/HX (50 mg/kg, i.p)) + L-NAME. Treated rats received three fractions 30 min before the injection of L-NAME and AngII in separate groups. The cardiovascular parameters were recorded by the Power Lab instrument via an angiocath inserted into the femoral artery. The peak changes (∆) of mean arterial pressure (MAP), systolic blood pressure (SBP), and heart rate (HR) in treated groups were compared with those of the hypertensive and control groups. Result: AngII and L-NAME significantly increased ∆MAP and ∆SBP and attenuated by pretreatment of LOS and SNP, respectively. Pretreatment with polar (AQ) and semipolar (EA) fractions of R. khorassanicum reduced the peak changes of MAP and SBP in both AngII and L-NAME-treated groups. Only the fraction of the herb attenuated the HR increased in the L-NAME group. The HR in other groups did not demonstrate any significant difference. Conclusion: All fractions of R. khorassanicum have an antihypertensive effect. However, the effect of polar fractions is more salient. It is also conceivable that the antihypertensive effect of fractions is mostly mediated by the inhibition of AngII.

scholarly journals Synthesis and self-assembly of curcumin-modified amphiphilic polymeric micelles with antibacterial activity

2021 ◽  
Vol 19 (1) ◽  
Author(s):  
Caio H. N. Barros ◽  
Dishon W. Hiebner ◽  
Stephanie Fulaz ◽  
Stefania Vitale ◽  
Laura Quinn ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Self Assembly ◽  
Glycolic Acid ◽  
Extracellular Polymeric Substances ◽  
Polymeric Micelles ◽  
Polymeric Nanoparticles ◽  
Enhanced Resistance ◽  
Antimicrobial Nanoparticles ◽  
Good Penetration ◽  
Antibiofilm Agents

Abstract Background The ubiquitous nature of bacterial biofilms combined with the enhanced resistance towards antimicrobials has led to the development of an increasing number of strategies for biofilm eradication. Such strategies must take into account the existence of extracellular polymeric substances, which obstruct the diffusion of antibiofilm agents and assists in the maintenance of a well-defended microbial community. Within this context, nanoparticles have been studied for their drug delivery efficacy and easily customised surface. Nevertheless, there usually is a requirement for nanocarriers to be used in association with an antimicrobial agent; the intrinsically antimicrobial nanoparticles are most often made of metals or metal oxides, which is not ideal from ecological and biomedical perspectives. Based on this, the use of polymeric micelles as nanocarriers is appealing as they can be easily prepared using biodegradable organic materials. Results In the present work, micelles comprised of poly(lactic-co-glycolic acid) and dextran are prepared and then functionalised with curcumin. The effect of the functionalisation in the micelle’s physical properties was elucidated, and the antibacterial and antibiofilm activities were assessed for the prepared polymeric nanoparticles against Pseudomonas spp. cells and biofilms. It was found that the nanoparticles have good penetration into the biofilms, which resulted in enhanced antibacterial activity of the conjugated micelles when compared to free curcumin. Furthermore, the curcumin-functionalised micelles were efficient at disrupting mature biofilms and demonstrated antibacterial activity towards biofilm-embedded cells. Conclusion Curcumin-functionalised poly(lactic-co-glycolic acid)-dextran micelles are novel nanostructures with an intrinsic antibacterial activity tested against two Pseudomonas spp. strains that have the potential to be further exploited to deliver a secondary bioactive molecule within its core. Graphic Abstract

Sign in / Sign up

Export Citation Format

Share Document