scholarly journals Comprehensive Study of Atorvastatin Nanostructured Lipid Carriers through Multivariate Conceptualization and Optimization

Pharmaceutics ◽  
2021 ◽  
Vol 13 (2) ◽  
pp. 178
Author(s):  
Heba A. Ghanem ◽  
Ali M. Nasr ◽  
Tamer H. Hassan ◽  
Mahmoud M. Elkhoudary ◽  
Reem Alshaman ◽  
...  
Keyword(s):  
Chemical Interaction ◽  
Amorphous State ◽  
Entrapment Efficiency ◽  
Serum Levels ◽  
Nanostructured Lipid Carriers ◽  
Polydispersity Index ◽  
Scanning Calorimetry ◽  
Lipid Mixture ◽  
Factors Affecting ◽  
Screening Design

The aim of the current study is to establish a comprehensive experimental design for the screening and optimization of Atorvastatin-loaded nanostructured lipid carriers (AT-NLCs). Initially, combined D-optimal screening design was applied to find the most significant factors affecting AT-NLCs properties. The studied variables included mixtures of solid and liquid lipids, the solid/liquid lipid ratio, surfactant type and concentration, homogenization speed as well as sonication time. Then, the variables homogenization speed (A), the ratio of solid lipid/liquid lipid (B), and concentration of the surfactant (C) were optimized using a central composite design. Particle size, polydispersity index, zeta potential, and entrapment efficiency were chosen as dependent responses. The optimized AT-NLCs demonstrated a nanometric size (83.80 ± 1.13 nm), Polydispersity Index (0.38 ± 0.02), surface charge (−29.65 ± 0.65 mV), and high drug incorporation (93.1 ± 0.04%). Fourier Transform Infrared Spectroscopy (FTIR) analysis showed no chemical interaction between Atorvastatin and the lipid mixture. Differential Scanning Calorimetry (DSC) analysis of the AT-NLCs suggested the transformation of Atorvastatin crystal into an amorphous state. Administration of the optimized AT-NLCs led to a significant reduction (p < 0.001) in serum levels of rats’ total cholesterol, triglycerides, and low-density lipoproteins. This change was histologically validated by reducing the relevant steatosis of the liver.

scholarly journals Preparation and Characterisation of Nobiletin-Loaded Nanostructured Lipid Carriers

2017 ◽  
Vol 2017 ◽  
pp. 1-10 ◽  
Author(s):  
Wei Huang ◽  
Huating Dou ◽  
Houjiu Wu ◽  
Zhigao Sun ◽  
Hua Wang ◽  
...  
Keyword(s):  
Zeta Potential ◽  
Chemical Interaction ◽  
Amorphous State ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Nanostructured Lipid Carriers ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Lipid Mixture ◽  
Food Response

The objective of this manuscript was to investigate and optimise the potential of nanostructured lipid carriers (NLCs) as a carrier system for nobiletin (NOB), which was prepared by high-pressure homogenisation method. Additionally, this study was focused on the application of NOB-loaded NLC (NOB-NLC) in functional food. Response surface method with a three-level Box–Behnken design was validated through analysis of variance, and the robustness of the design was confirmed through the correspondence between the values measured in the experiments and the predicted ones. Properties of the prepared NOB-NLC, such as Z-average, polydispersity, entrapment efficiency, zeta potential, morphology, and crystallinity, were investigated. NOB-NLC exhibited a spherical shape with a diameter of 112.27 ± 5.33 nm, zeta potential of −35.1 ± 2.94 mV, a polydispersity index of 0.251 ± 0.058, and an EE of 81.06%  ±  6.02%. Results from X-ray diffraction and differential scanning calorimetry of NOB-NLC reviewed that the NOB crystal might be converted to an amorphous state. Fourier transform infrared spectroscopic analysis demonstrated that chemical interaction was absent between the compound and lipid mixture in NOB-NLC.

scholarly journals OPTIMIZATION AND CHARACTERIZATION OF RIVASTIGMINE-LOADED NANOSTRUCTURED LIPID CARRIERS

2021 ◽  
pp. 46-51
Author(s):  
SWATHI GANNA ◽  
SAI MANOGNA KOTAKADI ◽  
RESHMA ANJUM MOHAMMED ◽  
MANNUR ISMAIL SHAIK ◽  
JOHN SUSHMA NANNEPAGA
Keyword(s):  
Particle Size ◽  
Chemical Interaction ◽  
Surfactant Solution ◽  
Entrapment Efficiency ◽  
Nanostructured Lipid Carriers ◽  
Sustained Delivery ◽  
Scanning Calorimetry ◽  
Atomic Force ◽  
Dsc Analyses

Objective: The objective of the present study was to develop Nanostructured lipid carriers (NLCs) for improvement in the oral bioavailability of RT. Methods: RT-loaded NLCs were prepared by high shear homogenization technique using fish oil and flaxseed oil respectively. The prepared RT-NLCs were characterized using a phase-contrast microscope, scanning electron microscope (SEM), atomic force microscope (AFM), Fourier transform-infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). Further, particle size, entrapment efficiency and sustained release of the drug were also studied. Results: SEM results revealed that the RT-NLCs were spherical in shape with a smooth surface. AFM results confirmed the formation of spherical particle dispersions by the NLCs in nanoscale. FTIR spectroscopy and DSC analyses revealed that there is no chemical interaction between the ingredients of RT-NLCs. The particle size of the RT-NLCs was found to be exponentially decreased with the increase in a surfactant solution. Conclusion: The results confirmed pronounced improvement in entrapment efficiency of optimized formulation of RT-NLCs. In vitro, drug release studies showed that RT-NLCs were capable of releasing the drug in a sustained manner. The experimental results showed that the NLCs are potential carriers for providing sustained delivery of rivastigmine.

scholarly journals Application of Plackett-Burman design for screening of factors affecting pitavastatin nanoparticle formulation development

Folia Medica ◽  
2021 ◽  
Vol 63 (5) ◽  
pp. 775-785
Author(s):  
Vinodkumar D. Ramani ◽  
Girish K. Jani ◽  
Girish U. Sailor
Keyword(s):  
Particle Size ◽  
Influential Factors ◽  
Polydispersity Index ◽  
Formulation Development ◽  
Relative Significance ◽  
Factors Affecting ◽  
Screening Design ◽  
Burman Design ◽  
Nanoparticle Formulation ◽  
Plackett Burman Design

Introduction: Nanoparticle formulation of pitavastatin calcium is a potential alternative to solve the solubility related problem. However, the formulation of nanoparticle involves various parameters that affect product quality. Plackett-Burman design could facilitate an economical experimental plan that focuses on determining the relative significance of many. Aim: The objective of this study was to screen the variables which could significantly affect the pitavastatin nanoparticle formulation. Materials and methods: The pitavastatin nanoparticles were formulated by preparing nanosuspension using the emulsion solvent evaporation technique followed by freeze-drying. A Plackett-Burman screening design methodology was employed in which seven factors at two levels were tested at 12 runs to study the effect of formulation and process variables on particle size and polydispersity index of nanoparticles. The surface morphology and crystalline nature of nanoparticle were also evaluated. Results: The particle size and polydispersity index of nanosuspension was found in the range of 113.1 to 768.5 nm and 0.068 to 0.508, respectively. Statistical analysis of various variables revealed that stabilizer concentration, injection flow rate, and stirring rate were the most influential factors affecting the particle size and polydispersity index of the formulation. X-ray diffraction (XRD) and scanning electron microscopy (SEM) study suggested the amorphous nature of nanoparticles. Conclusions: This study concluded that the Plackett-Burman design was an efficient tool for screening the process and formulation variables affecting the properties of pitavastatin nanoparticles and also for the identification of the most prominent factor.

Design, Optimization and Characterization of Nanostructured Lipid Carriers of Raloxifene Hydrochloride for Transdermal Delivery

2020 ◽  
Vol 10 (1) ◽  
pp. 57-67 ◽  
Author(s):  
Durga Puro ◽  
Rajani Athawale ◽  
Anjali Pandya
Keyword(s):  
Particle Size ◽  
Transdermal Delivery ◽  
Tween 80 ◽  
Nanostructured Lipid Carriers ◽  
Polydispersity Index ◽  
Tape Stripping ◽  
Cremophor El ◽  
Scanning Calorimetry ◽  
Raloxifene Hydrochloride

Introduction: Raloxifene Hydrochloride (RXL), a BCS class II drug, is used for the treatment of invasive breast cancer and osteoporosis in post menopausal women. Even though the drug is highly efficient, it shows poor bioavailability of 2% when administered orally. The aim of the study was to develop, statistically optimize, and characterize Raloxifene Hydrochloride loaded Nanostructured Lipid Carriers (NLC) for transdermal delivery to overcome the bioavailability issue. Methods: The RXL-NLC’s were developed using glyceryl behenate (Compritol® 888 ATO), glyceryl monostearate (GMS), and capric triglyceride (Miglyol® 810) as solid and liquid lipids, and Polysorbate 80 (Tween 80) and cremophor EL were used as surfactants and co-surfactant. A response surface methodology was applied for the optimization of NLC, using Box-Behnken experimental design. Amount of the drug, tween 80 and polyethoxylated castor oil (cremophor EL), each at three levels, were selected as independent variables, while particle size and polydispersity index were identified as dependent variables. The optimized batch was characterized for Particle size (79.8 nm±3), Polydispersity index (0.229±0.05), Zeta potential (-12.3±5) and Entrapment efficiency (79.14%±5). Surface morphology of the NLC’s were studied using Transmission Electron microscopy (TEM) and the shift in the endotherm of Differential scanning calorimetry confirmed the entrapment of the drug within NLC. In vitro drug release studies were performed using dialysis bag (12000-14000 Da) method. The optimized NLC dispersion was then incorporated into gel and characterized for gel uniformity, spreadability, pH, viscosity and drug content. Results: In vivo skin penetration study was carried out by tape stripping method, which showed increase in penetration when incorporated into nanogel as compared to plain drug gel. Conclusion: Based on the above result it can be concluded that transdermal delivery of NLC’s can be a superior alternative for orally low bioavailable drugs such as RXL which undergoes rapid first pass metabolism.

scholarly journals DESIGN, OPTIMIZATION AND IN VITRO EVALUATION OF ANTIFUNGAL ACTIVITY OF NANOSTRUCTURED LIPID CARRIERS OF TOLNAFTATE

2019 ◽  
pp. 109-115
Author(s):  
AHMED GARDOUH ◽  
Samar H. Faheim ◽  
Samar M. Solyman
Keyword(s):  
Zeta Potential ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Homogenization Method ◽  
Nanostructured Lipid Carriers ◽  
Scanning Calorimetry ◽  
Release Study ◽  
Vitro Release

Objective: The main purpose of this work was to prepare tolnaftate (TOL) loaded nanostructured lipid carriers (NLCs), Evaluate its characteristics and in vitro release study. Methods: Tolnaftate loaded Nanostructured lipid carriers were prepared by the high shear homogenization method using different liquid lipids types (DERMAROL DCO® and DERMAROL CCT®) and concentrations, different concentration ratios of tween80® to span20® and different homogenization speeds. All the formulated nanoparticles were subjected to particle size (PS), zeta potential (ZP), polydispersity index (PI), drug entrapment efficiency (EE), Differential Scanning Calorimetry (DSC), Transmission Electron microscopy (TEM), release kinetics and in vitro release study was determined. Results: The results revealed that NLC dispersions had spherical shapes with an average size between 154.966±1.85 nm and 1078.4±103.02 nm. High entrapment efficiency was obtained with negatively charged zeta potential with PDI value ranging from 0.291±0.02 to 0.985±0.02. The release profiles of all formulations were characterized by a sustained release behavior over 24 h and the release rates increased as the amount of surfactant decreased. The release rate of TOL is expressed following the theoretical model by Higuchi. Conclusion: From this study, It can be concluded that NLCs are a good carrier for tolnaftate delivery

Novel Self-Assembled Polycaprolactone–Lipid Hybrid Nanoparticles Enhance the Antibacterial Activity of Ciprofloxacin

2020 ◽  
Vol 25 (6) ◽  
pp. 598-607
Author(s):  
Mustafa E. Omer ◽  
Majed Halwani ◽  
Rayan M. Alenazi ◽  
Omar Alharbi ◽  
Shokran Aljihani ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Drug Loading ◽  
In Vitro Release ◽  
Amorphous State ◽  
Entrapment Efficiency ◽  
Release Profile ◽  
Hybrid Nanoparticles ◽  
Diffusion Method ◽  
Prolonged Release ◽  
Scanning Calorimetry

Ciprofloxacin (CIP), a widely used antibiotic, is a poor biopharmaceutical resulting in low bioavailability. We optimized a CIP polymer–lipid hybrid nanoparticle (CIP-PLN) delivery system to enhance its biopharmaceutical attributes and the overall therapeutic performance. CIP-PLN formulations were prepared by a direct emulsification–solvent–evaporation method. Varying the type and ratio of lipid was tried to optimize a CIP-PLN formulation. All the prepared formulations were evaluated for their particle size, polydispersity index, zeta potential, physical stability, and drug entrapment efficiency. The drug in vitro release profile was also studied. Antibacterial activities were tested by the agar diffusion method for all CIP-PLN formulations against an Escherichia coli clinical bacterial isolate (EC04). CIP-PLN formulations showed average sizes in the range of 133.9 ± 1.7 nm to 217.1 ± 0.8 nm, exhibiting high size uniformity as indicated by polydispersity indices lower than 0.25. The entrapment efficiency was close to 80% for all formulations. The differential scanning calorimetry (DSC) thermograms indicated the existence of CIP in the amorphous state in all PLN formulations. Fourier transform infrared spectra indicated deep incorporation of molecular CIP within the polymer matrix. The release profile of CIP from PLN formulas showed a uniform prolonged drug profile, extended for a week from most formulations with a zero-order kinetics. The antibacterial activity of CIP-PLN formulations showed significantly higher antibacterial activity only with F4 containing lecithin as the lipid component. In conclusion, we successfully optimized a CIP-PLN formulation with a low nanoparticle size in a close range, high percentage of entrapment efficiency and drug loading, uniform prolonged release rate, and higher antibacterial activity against the EC04 clinical isolate.

scholarly journals Ezetimibe-Loaded Nanostructured Lipid Carrier Based Formulation Ameliorates Hyperlipidaemia in an Experimental Model of High Fat Diet

Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1485
Author(s):  
Yogeeta O. Agrawal ◽  
Umesh B. Mahajan ◽  
Vinit V. Agnihotri ◽  
Mayur S. Nilange ◽  
Hitendra S. Mahajan ◽  
...  
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
High Fat Diet ◽  
Entrapment Efficiency ◽  
Polydispersity Index ◽  
Nanostructured Lipid Carrier ◽  
High Fat ◽  
Scanning Calorimetry ◽  
Bioavailability Enhancement

Ezetimibe (EZE) possesses low aqueous solubility and poor bioavailability and in addition, its extensive hepatic metabolism supports the notion of developing a novel carrier system for EZE. Ezetimibe was encapsulated into nanostructured lipid carriers (EZE-NLCs) via a high pressure homogenization technique (HPH). A three factor, two level (23) full factorial design was employed to study the effect of amount of poloxamer 188 (X1), pressure of HPH (X2) and number of HPH cycle (X3) on dependent variables. Particle size, polydispersity index (PDI), % entrapment efficiency (%EE), zeta potential, drug content and in-vitro drug release were evaluated. The optimized formulation displays pragmatic inferences associated with particle size of 134.5 nm; polydispersity index (PDI) of 0.244 ± 0.03; zeta potential of −28.1 ± 0.3 mV; % EE of 91.32 ± 1.8% and % CDR at 24-h of 97.11%. No interaction was observed after X-ray diffraction (XRD) and differential scanning calorimetry (DSC) studies. EZE-NLCs (6 mg/kg/day p.o.) were evaluated in the high fat diet fed rats induced hyperlipidemia in comparison with EZE (10 mg/kg/day p.o.). Triglyceride, HDL-c, LDL-c and cholesterol were significantly normalized and histopathological evaluation showed normal structure and architecture of the hepatocytes. The results demonstrated the superiority of EZE-NLCs in regard to bioavailability enhancement, dose reduction and dose-dependent side effects.

scholarly journals Screening of Most Effective Variables for Development of Gastroretentive Mucoadhesive Nanoparticles by Taguchi Design

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Ankit Anand Kharia ◽  
Akhlesh Kumar Singhai
Keyword(s):  
Entrapment Efficiency ◽  
Factors Affecting ◽  
Screening Design ◽  
Pareto Ranking ◽  
Loading Efficiency ◽  
Stirring Time ◽  
Addition Rate ◽  
One Step ◽  
Influential Variable ◽  
Time Required

The objective of this study was the selection of the most influential variable for the preparation of gastroretentive mucoadhesive nanoparticles of acyclovir. Nanoparticles were prepared by one-step desolvation method; effect of formulation and processing variables on various response variables were studied by a Taguchi standard orthogonal array L8 design. Independent variables studied were the amount of gelatin, amount of glutaraldehyde, amount of Pluronic F-68, acetone addition rate, pH, stirring time, and stirring speed. The dependent variables studied were the particle size, polydispersity index, amount of drug released in 6 h, time required to release 60% of drug, entrapment efficiency, loading efficiency, and mucoadhesiveness. The size of all nanoparticulate formulations prepared as per the experimental design (Taguchi screening design) varied between 165 and 1610 nm, PDI between 0.360 and 1.00, bioadhesiveness between 3.959 and 11.02 g, cumulative percent drug release in 24 h between 40.74 and 72.48, entrapment efficiency between 15.70 and 83.12, and loading efficiency between 39.72 and 80.49. Pareto ranking analyses showed that the two most important factors affecting the selected responses were amount of gelatin and amount of Pluronic F-68 (P<0.05).

scholarly journals Oral Bioavailability Enhancement of Raloxifene with Nanostructured Lipid Carriers

Nanomaterials ◽  
2020 ◽  
Vol 10 (6) ◽  
pp. 1085 ◽  
Author(s):  
Aditya Murthy ◽  
Punna Rao Ravi ◽  
Himanshu Kathuria ◽  
Shrinivas Malekar
Keyword(s):  
Oral Bioavailability ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Nanostructured Lipid Carriers ◽  
Scanning Calorimetry ◽  
Bioavailability Enhancement ◽  
Female Wistar Rats ◽  
Raloxifene Hydrochloride ◽  
Gut Metabolism

Raloxifene hydrochloride (RLX) shows poor bioavailability (<2%), high inter-patient variability and extensive gut metabolism (>90%). The objective of this study was to develop nanostructured lipid carriers (NLCs) for RLX to enhance its bioavailability. The NLC formulations were produced with glyceryl tribehenate and oleic acid. The particle characteristics, entrapment efficiency (EE), differential scanning calorimetry (DSC), in vitro drug release, oral bioavailability (in rats) and stability studies were performed. The optimized nanoparticles were 120 ± 3 nm in size with positive zeta potential (14.4 ± 0.5 mV); % EE was over 90% with the drug loading of 5%. The RLX exists in an amorphous form in the lipid matrix. The optimized RLX-NLC formulation showed sustained release in vitro. The RLX-NLC significantly (p < 0.05) enhanced oral bioavailability 3.19-fold as compared to RLX-free suspension in female Wistar rats. The RLX-NLC can potentially enhance the oral bioavailability of RLX. It can also improve the storage stability.

Does HbA1cc Play a Role in the Development of Cardiovascular Diseases?

2018 ◽  
Vol 24 (24) ◽  
pp. 2876-2882 ◽  
Author(s):  
Kailash Prasad
Keyword(s):  
Risk Factors ◽  
Cardiovascular Diseases ◽  
Cardiovascular System ◽  
Half Life ◽  
Serum Levels ◽  
Serum Glucose ◽  
Cvd Risk ◽  
Factors Affecting ◽  
Diagnosis And Management ◽  
Coronary Artery Atherosclerosis

Cardiovascular diseases (CVD) may be mediated through increases in the cardiovascular risk factors. Hemoglobin A1c (HbA1c) also called glycated hemoglobin is presently used for the diagnosis and management of diabetes. It has adverse effects on cardiovascular system. This review deals with its synthesis and effects on the cardiovascular system. The serum levels of HbA1c have been reported to be affected by various factors including, the lifespan of erythrocytes, factors affecting erythropoiesis, agents interfering glycation of Hb, destruction of erythrocytes, drugs that shift the formation of Hb, statins, and drugs interfering the HbA1c assay. Levels of HbA1c are positively correlated with serum glucose and advanced glycation end products ( AGE), but no correlation between AGE and serum glucose. AGE cannot replace HbA1c for the diagnosis and management of diabetes because there is no correlation of AGE with serum glucose, and because the half-life of protein with which glucose combines is only 14-20 days as compared to erythrocytes which have a half-life of 90-120 days. HbA1c is positively associated with CVD such as the carotid and coronary artery atherosclerosis, ischemic heart disease, ischemic stroke and hypertension.HbA1c induces dyslipidemia, hyperhomocysteinemia, and hypertension, and increases C-reactive protein, oxidative stress and blood viscosity that would contribute to the development of cardiovascular diseases. In conclusion, HbA1c serves as a useful marker for the diagnosis and management of diabetes. AGE cannot replace HbA1c in the diagnosis and management of diabetes. There is an association of HbA1c with CVD which be mediated through modulation of CVD risk factors.

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