Development and evaluation of coenzyme Q10 loaded solid lipid nanoparticle hydrogel for enhanced dermal delivery

Abstract Coenzyme Q10 (Q10) loaded solid lipid nanoparticles (SLN) were prepared by the high speed homogenization method and incorporated into Carbopol 974P hydrogels. Compritol 888 ATO (C888) was employed as the lipid base; Poloxamer 188 (P188) and Tween 80 (Tw80) were used as surfactant and co-surfactant. Optimum particle size with narrow distribution was obtained as 152.2 nm for blank and 142.4 nm for Q10 loaded SLNs. The overall charge of loaded SLNs was -13.7 ± 1.3 mV. Q10 entrapment efficiency was 89 % and the production yield was 94 %. Transmission electron microscopy analysis provided evidence of colloidal size, spherical shape while differential scanning calorimetry analysis confirmed recrystallization of the lipid after the preparation of SLNs. Trolox equivalent antioxidant capacity (TEAC) analysis has shown that antioxidant potential of Q10 can be protected in SLNs. Rheological characteristics demonstrated that the SLN incorporating gels were shear thinning and the mechanical strength of the gels was suitable for topical application. Diffusion studies from rat abdominal skin revealed that the delivery of Q10 was doubled in SLN incorporating gels, approximately 40 μg cm-2, in comparison with gels prepared with only Q10 (not incorporated in SLNs). As a result, it can be stated that Q10-SLN loaded gels can be successful delivery systems for carrying Q10 efficiently into the skin without losing its antioxidant properties.

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

Nanotechnology Development ◽

10.4081/nd.2012.e8 ◽

2012 ◽

Vol 2 (1) ◽

pp. 8 ◽

Cited By ~ 5

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.

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Formulation and Evaluation of Solid Lipid Nanoparticles of Olanzapine for the Treatment of Psychosis

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v10i5-s.4440 ◽

2020 ◽

Vol 10 (5-s) ◽

pp. 25-31

Author(s):

Shubhangi C. Daswadkar ◽

Abhijit Vasant Atole

Keyword(s):

Particle Size ◽

Solid Lipid Nanoparticles ◽

High Speed ◽

Entrapment Efficiency ◽

Antipsychotic Agent ◽

Tween 80 ◽

Lipid Nanoparticles ◽

Particle Size Analysis ◽

Size Analysis ◽

Solid Lipid

Solid lipid nanoparticles (SLN) are typically spherical with an average diameter between 1 nm to 1000 nm in range. It is alternative carrier systems to tradition colloidal carriers, such as liposomes emulsions and polymeric micro and nanoparticles. Olanzapine (OZP) is an atypical antipsychotic agent which is used for treatment of Schizophrenia. Its oral bioavailability is around of 40%. OZP is a class II drug so it having low aqueous solubility. To overcome that problem and to increase its bioavailability, the solid lipid nanoparticles of olanzapine are prepared. Formulation batches designed by modifying type of surfactant ( Span 80, Tween 80), concentration of surfactant, Concentration of co-surfactant, type of lipid ( glyceryl monostearate, Stearic acid), Lipid concentration, speed of stirring and time of stirring using customised design of DOE. The SLN were prepared by high speed homogenization technique, and then characterized by particle size analysis, Drug entrapment efficiency and Drug diffusion study. A formulation containing GMS as a lipid stabilised with tween 80 as surfactant show good drug release, smaller particle size, as compared with other formulations with different lipid and surfactant. The present research findings indicate that OZP loaded solid lipid Nano particulate system for delivery of OZP with better efficacy with minimum adverse effects. Keywords: Olanzapine, SLN, GMS, high speed homogenization and DOE.

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Optimization of Solid Lipid Nanoparticles of Ezetimibe in Combination with Simvastatin Using Quality by Design (QbD)

Nanoscience &Nanotechnology-Asia ◽

10.2174/2210681209666190218143736 ◽

2020 ◽

Vol 10 (4) ◽

pp. 404-418

Author(s):

Kruti Borderwala ◽

Ganesh Swain ◽

Namrata Mange ◽

Jaimini Gandhi ◽

Manisha Lalan ◽

...

Keyword(s):

Particle Size ◽

Solid Lipid Nanoparticles ◽

High Speed ◽

Entrapment Efficiency ◽

Lipid Nanoparticles ◽

Water Soluble ◽

Lipid Matrix ◽

Solid Lipid ◽

32 Factorial Design ◽

Full Factorial Experimental Design

Background: The objective of this study was to develop solid lipid nanoparticles (SLNs) of poorly water soluble anti-hyperlipidemic drugs-Ezetimibe in combination with Simvastatin. Methods: This study describes a 32 full factorial experimental design to optimize the formulation of drug loaded lipid nanoparticles (SLN) by the high speed homogenization technique. The independent variables amount of lipid (GMS) and amount of surfactant (Poloxamer 188) were studied at three levels and arranged in a 32 factorial design to study the influence on the response variables- particle size, % entrapment efficiency (%EE) and cumulative drug release (% CDR) at 24 h. Results: The particle size, % EE and % CDR at 24 h for the 9 batches (B1 to B9) showed a wide variation of 104.6-496.6 nm, 47.80-82.05% (Simvastatin); 48.60-84.23% (Ezetimibe) and 54.64-92.27% (Simvastatin); 43.8-97.1% (Ezetimibe), respectively. The responses of the design were analysed using Design Expert 10.0.2. (Stat-Ease, Inc, USA), and the analytical tools of software were used to draw response surface plots. From the statistical analysis of data, polynomial equations were generated. Optimized formulation showed particle size of 169.5 nm, % EE of 75.43% (Simvastatin); 79.10% (Ezetimibe) and 74.13% (Simvastatin); 77.11% (Ezetimibe) %CDR after 24 h. Thermal analysis of prepared solid lipid nanoparticles gave indication of solubilisation of drugs within lipid matrix. Conclusion: Fourier Transformation Infrared Spectroscopy (FTIR) showed the absence of new bands for loaded solid lipid nanoparticles indicating no interaction between drugs and lipid matrix and being only dissolved in it. Electron microscope of transmission techniques indicated sphere form of prepared solid lipid nanoparticles with smooth surface with size approximately around 100 nm.

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Mannosylated Solid Lipid Nanocarriers Of Chrysin To Target Gastric Cancer: Optimization and Cell line Study.

Current Drug Delivery ◽

10.2174/1567201818666210319142206 ◽

2021 ◽

Vol 18 ◽

Author(s):

Sonia S. Pandey ◽

Farhinbanu I. Shaikh ◽

Arti R. Gupta ◽

Rutvi J. Vaidya

Keyword(s):

Gastric Cancer ◽

Particle Size ◽

Ex Vivo ◽

Biological Effects ◽

Entrapment Efficiency ◽

X Ray Diffraction ◽

Scanning Calorimetry ◽

Solid Lipid ◽

Lipid Nanocarriers

Background: Despite significant biological effects, the clinical use of chrysin has been restricted because of its poor oral bioavailability. Objective: The purpose of the present research was to investigate the targeting potential of Mannose decorated chrysin (5,7- dihydroxyflavone) loaded solid lipid nanocarrier (MC-SLNs) for gastric cancer. Methods: The Chrysin loaded SLNs (C-SLNs) were developed optimized, characterized and further mannosylated. The C-SLNs were developed with high shear homogenizer, optimized with 32 full factorial designs and characterized by Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD) and Scanning Electron Microscope (SEM) and evaluated for particle size/polydispersity index, zeta-potential, entrapment efficiency, % release and haemolytic toxicity. The ex-vivo cytotoxicity study was performed on gastric cancer (ACG) and normal cell lines. Results: DSC and XRD data predict the chrysin encapsulation in lipid core and FTIR results confirm the mannosylation of C-SLNs. The optimized C-SLNs exhibited a narrow size distribution with a particle size of 285.65 nm. The % Entrapment Efficiency (%EE) and % controlled release were found to be 74.43% and 64.83%. Once C-SLNs were coated with mannose, profound change was observed in dependent variable - increase in the particle size of MC-SLNs (307.1 nm) was observed with 62.87% release and 70.8% entrapment efficiency. Further, the in vitro studies depicted MC- SLNs to be least hemolytic than pure chrysin and C-SLNs. MC-SLNs were most cytotoxic and were preferably taken up ACG tumor cells as evaluated against C-SLNs. Conclusion: These data suggested that the MC-SLNs demonstrated better biocompatibility and targeting efficiency to treat the gastric cancer.

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Effect of The Surfactant and Liquid Lipid Type in The Physico-chemical Characteristics of Beeswax-based Nanostructured Lipid Carrier (NLC) of Metformin

Pharmaceutical Nanotechnology ◽

10.2174/2211738509666210222143716 ◽

2021 ◽

Vol 09 ◽

Author(s):

Mona Qushawy

Keyword(s):

Drug Release ◽

Factorial Design ◽

Biological Membrane ◽

Entrapment Efficiency ◽

Tween 80 ◽

Full Factorial Design ◽

Nanostructured Lipid Carrier ◽

Class Iii ◽

Scanning Calorimetry ◽

Full Factorial

Background: Metformin (MF) is an antidiabetic drug that belongs to class III of the biopharmaceutical classification system (BCS) which is characterized by high solubility and low permeability. Objective: The study aimed to prepare metformin as nanostructured lipid carriers (MF-NLCs) to control the drug release and enhance its permeability through the biological membrane. Method: 22 full factorial design was used to make the design of MF-NLCs formulations. MF-NLCs were prepared by hot-melt homogenization-ultra sonication technique using beeswax as solid lipid in presence of liquid lipid (either capryol 90 or oleic acid) and surfactant (either poloxamer 188 or tween 80). Results: The entrapment efficiency (EE%) of MF-NLCs was ranged from 85.2±2.5 to 96.5±1.8%. The particle size was in the nanoscale (134.6±4.1 to 264.1±4.6 nm). The value of zeta potential has a negative value ranged from -25.6±1.1 to -39.4±0.9 mV. The PDI value was in the range of (0.253±0.01 to 0.496±0.02). The cumulative drug release was calculated for MF-NLCs and it was found that Q12h ranged from 90.5±1.7 % for MF-NLC1 to 99.3±2.8 for MF-NLC4. Infra-red (IR) spectroscopy and differential scanning calorimetry (DSC) studies revealed the compatibility of the drug with other ingredients. MF-NLC4 was found to the optimized formulation with the best responses. Conclusion: 22 full factorial design succeed to obtain an optimized formulation which controls the drug release and increases the drug penetration.

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Implementation of experimental design methodology in preparation and characterization of zolmitriptan loaded chitosan nanoparticles

International Current Pharmaceutical Journal ◽

10.3329/icpj.v6i3.32684 ◽

2017 ◽

Vol 6 (3) ◽

pp. 16-22 ◽

Cited By ~ 2

Author(s):

Satish K. Mandlik ◽

Nisharani S. Ranpise

Keyword(s):

Statistical Analysis ◽

Factorial Design ◽

High Speed ◽

Chitosan Nanoparticles ◽

Spherical Shape ◽

Entrapment Efficiency ◽

Pharmaceutical Journal ◽

Optimization Method ◽

Fickian Diffusion ◽

Contour Plots

The present study investigated the implementation of 32 factorial design of experiment and statistical analysis for the optimization of chitosan nanoparticles containing zolmitriptan an antimigraine drug. The influence of chitosan concentration (X1) and sodium tripoly phosphate (X2) on responses namely nanoparticle size (Y1), and entrapment efficiency (Y2), was studied. As per design, nine runs of nanoparticles were prepared by modified ionic gelation method using high speed vortex mixing. The particle size was found in the range of 151-880 nm and entrapment efficiency was 72.3-81.2%. A statistical analysis was performed using licensed design expert software V.8.0 with respect to ANOVA, regression analysis. The contour plots and response surface plots showed visual representation of relationship between the experimental responses and the set of independent variables. Regression model equations were validated by a numerical and graphical optimization method. Further, optimized drug loaded nanoparticles showed +23.7mV zeta potential indicating storage stability, electron micrograph reflects spherical shape and mixed type of drug release followed by Fickian diffusion (n=0.266) was observed. Thus, using systematic factorial design approach, desirable goals can be achieved in shortest possible time with lesser number of experiments which was proven to be an effective tool in quality by design.Mandlik and Ranpise, International Current Pharmaceutical Journal, February 2017, 6(3): 16-22http://www.icpjonline.com/documents/Vol6Issue3/01.pdf

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PREPARATION, CHARACTERIZATION, AND FORMULATION OF SOLID LIPID NANOPARTICLES LOTION FROM MULBERRY ROOTS (MORUS ALBA L.)

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2020.v12s1.ff041 ◽

2020 ◽

pp. 182-186

Author(s):

MUHAMAD WILDAN NUGRAHA ◽

RADITYA ISWANDANA ◽

MAHDI JUFRI

Keyword(s):

Particle Size ◽

Zeta Potential ◽

Solid Lipid Nanoparticles ◽

High Speed ◽

Tween 80 ◽

Lipid Nanoparticles ◽

Morus Alba ◽

Glyceryl Monostearate ◽

Optimum Result ◽

Solid Lipid

Objective: Tween 80 has been used as a solvent for the extraction of phenolic compounds because this surfactant has both hydrophilic and hydrophobicproperties. Solid lipid nanoparticles (SLNs) have been developed to improve penetration through the skin layer. We investigated the efficacy of usingthe microwave-assisted micellar extraction (MAME) approach for extracting oxyresveratrol from Morus alba roots and also to develop an SLN lotion.Methods: The M. alba roots were extracted with Tween 80 in a microwave for 18 min, and the extract was used to develop SLN with differentconcentrations of glyceryl monostearate. The SLNs from M. alba root extracts were prepared by a high-speed homogenization technique (25,000 rpmfor 15 min). The SLNs produced were characterized as per particle size, polydispersity index (PDI), and zeta potential. The SLNs with the bestcharacteristics were used to formulate a lotion using a high-pressure homogenizer.Results: Extraction using MAME showed improved extraction efficiency. The oxyresveratrol concentration from the extract was 2.77%. The SLN with2.5% glyceryl monostearate showed the optimum result, with a particle size of 130.20 nm, a PDI of 0.278, and a zeta potential of −21.8 mV. The SLNlotion exhibited a particle size of 285.9 nm and a PDI of 0.360. The SLN lotion also had good penetration, with a flux of 4.70 μg cm−2/h.Conclusion: MAME is an efficient method for extracting oxyresveratrol from M. alba roots. The SLN with 2.5% glyceryl monostearate exhibited theoptimum characteristics, and the SLN lotion showed good characteristics, including skin penetration.

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A COMPARATIVE ASSESSMENT OF VESICULAR FORMULATIONS: TRANSFERSOMES AND CONVENTIONAL LIPOSOMES LOADED IVABRADINE HYDROCHLORIDE

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2020v12i6.39391 ◽

2020 ◽

pp. 51-55

Author(s):

GITA CHAURASIA ◽

NARENDRA LARIYA

Keyword(s):

Drug Release ◽

Physical Stability ◽

Physical Appearance ◽

Spherical Shape ◽

Entrapment Efficiency ◽

Tween 80 ◽

Molar Ratio ◽

Drug Release Study ◽

Release Study

Objective: Ivabradine hydrochloride (IH), a benzazepine derivative used to treat cardiovascular disease angina pectoris. In this study IH-loaded novel carrier systems transfersomes (TFs) and conventional liposomes (CLs) were developed and compared for their efficacy to enhance the stability of drugs from degradation. Methods: TFs formulations (TF-1, TF-2 and TF-3) were prepared by using different biocompatible surfactants; tween-80 (TW), span-80(S) and sodium deoxycholate (SC) in the concentration ratio of 15 parts with 85 parts of soy phosphatidylcholine as phospholipid by thin-film hydration method. These vesicles were compared with CLs formulation (L-1) prepared in 7:3 molar ratio of soy phosphatidylcholine: cholesterol by following the same method. These vesicles were compared for physical appearance, vesicle shape, and size, percentage drug entrapment efficiency (%DEE), deformability index (DI), in vitro percentage cumulative drug release study, and physical stability studies. The chosen optimized novel carriers were observed under scanning electron microscopy. Results: The compared data demonstrated that the physical appearance for all vesicles was turbid and had a spherical shape. The size distribution was in the range of 129.0 nm to 273.5 nm in vesicles. The %DEE (79.0±0.94) and DI (35.0±1.9) was found maximum in TF-1 formulation that was 2.3 times higher than L-1 formulation. The in vitro percentage cumulative drug release study followed second-order polynomial kinetics that was 2.0 times higher than L-1and 2.9 times higher than the plain drug in 30 min (90.4±0.06%) from TF-1. The vesicles were found to be stable at refrigeration conditions. Conclusion: Thus, amongst of all vesicles TW loaded TFs (TF-1) was chosen as an excellent novel vesicular carrier for hydrophilic drugs due to its higher deformability behavior than CLs that protects the certain drugs from biodegradation and provides stability.

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Preparation and Characterisation of Nobiletin-Loaded Nanostructured Lipid Carriers

Journal of Nanomaterials ◽

10.1155/2017/2898342 ◽

2017 ◽

Vol 2017 ◽

pp. 1-10 ◽

Cited By ~ 6

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.

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Preparation and Characterization of Solid Lipid Nanoparticles Loaded with Cisplatin

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v8i6.2033 ◽

2018 ◽

Vol 8 (6) ◽

pp. 125-131

Author(s):

Indrayani D. Raut ◽

Rajendra C. Doijad ◽

Shrinivas K. Mohite ◽

Arehalli S. Manjappa

Keyword(s):

Particle Size ◽

Zeta Potential ◽

Solid Lipid Nanoparticles ◽

Drug Loading ◽

Acquired Resistance ◽

Spherical Shape ◽

Entrapment Efficiency ◽

Lipid Nanoparticles ◽

Platinum Drug ◽

Solid Lipid

Cisplatin (Cis diaminedichloro platinum) was the first platinum drug to be used as an anticancer drug, and it is widely used in the treatment of testicular, head, neck, ovarian and lung cancer. The use of Cisplatin is limited due to its intrinsic and acquired resistance and severe side effects such as chronic neurotoxicity and nephrotoxicity. The colloidal carriers such as emulsion, liposomes, polymeric nanoparticles have been extensively studied to overcome above limitations. The solid lipid nanoparticles (SLNs), amongst other colloidal carriers, were found to be an ideal carrier for lipophillic drug for better stability and release retardation. Cisplatin loaded solid lipid nanoparticles was prepared by microemulsion technique. Stearic acid was used as lipid. The other excipients were used as DPPG, Soya lecithin and Poloxamer P407 and acidic buffer PH4. Also used Probe sonication for 10 min at 79 Amplitude. Cisplatin SLNs Batch C13 showed particle size of 119.23±1.52 nm, Zeta potential of -37.33±2.47 mV, % Entrapment efficiency of 90.2 ± 2.1 %., % Drug loading capacity of 1.62 ± 1.34 %., The TEM study of optimized Cisplatin SLN illustrated the spherical shape of nanoparticles. Total release amount of Cisplatin was 82.62± 2.04 % after 48 hrs. The formulation performed kinetics study followed Peppas plot equation The SLNs of Cisplatin met all the requirements of a colloidal drug delivery system. They had particle size in nanosize; their size distribution was narrow and all the particles were in spherical shape and stable. Keywords: Cisplatin, Solid Lipid nanoparticles, zeta potential, Particle size, Transmission electron Microscopy.

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