Investigating the Effect of Particle Size on Cellular Uptake by Aggregation-Caused Quenching Probe–Encapsulating Solid Lipid Nanoparticles, Inhaled

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.

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Solid Lipid Nanoparticles for Topical Delivery of Acitretin for the Treatment of Psoriasis by Design of Experiment

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2019.12.2.5 ◽

2020 ◽

Vol 12 (2) ◽

pp. 4474-4491

Author(s):

Rajkumar Aland ◽

Ganesan M ◽

P. Rajeswara Rao ◽

Bhikshapathi D. V. R. N.

Keyword(s):

Particle Size ◽

Drug Release ◽

Solid Lipid Nanoparticles ◽

Drug Loading ◽

Entrapment Efficiency ◽

Lipid Nanoparticles ◽

Tem Analysis ◽

In Vitro Drug Release ◽

Solid Lipid

The main objective for this investigation is to develop and optimize the solid lipid nanoparticles formulation of acitretin for the effective drug delivery. Acitretin loaded SLNs were prepared by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency. Based on the results from the analyses of the responses obtained from Taguchi design, three different independent variables including surfactant concentration (%), lipid to drug ratio (w/w) and sonication time (s) were selected for further investigation using central composite design. The lipid Dynasan-116, surfactant poloxomer-188 and co surfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, zeta potential, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. TEM analysis has demonstrated the presence of individual nanoparticles in spherical shape and the results were compatible with particle size measurements. In vitro drug release of optimized SLN formulation (F2) was found to be 95.63 ± 1.52%, whereas pure drug release was 30.12 after 60 min and the major mechanism of drug release follows first order kinetics release data for optimized formulation (F2) with non-Fickian (anomalous) with a strong correlation coefficient (R2 = 0.94572) of Korsemeyer-Peppas model. The total drug content of acitretin gel formulation was found to 99.86 ± 0.012% and the diameter of gel formulation was 6.9 ± 0.021 cm and that of marketed gel was found to be 5.7 ± 0.06 cm, indicating better spreadability of SLN based gel formulation. The viscosity of gel formulation at 5 rpm was found to be 6.1 x 103 ± 0.4 x 103 cp. The release rate (flux) of acitretin across the membrane and excised skin differs significantly, which indicates about the barrier properties of skin. The flux value for SLN based gel formulation (182.754 ± 3.126 μg cm−2 h−1) was found to be higher than that for marketed gel (122.345 ± 4.786 μg cm−2 h−1). The higher flux and Kp values of SLN based gel suggest that it might be able to enter the skin easily as compared with marketed gel with an advantage of low interfacial tension of the emulsifier film that ensures an excellent contact to the skin. This topically oriented SLN based gel formulation could be useful in providing site-specific dermal treatment of psoriasis

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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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Anti-glioma activity and the mechanism of cellular uptake of asiatic acid-loaded solid lipid nanoparticles

International Journal of Pharmaceutics ◽

10.1016/j.ijpharm.2016.01.018 ◽

2016 ◽

Vol 500 (1-2) ◽

pp. 305-315 ◽

Cited By ~ 30

Author(s):

Tanem Garanti ◽

Aneta Stasik ◽

Andrea Julie Burrow ◽

Mohamed A. Alhnan ◽

Ka-Wai Wan

Keyword(s):

Cellular Uptake ◽

Solid Lipid Nanoparticles ◽

Lipid Nanoparticles ◽

Asiatic Acid ◽

Solid Lipid

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Development of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers of Loteprednol Etabonate: Physicochemical Characterization and Ex Vivo Permeation Studies

10.21203/rs.3.rs-1145116/v1 ◽

2021 ◽

Author(s):

Burcu Üner ◽

Samet Özdemir ◽

Çetin Taş ◽

Yıldız Özsoy ◽

Melike Üner

Keyword(s):

Particle Size ◽

Solid Lipid Nanoparticles ◽

Drug Loading ◽

Physicochemical Characterization ◽

Lipid Nanoparticles ◽

Nanostructured Lipid Carriers ◽

Fickian Diffusion ◽

Control Group ◽

Loteprednol Etabonate ◽

Solid Lipid

Abstract Purpose Loteprednol etabonate (LE) is a new generation corticosteroid that is used for the treatment of inflammatory and allergic conditions of the eye, and management of seasonal allergic rhinitis nasally. LE which is a poorly soluble drug with insufficient bioavailability, has a high binding affinity to steroid receptors. Sophisticated colloidal drug delivery systems of LE could present an alternative for treatment of inflammatory and allergic conditions of the skin. For this purpose, solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) were attempted to improve for transdermal LE delivery for the first time. Methods SLN and NLC were produced by hot homogenization and ultrasonication technique. Formulations were characterized by dynamic light scattering, scanning electron microscopy, fourier transform infrared spectroscopy and differential scanning calorimetry. Their physical stability was monitored for 3 months of storage. Drug release profiles and permeation properties of SLN and NLC through the porcine skin were investigated. Results It was determined that SLN and NLC below 150 nm particle size had a homogeneous particle size distribution as well as high drug loading capacities. They were found to be stable both physically and chemically at room temperature for 90 days. In terms of release kinetics, it was determined that they released from SLN and NLC in accordance with Fickian diffusion release. Formulations prepared in this study were seen to significantly increase drug penetration through pig skin compared to the control group (p ≤ 0.05). Conclusion SLN and NLC formulations of LE can be stated among the systems that can be an alternative to conventional systems with less side-effect profile in the treatment of inflammatory problems on the skin.

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Enhancement of ciprofloxacin activity by incorporating it in solid lipid nanoparticles

Tropical Journal of Pharmaceutical Research ◽

10.4314/tjpr.v19i5.1 ◽

2020 ◽

Vol 19 (5) ◽

pp. 909-918

Author(s):

Saqer Alarifi ◽

Salam Massadeh ◽

Mohammed Al-Agamy ◽

Manal A.l. Aamery ◽

Abdulkareem Al Bekairy ◽

...

Keyword(s):

Escherichia Coli ◽

Pseudomonas Aeruginosa ◽

Antimicrobial Activity ◽

Particle Size ◽

Solid Lipid Nanoparticles ◽

Entrapment Efficiency ◽

Lipid Nanoparticles ◽

Release Profile ◽

Drug Release Profile ◽

Solid Lipid

Purpose: To incorporate ciprofloxacin (CIP) into solid lipid nanoparticles (SLN) in order to enhance its biopharmaceutical properties and antibacterial activity.Methods: A sonication melt-emulsification method was employed for the preparation of CIP-loaded SLN. The composition of the SLN was varied in order to investigate factors such as lipid type and combination ratio, drug to lipid ratio, and surfactant ratio. The produced SLN formulations wereevaluated for their particle size and shape, zeta potential, and entrapment efficiency. In addition, the effect of SLN formulation composition on its drug release profile and antimicrobial activity against Escherichia coli, Pseudomonas Aeruginosa, and Staphylococcus Aureus was also investigated.Results: The generated nanoparticles had particle size in the range of 165 to 320 nm. The zetapotential values were generally low within ± 5. All formulations exhibited entrapment efficiency between 50 and 90 %. CIP release exhibited a biphasic release profile with a low burst phase, followed by uniform controlled-release behavior of various rates. SLN-loaded CIP exhibited one-fold reduction in minimum inhibitory concentration (MIC) and caused significant inhibition of all the three bacterial strains tested, when compared with pure CIP.Conclusion: Loading of CIP into SLN significantly enhances its antimicrobial activity in vitro which can translate to significant enhancement of therapeutic outcomes by minimizing the dose-dependent adverse and side effects and/or enhancing the antimicrobial spectrum of activity. Keywords: Solid lipid nanoparticles, Sonication melt-emulsification, Ciprofloxacin, Escherichia coli, Pseudomonas aeruginosa

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Development of Mupirocin- Tinidazole solid- Lipid Nanoparticles Loaded Topical gel for the Management of Bacterial Wound Infections

Research Journal of Pharmacy and Technology ◽

10.52711/0974-360x.2021.00491 ◽

2021 ◽

pp. 2785-2790

Author(s):

Veintramuthusankar Veintramuthusankar ◽

Pushparajudayakumar Pushparajudayakumar ◽

Rajanduraibabyroselin Rajanduraibabyroselin

Keyword(s):

Particle Size ◽

Drug Release ◽

Solid Lipid Nanoparticles ◽

Lipid Nanoparticles ◽

Fickian Diffusion ◽

Standard Drug ◽

Topical Gel ◽

Solid Lipid ◽

Homogenization Technique ◽

Significant Difference

Solid lipid nanoparticles (SLNs) are novel drug carrier system which consists of a solid matrix composed of a lipid being solid at both room and body temperatures with a mean Particle Size (PS) between 50 and 1000 nm Mupirocin -Tinidazole solid-lipid nanoparticles were prepared using hot homogenization technique using Glyceryl monosterate, Stearic acid, Tween 80 and Poloxamer 188 using hot homogenization technique. Size of the nanoparticles was in the range of 83 to 211 nm with the zeta potential values between -2.1 to -5.2. Atomic Force Microscopy (AFM) confirms the spherical shape of solid lipid nanoparticles. Entrapment efficiency was best in the F1 formulation. In vitro release of the pure drug was found to be 75% of mupirocin and 66.5% of tinidazole at the end of 1 hr. Drug release from SLNs dispersion followed Korsermeyrs peppas-model, indicating fickian diffusion drug release, while that from the gel followed non Fickian model drug release. Antibacterial activity of the SLNs was less but the SLNs based gel shows no significant difference in activity to that of standard drug gentamycin against aerobic bacteria. The SLNs dispersion exhibited physicochemical stability under refrigeration upto 45 days without significant difference in particle size. Best formulation was developed into a topical gel using sodium alginate and it was evaluated for pH, viscosity, spreadbility, extrudability, bloom strength, Minimum Inhibitory Concentration (MIC) and Methicillin resistant staphylococcus aureus (MRSA). Extrudability and spreadability parameters of the gel are similar to that of marketed Mupirocin 2% cream formulation

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FORMULATION AND EVALUATION OF DASATINIB LOADED SOLID LIPID NANOPARTICLES

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2018v10i12.27567 ◽

2018 ◽

Vol 10 (12) ◽

pp. 14 ◽

Cited By ~ 2

Author(s):

M. Yasmin Begum ◽

Prathyusha Reddy Gudipati

Keyword(s):

Particle Size ◽

Drug Release ◽

Zeta Potential ◽

Solid Lipid Nanoparticles ◽

Entrapment Efficiency ◽

Lipid Nanoparticles ◽

Size Analysis ◽

Compatibility Study ◽

Solid Lipid ◽

Poly Dispersity Index

Objective: The aim of present work was to formulate and evaluate Dasatinib (DST) loaded solid lipid nanoparticles (SLNs) as a potential anticancer drug delivery system by enhancing its solubility.Methods: SLNs consist of a solid lipid matrix where the drug was incorporated. Surfactants of GRAS grade were used to avoid aggregation and to stabilize the SLNs. DST-SLNs formulations of varying concentrations were prepared by high speed homogenization technique and evaluated for drug excipients compatibility study, poly-dispersity index, particle size analysis, surface morphology, zeta potential and drug release features.Results: It was observed that DST-SLNs with optimum quantities of poloxomer: lecithin ratio showed 88.06% drug release in 6h with good entrapment efficiency of 76.9±0.84 %. Particle size, Poly dispersity index, zeta potential and drug entrapment efficiency for the optimized formulation was found to be optimum. Stability studies revealed that the entrapment efficiency of the SLN dispersion stored in 4 °C was stable.Conclusion: Thus, it can be concluded that formulations of DST loaded SLNs are suitable carriers for improving the solubility and dissolution related problems.

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