scholarly journals Atorvastatin Solid Lipid Nanoparticles as a Promising Approach for Dermal Delivery and an Anti-inflammatory Agent

2020 ◽  
Vol 21 (7) ◽  
Author(s):  
Seyed Sadegh Shahraeini ◽  
Jafar Akbari ◽  
Majid Saeedi ◽  
Katayoun Morteza-Semnani ◽  
Shidrokh Abootorabi ◽  
...  
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Solid Lipid ◽  
Inflammatory Agent ◽  
Drug Entrapment Efficiency ◽  
Anti Inflammatory ◽  
Dermal Delivery

Abstract In the current research, the main focus was to overcome dermal delivery problems of atorvastatin. To this end, atorvastatin solid lipid nanoparticles (ATR-SLNs) were prepared by ultra-sonication technique. The prepared SLNs had a PDI value of ≤ 0.5, and the particle size of nanoparticles was in the range 71.07 ± 1.72 to 202.07 ± 8.40 nm. It was noticed that, when the concentration of lipid in ATR-SLNs increased, the size of nanoparticles and drug entrapment efficiency were also increased. Results showed that a reduction in the HLB of surfactants used in the preparation of SLN caused an increase in the particle size, zeta potential (better stability), and drug entrapment efficiency. Despite Tween and Span are non-ionic surfactants, SLNs containing these surfactants showed a negative zeta potential, and the absolute zeta potential increased when the concentration of Span 80 was at maximum. DSC thermograms, FTIR spectra, and x-ray diffraction (PXRD) pattern showed good incorporation of ATR in the nanoparticles without any chemical interaction. In vitro skin permeation results showed that SLN containing atorvastatin was capable of enhancing the dermal delivery of atorvastatin where a higher concentration of atorvastatin can be detected in skin layers. This is a hopeful promise which could be developed for clinical studies of the dermal delivery of atorvastatin nanoparticles as an anti-inflammatory agent.

scholarly journals FORMULATION AND EVALUATION OF DASATINIB LOADED SOLID LIPID NANOPARTICLES

2018 ◽  
Vol 10 (12) ◽  
pp. 14 ◽  
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. 

scholarly journals Preparation and Characterization of Solid Lipid Nanoparticles Loaded with Cisplatin

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.

scholarly journals TOPICAL SOLID LIPID NANOPARTICLES BASED GEL OF LAVENDER ESSENTIAL OIL FOR ANTI‑INFLAMMATORY ACTIVITY

2019 ◽  
pp. 175-182
Author(s):  
PALLAVI M CHAUDHARI ◽  
VAISHNAVI M BIND
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Essential Oil ◽  
Solid Lipid Nanoparticles ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Inflammatory Activity ◽  
Solid Lipid ◽  
Anti Inflammatory

Objective: The main objective of the study was to formulate and evaluate and perform an optimization study of lavender essential oil loaded solid lipid nanoparticles (SLNs) based gel. Materials and Methods: SLNs were prepared by the hot homogenization technique. A total of eight formulations were formulated as per 23 factorial design by design expert 11 software. The formulated SLNs were further evaluated for particle size, entrapment efficiency, drug release profile. After evaluation, the optimized batch was further used for formulating gel. The formulated gel was further subjected to ex vivo studies. Results: After the evaluation of all the parameters, batch 7 was found to be optimized. Batch 7 was found to have the lowest particle size of 30.91±0.30, higher entrapment efficiency of 89.99±0.87, and higher drug release of 90.41±0.55. It was further used for formulating gel which was found to be consistent, homogenous, smooth, and spreadable. The % inhibition of the formulated SLN based gel was found to be 28±0.1%. Conclusion: The SLNs were prepared and were formulated into the gel. The gel showed anti-inflammatory activity.

scholarly journals FORMULATION DEVELOPMENT, CHARACTERIZATION, AND IN VITRO-IN VIVO STUDY OF ANTIHYPERLIPIDEMIC DRUG ROSUVASTATIN CALCIUM - SOLID LIPID NANOPARTICLES

2018 ◽  
Vol 11 (7) ◽  
pp. 436 ◽  
Author(s):  
Harjeet Singh ◽  
Ram Dayal Gupta ◽  
Girendra Gautam
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Pharmacokinetic Studies ◽  
In Vitro Drug Release ◽  
Drug Entrapment Efficiency ◽  
Rosuvastatin Calcium

Objective: The aim of this study was to formulate and optimize solid lipid nanoparticles (SLNs) for the enhancement of solubility and bioavailability of the poorly aqueous soluble drug rosuvastatin calcium.Methods: SLNs were prepared by slight modification of solvent emulsification-diffusion technique and analyzed for particle size, zeta potential, drug entrapment efficiency, in vitro drug release, stability, and pharmacokinetic studies. Rosuvastatin calcium SLNs were formulated using stearic acid as main lipid, poloxamer 407 as surfactant, and Tween 80 as cosurfactant.Results: All parameters were found to be in an acceptable range. Optimized formulation OR2 SLNs have shown mean particle size 115.49±2.97 nm with polydispersity index value of 0.456, zeta potential - 18.40 mV, 60.34% drug loading, and 97.16% drug entrapment efficiency. In vitro drug release was found to be 88.70±3.59% after 12 h with sustained release and was fitted with Higuchi model with a very high correlation coefficient (R2=0.9905). Transmission electron microscopy confirms that the SLNs of selected optimized formulation are circular in shape. Differential scanning calorimetry and X-ray diffraction confirm the formation of amorphous product. 1H nuclear magnetic resonance studies confirm the intermolecular hydrogen bonding between drug and lipid. Pharmacokinetic studies showed an optimized formulation OR2 SLNs enhanced bioavailability with 4.44-fold as compare to plain drug suspension. Optimized formulation OR2 SLNs have shown good stability at 25±2°C and 60±5°C relative humidity for 180 days.Conclusion: Thus, the current study can be useful for the successful development of optimized SLNs and able to enhance the bioavailability of poorly soluble drug rosuvastatin calcium.

Research: Design, development and optimization of ramipril solid lipid nanoparticles using solvent emulsification and evaporation method

2019 ◽  
Vol 09 ◽  
Author(s):  
Rohan R. Vakhariya ◽  
Vijay R. Salunkhe ◽  
Dheeraj S. Randive ◽  
Mangesh A. Bhutkar ◽  
Somnath D. Bhinge
Keyword(s):  
Particle Size ◽  
Side Effects ◽  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Evaporation Method ◽  
Solid Lipid ◽  
Particle Size Analyzer

Background: Ramipril, an antihypertensive drug exhibit 28% of oral bioavailability and also expelled quickly through the kidneys. Moreover, numerous side effects reported by the ramipril such as, hypotension (postural), increasing potassium level, and angioedema, when presented as an immediate dosage form. Hence, to conquer the side-effects associated with the drug and to increase its bioavailability. Objective: The intention of the proposed approach was to design, develop and optimize Ramipril loaded solid lipid nanoparticles. Methods: Solvent emulsification and evaporation method were employed to prepare Ramipril loaded solid lipid nanoparticles containign stearic acid and phosphatidylcholine as a lipid and surfactant respectively. The prepared formulations have been confirmed with particle size analyzer, %entrapment efficiency, Zeta Potential, SEM, X-ray diffraction study, FTIR, NMR spectroscopy, in-vitro release study and stability study. Result: The obtained results were noted to be within the standard limits. No interaction between Ramipril and other excipients, were confirmed with the FT-IR study of the formulations. Particle size analyzer confirmed that the nanometer size of prepared formulations ranges between 200-350nm. Percent entrapment efficiency was observed in the range of 70.61–91.60%. Entrapment and particle size results of the nanoparticles from R5 batch was an adjudged. The designed formulation noted 70.50% cumulative drug release within a period of 7hrs. The designed batch showed mean of zeta potential at-29.4 mV exhibiting good stability of formulation. Conclusion: The developed formulation was found to be stable and safe, and represents a promising system for the sustained and controlled delivery of Ramipril.

scholarly journals Development and Evaluation of Lapatinib Solid Lipid Nanoparticles in the Management of Breast Cancer

2019 ◽  
Vol 11 (05) ◽  
Author(s):  
Pamu Sandhya
Keyword(s):  
Breast Cancer ◽  
Particle Size ◽  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Drug Dissolution ◽  
Dissolution Studies ◽  
Solid Lipid

The current research was aimed at formulation of Lapatinib loaded solid lipid nanoparticles (SLNs) followed by evaluation for effective treatment of breast cancer. The formulations prepared by homogenization and ultrasonication and evaluated for zeta potential, particle size, polydispersity index, entrapment efficiency and in- vitro dissolution studies. Entrapment efficiency studies indicated proportional relation between concentration of lipid and the amount of drug entrapped. The physicochemical parameter evaluation data indicated 94.27% entrapment efficiency, 130 nm particle size and -19.9 zeta potential for stable formulation. The in vitro drug dissolution studies indicated that Lapatinib loaded SLNs (F6) formulated with Dynasan 116 and Egg Lecithin was suitable for anti-cancer therapy with higher drug dissolution rate.

Optimization of Itroconazole Solid Lipid Nanoparticles for Topical Delivery

2020 ◽  
Vol 10 (4) ◽  
pp. 381-389
Author(s):  
Pallavi M. Chaudhari ◽  
Amruta R. Patil
Keyword(s):  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Topical Delivery ◽  
Lipid Nanoparticles ◽  
X Ray Diffraction ◽  
High Concentration ◽  
Solid Lipid ◽  
Drug Entrapment Efficiency

Introduction: The objective of this study was to formulate water-insoluble drug Itraconazole (ITZ) into Solid Lipid Nanoparticles (SLNs) for topical delivery. Methods: The drug-loaded SLNs were prepared by Microemulsion method using cholesterol (CH) and Lubritab (LU) and further characterized for different parameters like particle size, zeta potential, drug entrapment efficiency etc. The mean particle size with Lubritab SLN was in the range 155.01-161.67 nm, whereas for Cholestrol SLN it was in the range of 218.87-230.16 nm. SEM showed spherical nature of the SLNs. Results: The entrapment efficiency of SLN was found to be more for cholesterol as compared to Lubritab. The crystalline properties of drug was reduced in SLNs as evaluated by X-ray diffraction (XRD). Ex vivo study indicated the ITZ-SLN exhibited high concentration. Conclusion: The permeability of drug was studied by use of Franz-diffusion cell, and permeation of drug through Lubritab SLN (ITZ LU) was higher than that of Cholesterol SLN (ITZ CH). The formulated ITZ-SLNs exhibited clear zone.

scholarly journals DEVELOPMENT AND EVALUATION OF TIZANIDINE HYDROCHLORIDE LOADED SOLID LIPID NANOPARTICLES

2019 ◽  
pp. 152-158
Author(s):  
PAVITHRA K ◽  
BHAGAWATI ST ◽  
MANJUNATH K
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Primary Objective ◽  
Release Mechanism ◽  
Release Kinetic ◽  
Solid Lipid

Objectives: The primary objective of the present study is to develop and evaluate tizanidine hydrochloride (TZ) solid lipid nanoparticles (SLNs) using solid lipids/triglycerides. Methods: TZ SLNs were prepared by hot homogenization followed by ultrasonication technique. The prepared SLNs were characterized for drug content, entrapment and loading efficiency, particle size, zeta potential, polydispersity index (PDI), and in intro release kinetics. Results: TZ SLNs were prepared. The particle size ranged from 49.7 to 523.7 nm. PDI of all formulations was good within the range of 0.189–0.487. The zeta potential of blank SLNs was −15.2 mV whereas drug-loaded SLNs showed zeta potential from −8.85 mV to −42.0 mV. Entrapment efficiency observed was in the range of 34.5–75.0%. The cumulative percentage release of TZ from different TZ nanoparticles varied from 35.28% to 83.98% depending on the drug-lipid ratio and the type of lipid and surfactant used. The release kinetic studies of optimized formulation showed that the release was first order and the release mechanism was non-Fickian type. Conclusion: The prepared SLNs were able to sustain the drug release for 24 h, thus reducing dosing frequency and occurrence of side effects, thereby increasing the effectiveness of the drug.

scholarly journals Development of Perphenazine-Loaded Solid Lipid Nanoparticles: Statistical Optimization and Cytotoxicity Studies

2021 ◽  
Vol 2021 ◽  
pp. 1-14
Author(s):  
Parisa Abbasi Farsani ◽  
Reza Mahjub ◽  
Mojdeh Mohammadi ◽  
Seyed Sajad Oliaei ◽  
Mohammad Mehdi Mahboobian
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Statistical Optimization ◽  
Oral Dosage ◽  
Solid Lipid ◽  
Cytotoxicity Studies ◽  
Xrd Studies

Objective. Perphenazine (PPZ), as a typical antipsychotic medical substance, has the same effectiveness compared to atypical antipsychotic medications for the treatment of schizophrenia. Despite the lipophilic essence, PPZ encounters limited bioavailability caused by the first-pass metabolism following oral administration. In the present study, PPZ-containing solid lipid nanoparticles (PPZ-SLNs) were prepared and optimized based on different factors, including lipid and surfactant amount, to develop appropriate and safe novel oral dosage forms of PPZ. Methods. The solvent emulsification-evaporation method was utilized to form SLNs by using soybean lecithin, glycerol monostearate (GMS), and Tween 80. Statistical optimization was done by the Box-Behnken design method to achieve formulation with optimized particle size, entrapment efficiency, and zeta potential. Also, transmission electron microscopy, in vitro release behavior, differential scanning calorimetry (DSC), and powder X-ray diffractometry (P-XRD) studies and cytotoxicity studies were assessed. Results. Optimization exhibited the significant effect of various excipients on SLN characteristics. Our finding indicated that the mean particle size, zeta potential, and entrapment efficiency of optimized PPZ-SLN were, respectively, 104 ± 3.92   nm , − 28 ± 2.28   mV , and 83 % ± 1.29 . Drug release of PPZ-SLN was observed to be greater than 90% for 48 h that emphasized a sustained-release pattern. The DSC and P-XRD studies revealed the amorphous state of PPZ-SLN. FTIR spectra showed no incompatibility between the drug and the lipid. Performing cytotoxicity studies indicated no significant cytotoxicity on HT-29 cell culture. Conclusion. Our study suggests that PPZ-SLNs can make a promising vehicle for a suitable therapy of schizophrenia for the oral drug delivery system.

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. 

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