scholarly journals Formulation of Solid Lipid Nanoparticles of Cilnidipine for the Treatment of Hypertension

2019 ◽  
Vol 9 (3) ◽  
pp. 212-221 ◽  
Author(s):  
Aparna Bhalerao ◽  
Pankaj Prakash Chaudhari
Keyword(s):  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Lipid Nanoparticles ◽  
Water Soluble ◽  
Solid Lipid Nanoparticle ◽  
Solid Lipid ◽  
Lipid Nanoparticle

Cilinidipine is a fourth generation N and L-type calcium channel antagonists used alone or in combination with another drug to treat hypertension. Cilnidipine is poorly water -soluble, BCS class II drug with 6 to 30 percent oral bioavailability due to first pass metabolism. So to protect the drug from degradation and improve its dissolution, solid lipid nanoparticles were prepared. Glyceryl monostearate was selected as lipid while span 20: tween 20 were selected as surfactant blends. The formulations were evaluated for various parameters, as percent transmittance, drug content, percent encapsulation efficiency; percent drug loading, In vitro drug release and particle size. Optimized formulation was lyophilized using lactose as a cryo-protectant. The lyophilized formulation was evaluated for micromeritic properties, particle size and in vitro dissolution. It was further evaluated for DSC, XRD, and SEM. Percent encapsulation efficiency and percent drug loading of optimized formulation (F3) were 78.66percent and 9.44percent respectively. The particle size of F3 formulation without drug was 204 nm and with the drug was 214 nm. The particle size of the reconstituted SLN was 219 nm. In DSC study, no obvious peaks for cilnidipine were found in the SLN of cilnidipine indicated that the cilnidipine must be present in a molecularly dissolved state in SLN. In X-ray diffractometry absence of peaks representing crystals of cilnidipine in SLN indicated that the drug was in an amorphous or disordered crystalline phase in the lipid matrix. Thus, solid lipid nanoparticle formulation is a promising way to enhance the dissolution rate of cilnidipine. Keywords: Cilnidipine, Solid Lipid Nanoparticle, Hypertension

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

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

scholarly journals DEVELOPMENT AND OPTIMIZATION OF TAZAROTENE LOADED SOLID LIPID NANOPARTICLES FOR TOPICAL DELIVERY

2019 ◽  
pp. 63-77
Author(s):  
RAJKUMAR ALAND ◽  
GANESAN M ◽  
RAJESWARA RAO P
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Lipid Nanoparticles ◽  
World Population ◽  
Transmission Electron Microscopy Analysis ◽  
In Vitro Drug Release ◽  
Solid Lipid

Objective: Psoriasis is an unswervingly recurring, inflammatory, autoimmune disorder of the skin, disturbing about 2–5% of the world population. The main objective for this investigation is to develop and optimize the solid lipid nanoparticles (SLN) formulation of tazarotene for effective drug delivery. Methods: Tazarotene SLNs were fabricated by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency (EE). In view of the outcomes from the examinations of the responses acquired from Taguchi design, three diverse independent variables including sonication time (s), lipid to drug ratio (w/w), and surfactant concentration (%) were carefully chosen for further investigation utilizing central composite design. The lipid dynasan-116, surfactant poloxamer-188, and cosurfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, drug EE, zeta potential, in vitro drug release, and stability. Results: The prepared nanoformulations were evaluated for different parameters and found to be in an acceptable range. In vitro drug release of optimized SLN formulation (F1) was found to be 98.12±1.52%, whereas pure drug release was 42.12 after 60 min, and the major mechanism of drug release follows zero-order kinetics release data for optimized formulation (F1) with non-Fickian (anomalous) with a strong correlation coefficient (R2=0.98598) of Korsmeyer-Peppas model. Transmission electron microscopy analysis has demonstrated the presence of individual nanoparticles in spherical shape, and the results were also compatible with particle size measurements. The drug content of tazarotene gel formulation was found to 98.96±0.021%, and the viscosity of gel formulation at 5 rpm was found to be 5.98×103±0.34×103 cp. The release rate (flux) of tazarotene across the membrane and expunged skin diverges pointedly, which specifies the barrier nature of skin. The flux value for SLN based gel formulation (193.454±4.324 μg/cm2/h) was found to be higher than that for marketed gel (116.345±2.238 μg/cm2/h). 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. Conclusion: From the obtained results, the topically oriented SLN-based gel formulation of tazarotene could be useful in providing effective and site-specific psoriasis treatment.

scholarly journals Formulation and evaluation of prazosin hydrochloride loaded solid lipid nanoparticles

2018 ◽  
Vol 8 (6-s) ◽  
pp. 63-69
Author(s):  
Sandip Akaram Bandgar ◽  
Pranali Dhavale ◽  
Pravin Patil ◽  
Sardar Shelake ◽  
Shitalkumar Patil
Keyword(s):  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
Entrapment Efficiency ◽  
Aqueous Solubility ◽  
Lipid Nanoparticles ◽  
Solid Lipid Nanoparticle ◽  
Bioavailability Enhancement ◽  
Solid Lipid ◽  
Lipid Nanoparticle ◽  
Optimum Stability

Solid Lipid Nanoparticles (SLN) are rapidly developing field of nanotechnology with several potential application in drug delivery and research. Drugs having low aqueous solubility not only give low oral bioavailability but provide high inter-and intra subject variability. The purpose of the present study was to investigate the bioavailability enhancement of Prazosin Hydrochloride drug by formulating solid lipid nanoparticle. Prazosin Hydrochloride Drug is an antihypertensive drug with limited bioavailability so that solid lipid nanoparticle (SLN) is one of the approaches to improve bioavailability. SLN were prepared using glyceryl monostearate by hot homogenization followed by Solvent emulsification-ultrasonication. Prazosin Hydrochloride loaded SLN were characterized and optimized by parameters like particle size, zeta potential, XRD, DSC. Proposing Hydrochloride loaded SLN having the particle size 263.8±1.88 and entrapment efficiency 89.29±0.65% shows better bioavailability and optimum stability in studies. The SLN studies prepared using glyceryl mono stearate   as a lipid and Polaxamer 407 as a polymer leads to improve bioavailability of the drug. Keywords: Prazosin Hydrochloride, Solid Lipid Nanoparticles, Entrapment efficiency, DSC

scholarly journals Short Term Stability Testing of Efavirenz-Loaded Solid Lipid Nanoparticle (SLN) and Nanostructured Lipid Carrier (NLC) Dispersions

Pharmaceutics ◽  
2019 ◽  
Vol 11 (8) ◽  
pp. 397 ◽  
Author(s):  
Pedzisai A. Makoni ◽  
Kasongo Wa Kasongo ◽  
Roderick B. Walker
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Encapsulation Efficiency ◽  
Lipid Nanoparticles ◽  
Nanostructured Lipid Carriers ◽  
Nanostructured Lipid Carrier ◽  
Solid Lipid Nanoparticle ◽  
Short Term ◽  
Term Stability ◽  
Solid Lipid ◽  
Lipid Nanoparticle

The short term stability of efavirenz-loaded solid lipid nanoparticle and nanostructured lipid carrier dispersions was investigated. Hot High Pressure Homogenization with the capability for scale up production was successfully used to manufacture the nanocarriers without the use of toxic organic solvents for the first time. Glyceryl monostearate and Transcutol® HP were used as the solid and liquid lipids. Tween® 80 was used to stabilize the lipid nanocarriers. A Box-Behnken Design was used to identify the optimum operating and production conditions viz., 1100 bar for 3 cycles for the solid lipid nanoparticles and 1500 bar for 5 cycles for nanostructured lipid carriers. The optimized nanocarriers were predicted to exhibit 10% efavirenz loading with 3% and 4% Tween® 80 for solid lipid nanoparticles and nanostructured lipid carriers, respectively. Characterization of the optimized solid lipid nanoparticle and nanostructured lipid carrier formulations in relation to shape, surface morphology, polymorphism, crystallinity and compatibility revealed stable formulations with particle sizes in the nanometer range had been produced. The nanocarriers had excellent efavirenz loading with the encapsulation efficiency >90%. The optimized nanocarriers exhibited biphasic in vitro release patterns with an initial burst release during the initial 0–3 h followed by sustained release over a 24 h period The colloidal systems showed excellent stability in terms of Zeta potential, particle size, polydispersity index and encapsulation efficiency when stored for 8 weeks at 25 °C/60% RH in comparison to when stored at 40 °C/75% RH. The formulations manufactured using the optimized conditions and composition proved to be physically stable as aqueous dispersions.

scholarly journals Preparation of Curcumin Solid Lipid Nanoparticles Loaded with Flower-Shaped Lactose for Lung Inhalation and Preliminary Evaluation of Cytotoxicity In Vitro

2021 ◽  
Vol 2021 ◽  
pp. 1-15
Author(s):  
Nan Li ◽  
Xu Li ◽  
Peng Cheng ◽  
Ping Yang ◽  
Pengcheng Shi ◽  
...  
Keyword(s):  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
Freeze Drying ◽  
Drug Loading ◽  
In Vitro Release ◽  
Dry Powder Inhaler ◽  
Lipid Nanoparticles ◽  
Solid Lipid ◽  
Vitro Release

The purpose of this study is to design a flower-shaped lactose loaded curcumin solid lipid nanoparticles dry powder inhaler and characterize it to improve the solubility and dissolution rate of curcumin in lung. Curcumin solid lipid nanoparticles (Cur-SLNs) were prepared by solvent evaporation method, and then they were micronized by freeze-drying technology. Finally, Cur-SLN micropowder obtained by freeze-drying was mixed with flower-shaped lactose (FL) at a ratio of 2 : 1 and then passed through a 200-mesh sieve to obtain Cur-SLN-FL powder. Tween-80 was selected as the surfactant to inhibit the aggregation of drug solid lipid nanoparticles. Under the optimum conditions, the solid lipid nanoparticles (SLN) were relatively spherical, with an average particle size of 14.7 nm, narrow distribution, Zeta potential of −22.5 mV, encapsulation efficiency of 90.21%, and drug loading of 8.56%. According to the particle size, PI, Zeta potential, drug loading (LC%), encapsulation efficiency (EE%), morphology, and in vitro release characteristics, the prescription of solid lipid nanoparticles was screened. Dry powder inhaler (DPI) was characterized by differential scanning calorimetry, scanning electron microscopy, particle size, density, and in vitro release performance. Its cytotoxicity to mouse fibroblasts (L929) and human normal lung epithelial cells (BEAS-2B) in vitro was investigated, and its safety for pulmonary inhalation was preliminarily determined. FTIR analysis shows that the micronized Cur-SLN-FL has the same chemical structure as FL. FTIR and DSC analysis confirmed that the characteristic absorption peak of curcumin was not found in Cur-SLN-FL, showing similar structure to SLN and FL. In addition, curcumin was coated in solid lipid nanoparticles to make powder mist, which increased its drug loading, kept its aerodynamic particle size (4.03 ± 0.40) μm, and significantly improved its drug release performance in artificial lung fluid. In vitro cytotoxicity test results confirmed that Cur-SLN-FL was less toxic to BEAS-2B cells than L929 cells. Therefore, curcumin was prepared into solid lipid nanoparticles by emulsion evaporation-low temperature solidification method and then micronized and mixed with FL to prepare curcumin solid lipid nanoparticle powder mist loaded with flower-shaped lactose. The process is simple and feasible, and it has better safety performance for lung cells, which is expected to become a safe and effective delivery system for pulmonary inhalation drugs.

Folate conjugated solid lipid nanoparticle: formulation development, optimization and characterization

2021 ◽  
Vol 11 ◽  
Author(s):  
Vaibhav Rajoriya ◽  
Varsha Kashaw ◽  
Sushil Kumar Kashaw
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
In Vitro Drug Release ◽  
Solid Lipid ◽  
Release Study

Objective: The current paper represents the development, optimization, and characterization of paclitaxel-loaded folate conjugated solid lipid nanoparticles (FA-SLNs). Methods: The ligand (FA-SLNs) conjugated and non-conjugated SLNs (PTX-SLNs) were prepared by hot homogenization method. Both of the formulations (FA-SLNs and PTX-SLNs) were optimized with various parameters i.e. drug loading, stirring time, stirring speed, particle size, and polydispersity index, and characterized. The in-vitro drug release study was performed in different pH environments by using the dialysis bag method. The surface morphology and particle size were determined through scanning electron micorscopy and Transmission Electron Microscopy respectively, The SLNs formulations were also evaluated for the stability study. Result: The particle size of PTX-SLNs and FA-SLNs was determined and found to be 190.1±1.9 and 231.3±2.3 nm respectively. The surface morphology of the SLNs indicates that the prepared formulations are round-shaped and show smooth surfaces. The TEM study indicated that particles were in the range of 100-300 nm. The entrapment efficiency and drug loading capacity of FA-SLNs were found to be 79.42±1.6% and 17.3±1.9%, respectively. In-vitro drug release study data, stated that the optimum drug release was found in an acidic environment at pH 4.0, that showed 94.21% drug release after 16 hours and it proves that optimized formulation FA-SLNs will gave the sustained and better release in tumor tissue that owing acidic environment because of the angiogenesis process. Conclusion: In this research paper, different formulation parameters, found to influence fabrication of drug into Solid lipid nanoparticles, were optimized for high entrapment efficiency and drug loading. The most important parameters were drug:lipid ratio, drug:polymer ratio and lipid: surfactant ratio. Higher in-vitro drug release was observed in pH 4 as compared to the pH 7.4. These result data concludes that FA-SLNs formulation was successfully prepared, optimized and characterized.

Comparison of Freeze and Spray Drying to Obtain Primaquine-Loaded Solid Lipid Nanoparticles

2017 ◽  
Vol 2 (2) ◽  
pp. 31-50
Author(s):  
James Jorum Owuor ◽  
Florence Oloo ◽  
Japheth Kibet Ngetich ◽  
Mwaiwa Kivunzya ◽  
Wesley Nyaigoti Omwoyo ◽  
...  
Keyword(s):  
Spray Drying ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Lipid Nanoparticles ◽  
Solid Lipid Nanoparticle ◽  
Drug Release Profile ◽  
Solid Lipid ◽  
Freeze Dried

This article describes how the spray drying and freeze drying of various nanosized Solid Lipid Nanoparticle (SLN) and the physicochemical attributes of the acquired particles were examined. Primaquine loaded Solid Lipid Nanoparticles dried by the two strategies is examined. Particles were characterised by determination of size, drug loading, encapsulation efficiency and surface morphology. In vitro and kinetic drug discharge models were also considered. Preparation parameters have no impact on the molecule morphology and properties, and the main parameter deciding the molecule attributes in the drug substance of the nanoparticle, either in the spraying or in the freezing technique of drying. The drug release profile of spray dried SLN is superior to that of the freeze dried SLN.

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. 

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

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.

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

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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