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.

scholarly journals Evaluation and Comparison of Solid Lipid Nanoparticles (SLNs) and Nanostructured Lipid Carriers (NLCs) as Vectors to Develop Hydrochlorothiazide Effective and Safe Pediatric Oral Liquid Formulations

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 437
Author(s):  
Paola Mura ◽  
Francesca Maestrelli ◽  
Mario D’Ambrosio ◽  
Cristina Luceri ◽  
Marzia Cirri
Keyword(s):  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Physical Stability ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Nanostructured Lipid Carriers ◽  
Particle Size Reduction ◽  
Solid Lipid ◽  
Oral Liquid

The aim of this study was the optimization of solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) in terms of physicochemical and biopharmaceutical properties, to develop effective and stable aqueous liquid formulations of hydrochlorothiazide, suitable for paediatric therapy, overcoming its low-solubility and poor-stability problems. Based on solubility studies, Precirol® ATO5 and Transcutol® HP were used as solid and liquid lipids, respectively. The effect of different surfactants, also in different combinations and at different amounts, on particle size, homogeneity and surface-charge of nanoparticles was carefully investigated. The best formulations were selected for drug loading, and evaluated also for entrapment efficiency and release behaviour. For both SLN and NLC series, the use of Gelucire® 44/14 as surfactant rather than PluronicF68 or Tween® 80 yielded a marked particle size reduction (95–75 nm compared to around 600–400 nm), and an improvement in entrapment efficiency and drug release rate. NLC showed a better performance than SLN, reaching about 90% entrapped drug (vs. 80%) and more than 90% drug released after 300 min (vs. about 65%). All selected formulations showed good physical stability during 6-month storage at 4 °C, but a higher loss of encapsulated drug was found for SLNs (15%) than for NLCs (<5%). Moreover, all selected formulations revealed the absence of any cytotoxic effect, as assessed by a cell-viability test on Caco-2 cells and are able to pass the intestinal epithelium as suggested by Caco-2 uptake experiments.

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

Nephrotoxicity of Albendazole and Albendazole-Loaded Solid Lipid Nanoparticles in Mice with Experimental Hydatidosis

2021 ◽  
Author(s):  
Kobra Kohansal ◽  
Abdollah Rafiei ◽  
Heibatullah Kalantari ◽  
Ali Jelowdar ◽  
Anayatollah Salimi ◽  
...  
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Physicochemical Characterization ◽  
Public Health Problem ◽  
New Product ◽  
Lipid Nanoparticles ◽  
Control Group ◽  
Histopathological Study ◽  
Normal Range ◽  
Solid Lipid

Purposes: Cystic echinococcosis (CE) is a serious contemporary public health problem. Different CE treatment methods are of considerable importance, with albendazole (ABZ) being one of the most preferred drugs for CE treatment and prophylaxis. In this study, we evaluated the nephrotoxicity caused by ABZ and ABZ-loaded solid lipid nanoparticles (SLNs) in mice with experimental hydatid cyst. Methods: ABZ-loaded SLNs were produced by micro-emulsification and a high shear homogenization technique. Thereafter, we evaluated the physicochemical characterization of the product. Live protoscolices were injected into mice to induce experimental hydatidosis. Mice were then treated with ABZ and ABZ-loaded SLNs. The nephrotoxicity effects were evaluated by biochemical and histopathological surveys. Results: Significantly different blood urea nitrogen (BUN) levels were observed between the two infected groups (ABZ treatment and ABZ-loaded SLN treatment) and the control group. The kidney malondialdehyde (MDA) and glutathione (GSH) levels of the infected groups were not significantly different from those of the control group. The histopathological study revealed nephropathic and pathologic changes in the ABZ and ABZ-loaded SLN groups. Conclusion: ABZ formulated for ABZ-loaded SLNs had a more prominent chemoprophylactic efficacy on CE and fewer side effects than ABZ alone. Neither ABZ nor ABZ-loaded SLNs caused significant biochemical and histopathological defects on the kidney, and all functional biochemical markers stayed within the normal range. Therefore, ABZ-loaded SLNs could be a potential new product for CE treatment.

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

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

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

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 Experimental Study on the Resistance of Synthetic Penicillin Solid Lipid Nanoparticles to Clinically Resistant Staphylococcus aureus

2021 ◽  
Vol 2021 ◽  
pp. 1-7
Author(s):  
Enliang Zhao ◽  
Tonghui Yi ◽  
Juan Du ◽  
Jing Wang ◽  
Shan Cong ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Particle Size ◽  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Lipid Nanoparticles ◽  
Inhibitory Effect ◽  
Polydispersity Index ◽  
Drug Resistant ◽  
Solid Lipid

Background. With the increasing resistance of antibiotics to bacteria, new and effective methods are needed to transform existing antibiotics to solve the problem of long development cycles for new drugs. The antibiotic nanodelivery system has proven to be a promising strategy. Aim. The purpose of this study is to synthesize penicillin solid lipid nanoparticles (penicillin SLNs) to enhance the antibacterial activity of penicillin against drug-resistant Staphylococcus aureus. Materials and Methods. Penicillin SLNs were synthesized. And particle size, the polydispersity index (PI), and zeta potential (ZP) of penicillin SLNs were measured. The surface morphology of penicillin SLNs was observed using a transmission electron microscope. Results. The particle size of penicillin SLNs is 112.3 ± 11.9   nm , the polydispersity index (PI) and zeta potential (ZP) of penicillin SLNs are 0.212 ± 0.03 and − 27.6 ± 5.5   mV . The encapsulation efficiency and drug loading were 98.31 ± 1.2 % and 4.98 ± 0.05 ( % w / w ), respectively. Penicillin SLNs had a more significant inhibitory effect on the growth of methicillin-sensitive Staphylococcus aureus (MSSA) after the drug and the bacteria were incubated for 12 hours. The number of MRSA colonies in the penicillin group increased after 12 hours, while the number of MRSA colonies in the penicillin SLNs group did not change significantly. Conclusion. Penicillin SLNs enhance the ability of penicillin to enter cells and increase the concentration of penicillin in the cell and also extend the residence time of penicillin in the cell. Our findings indicated that penicillin SLNs enhance the inhibitory effect of penicillin on drug-resistant Staphylococcus aureus.

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 Preparation, In Vitro characterization and stability studies of ropinirole lipid nanoparticles enriched hydrogel for treatment of neurodegeneration diseases

2021 ◽  
Vol 11 (2-S) ◽  
pp. 66-75
Author(s):  
Kumara Swamy Samanthula ◽  
Ramesh Alli ◽  
Thirupathi Gorre
Keyword(s):  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Nanostructured Lipid Carriers ◽  
Solid Lipid ◽  
Release Studies ◽  
Vitro Release

Ropinirole (RP), is a selective dopamine agonist that is used alone or with other medications to treat the symptoms of Parkinson’s disease (PD). RP has low bioavailability of only about 50% due to the first-pass metabolism, and it requires frequent dosing during oral administration. The objective of the current research was to develop RP loaded solid lipid nanoparticles (RP-SLNs), nanostructured lipid carriers (RP-NLCs), and their corresponding hydrogels (RP-SLN-C and RP-NLC-C) that might improve efficacy in PD treatment. RP nanoparticles were prepared by homogenization aided probe sonication method and optimized based on particle size, polydispersity index (PDI), zeta potential (ZP), assay, entrapment efficiency, and in vitro release studies. Optimized formulations were converted to hydrogel formulations using Carbopol 934 as a gelling polymer and optimized based on rheological and release characteristics. Optimized formulations were further evaluated using differential scanning calorimetry (DSC), powder X-ray diffractometry (PXRD), scanning electron microscopy (SEM), freeze-drying, and stability study at refrigerated and room temperatures. The optimized RP-SLN formulation showed particle size and entrapment efficiency of 213.5±3.8 nm and 77.9±3.1% compared to 190.6±3.7 nm and 85.7±1.7% for optimized RP-NLC formulation. PXRD supplemented and confirmed DSC results, RP was entrapped in a molecularly dispersed state inside the core of the lipid nanocarrier. Furthermore, RP loaded lipid nanocarriers revealed a spherical shape in SEM images. In vitro release studies demonstrated sustained release profiles for RP from SLNs, NLCs, and their hydrogels over 24 h and were stable over three months at 4ºC and 25ºC storage conditions. Keywords: Parkinson’s disease, Ropinirole, Solid lipid nanoparticles, Nanostructured lipid carriers, Hydrogel.

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