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.

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. 

Preliminary studies on optimization of anti-parkinson drug loaded lipid nanoparticles enriched hydrogel formulations for management of Parkinson’s disease

2021 ◽  
Vol 11 ◽  
Author(s):  
Kumara Swamy ◽  
Ramesh Alli ◽  
Thirupathi Gorre
Keyword(s):  
Parkinson’S Disease ◽  
Particle Size ◽  
Parkinson's Disease ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Release Studies ◽  
Lipid Nanocarriers ◽  
Vitro Release

Purpose: 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. Aim: 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 could enhance RP therapeutic outcomes during PD treatment. Methods: RP nanoparticles were prepared by homogenization followed by probe sonication 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. Results: 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. Optimized SLN, NLC, and nanocarrier loaded hydrogel formulations were stable over three months at 4ºC and 25ºC storage conditions. Conclusion: Overall, the results demonstrated that lipid nanocarriers and their corresponding hydrogel formulations can be considered as a topical drug delivery vehicle for RP during the treatment of PD.

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.

scholarly journals Effect of Lipids on Physicochemical Properties of Letrozole Loaded Solid Lipid Nanoparticles

2016 ◽  
Vol 8 (05) ◽  
Author(s):  
Archana Nerella ◽  
Basava Dontamsetti ◽  
Aruna Mantena
Keyword(s):  
Particle Size ◽  
Physicochemical Properties ◽  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Physicochemical Characteristics ◽  
Lipid Nanoparticles ◽  
Solid Lipid ◽  
Stabilizer Concentration ◽  
Vitro Release

The objective of the current investigation was to prepare solid lipid nanoparticles (SLNs) from different lipids and to study the effect of lipids on physicochemical characteristics of letrozole loaded SLN. In order to prepare small, stable, uniform and high Letrozole loaded SLNs, many factors such as lipid and stabilizer concentration and preparation parameters can be considered. Out of these, we have selected solid lipid as lipid matrix to investigate an effect on SLNs. SLNs were prepared using different lipids by modified hot sonication method. The effect of different lipids and stabilizers on physicochemical characteristics of Letrozole loaded SLNs were investigated. Letrozole loaded SLNs showed different physicochemical properties and release profiles according to used solid lipid. In case of particle size, SLN1 showed biggest particle size (532.5 ± 26.4nm) and highest encapsulation efficiency (81.37 ± 6.72%) and, SLN4 showed highest cumulative drug percentage (89.4 ± 1.8%, 24 h) release. These results suggest that lipids type affect physicochemical properties and release profile of SLN. The choice of lipid and stabilizer played important role on the physicochemical characteristics and in vitro release of Letrozole loaded SLNs.

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

Enhanced Oral Absorption of All-trans Retinoic Acid upon Encapsulation in Solid Lipid Nanoparticles

2020 ◽  
Vol 8 (6) ◽  
pp. 495-510
Author(s):  
Manoj Kumar ◽  
Garima Sharma ◽  
Dinesh Singla ◽  
Sukhjeet Singh ◽  
Vandita Kakkar ◽  
...  
Keyword(s):  
Retinoic Acid ◽  
Side Effects ◽  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Lipid Nanoparticles ◽  
Solid Lipid ◽  
Trans Retinoic Acid ◽  
All Trans Retinoic Acid ◽  
Vitro Release

Background:: All-trans retinoic acid (ATRA) is widely employed in the treatment of various proliferative and inflammatory diseases. However, its therapeutic efficacy is imperiled due to its poor solubility and stability. Latter was surmounted by its incorporation into a solid matrix of lipidic nanoparticles (SLNs). Methods:: ATRA loaded SLNs (ATRA-SLNs) were prepared using a novel microemulsification technique (USPTO 9907758) and an optimal composition and were characterized in terms of morphology, differential scanning calorimetry (DSC), and powder X-ray diffraction studies (PXRD). In vitro release, oral plasma pharmacokinetics (in rats) and stability studies were also done. Results:: Rod-shaped ATRA-SLNs could successfully incorporate 3.7 mg/mL of ATRA, increasing its solubility (from 4.7 μg/mL) by 787 times, having an average particle size of 131.30 ± 5.0 nm and polydispersibility of 0.283. PXRD, DSC, and FTIR studies confirmed the formation of SLNs. Assay/total drug content and entrapment efficiency of ATRA-SLNs was 92.50 ± 2.10% and 84.60 ± 3.20% (n=6), respectively, which was maintained even on storage for one year under refrigerated conditions as an aqueous dispersion. In vitro release in 0.01 M phosphate buffer (pH 7.4) with 3% tween 80 was extended 12 times from 2h for free ATRA to 24 h for ATRA-SLNs depicting Korsmeyer Peppas release. Oral administration in rats showed 35.03 times enhanced bioavailability for ATRA-SLNs. Conclusion:: Present work reports preparation and evaluation of bioenhanced ATRA-SLNs containing a high concentration of ATRA (>15 times than that reported by others). Latter is attributed to the novel preparation process and intelligent selection of components. Lay Summary: All-trans retinoic acid (ATRA) shows an array of pharmacological activities but its efficacy is limited due to poor solubility, stability and side effects. In present study its solubility and efficacy is improved by 787 and 35.5 times, respectively upon incorporation into solid lipid nanoparticles (ATRA-SLNs). Latter extended its release by 12 times and provided stability for at least a year under refrigeration. A controlled and sustained release will reduce dose related side effects. ATRA-SLNs reported presently can thus be used in treatment /prophylaxis of disorders like cancers, tuberculosis, age related macular degeneration and acne and as an immune-booster.

Development and In Vitro Characterization of Paclitaxel Loaded Solid Lipid Nanoparticles

2019 ◽  
Vol 9 (1) ◽  
pp. 76-85 ◽  
Author(s):  
R. Nithya ◽  
K. Siram ◽  
R. Hariprasad ◽  
H. Rahman
Keyword(s):  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Lipid Nanoparticles ◽  
Release Profile ◽  
Mcf7 Cells ◽  
Solid Lipid ◽  
Cancerous Cells ◽  
Vitro Release

Background: Paclitaxel (PTX) is a potent anticancer drug which is highly effective against several cancers. Solid lipid nanoparticles (SLNs) loaded with anticancer drugs can enhance its toxicity against tumor cells at low concentrations. Objective: To develop and characterize SLNs of PTX (PSLN) to enhance its toxicity against cancerous cells. Method: The solubility of PTX was screened in various lipids. Solid lipid nanoparticles of PTX (PSLN) were developed by hot homogenization method using Cutina HR and Gelucire 44/14 as lipid carriers and Solutol HS 15 as a surfactant. PSLNs were characterized for size, morphology, zeta potential, entrapment efficiency, physical state of the drug and in vitro release profile in 7.4 pH phosphate buffer saline (PBS). The ability of PTX to enhance toxicity towards cancerous cells was tested by performing cytoxicity assay in MCF7 cell line. Results: Solubility studies of PTX in lipids indicated better solubility when Cutina HR and Gelucire 44/14 were used. PSLNs were found to possess a neutral zeta potential with a size range of 155.4 ± 10.7 nm to 641.9 ± 4.2 nm. In vitro release studies showed a sustained release profile for PSLN over a period of 48 hours. SLNs loaded with PTX were found to be more toxic in killing MCF7 cells at a lower concentration than the free PTX.

scholarly journals Development of nitazoxanide-loaded colon-targeted formulation for intestinal parasitic infections: centre composite design-based optimization and characterization

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Charu Bharti ◽  
Upendra Nagaich ◽  
Jaya Pandey ◽  
Suman Jain ◽  
Neha Jain
Keyword(s):  
Particle Size ◽  
Desirability Function ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
Percentage Yield ◽  
Vitro Release ◽  
Selection Of

Abstract Background The current investigation is focused on the development and characterization of Eudragit S100 coated nitazoxanide-loaded microbeads as colon-targeted system utilizing central composite design (CCD) and desirability function. The study initiated with the selection of a BCS class II drug nitazoxanide and its preformulation screening with excipients, selection of polymer and identification of concentration for CCD, selection of optimized formulation based on desirability function, and in vitro release studies in simulated gastric and colonic media and stability studies. A two-factor, three-level CCD was employed with two independent variables, i.e. X1 (chitosan % w/v) and X2 (sodium tripolyphosphate % w/v), and three dependent variables, i.e. Y1 (particle size in micrometres), Y2 (percentage yield) and Y3 (percent entrapment efficiency), were chosen. Additionally, surface morphology, mucoadhesion and in vitro drug release studies were also conducted. Result Chitosan concentration showing maximum entrapment and optimum particle size was selected to formulate chitosan beads. The polynomial equation and model graphs obtained from the Design-Expert were utilized to examine the effect of independent variables on responses. The effect of formulation composition was found to be significant (p ˂ 0.05). Based on the desirability function, the optimized formulation was found to have 910.14 μm ± 1.03 particle size, 91.84% ± 0.64 percentage yield and 84.75% ± 0.38 entrapment efficiency with a desirability of 0.961. Furthermore, the formulations were characterized for in vitro drug release in simulated colonic media (2% rat caecal content) and have shown a sustained release of ∼ 92% up to 24 h as compared to in vitro release in simulated gastric fluid. Conclusion The possibility of formulation in enhancing percentage yield and entrapment efficiency of nitazoxanide and the utilization of CCD helps to effectively integrate nitazoxanide microbeads into a potential pharmaceutical dosage form for sustained release.

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