scholarly journals Development and Evaluation of Solid Lipid Nanoparticles of Raloxifene Hydrochloride for Enhanced Bioavailability

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Anand Kumar Kushwaha ◽  
Parameswara Rao Vuddanda ◽  
Priyanka Karunanidhi ◽  
Sanjay Kumar Singh ◽  
Sanjay Singh
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Aqueous Solubility ◽  
Lipid Nanoparticles ◽  
Dsc Studies ◽  
Solid Lipid ◽  
Raloxifene Hydrochloride ◽  
Dialysis Bag

Raloxifene hydrochloride (RL-HCL) is an orally selective estrogen receptor modulator (SERM) with poor bioavailability of nearly 2% due to its poor aqueous solubility and extensive first pass metabolism. In order to improve the oral bioavailability of raloxifene, raloxifene loaded solid lipid nanoparticles (SLN) have been developed using Compritol 888 ATO as lipid carrier and Pluronic F68 as surfactant. Raloxifene loaded SLN were prepared by solvent emulsification/evaporation method, and different concentrations of surfactant, and homogenization speed were taken as process variables for optimization. SLN were characterized for particle size, zeta potential, entrapment efficiency, surface morphology, and crystallinity of lipid and drug.In vitrodrug release studies were performed in phosphate buffer of pH 6.8 using dialysis bag diffusion technique. Particle sizes of all the formulations were in the range of 250 to 1406 nm, and the entrapment efficiency ranges from 55 to 66%. FTIR and DSC studies indicated no interaction between drug and lipid, and the XRD spectrum showed that RL-HCL is in amorphous form in the formulation.In vitrorelease profiles were biphasic in nature and followed Higuchi model of release kinetics. Pharmacokinetics of raloxifene loaded solid lipid nanoparticles after oral administration to Wistar rats was studied. Bioavailability of RL-HCL loaded SLN was nearly five times than that of pure RL-HCL.

Development and In Vitro Characterization of Solid Lipid Nanoparticles(SLN) Containing Methotrexate And Doxycycline

2018 ◽  
Vol 8 (3) ◽  
Author(s):  
Vijaya R ◽  
Ram Kishan K R
Keyword(s):  
Sustained Release ◽  
Solid Lipid Nanoparticles ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
X Ray Diffraction ◽  
Solid Lipid ◽  
Inflammatory Conditions ◽  
In Vitro Characterization ◽  
Dialysis Bag

Solid lipid nanoparticles (SLN) containing Disease Modifying Antirheumatic drugs (DMARDs) Methotrexate (MTX) and Doxycycline (DOX) was developed using a triglyceride (tristearin) and a polaxamer (pluronic F68). Hot homogenization of melted lipid and aqueous phase at temperature above the melting point of lipid had produced SLN dispersion. Optimization of process and formulation variables have yielded SLN having an entrapment efficiency of 65.07%±1.23% and 79.56%±0.92% for MTX and DOX respectively. Particle size and zeta potential measured using Malvern Zetasizer showed 157.2nm and -9.6mv respectively for the optimized SLN formulation. The compatibility between the drug and the formulation excipients was tested by Fourier Transform Infrared Spectroscopy (FTIR) and found to be compatible. Powder X-ray diffraction (PXRD) study revealed that the drugs and lipid were dispersed in crystalline state in SLN. The in vitro drug release studies performed in phosphate buffer of pH 7.4 using dialysis bag showed a sustained release of both the drugs (andgt;75%±1.4%) up to a period of two days. From the in vitro results, it can be concluded that SLN was found to be a suitable nano carrier for the incorporation of DMARDS: MTX and DOX without any significant interaction. The developed system produced sustained release of both the drugs (based on their concentration) for longer duration and thus suitable for the chronic inflammatory conditions of RA.

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. 

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 Formulation and evaluation of in-situ gels enriched with Tropicamide loaded solid lipid nanoparticles

2018 ◽  
Vol 9 (1) ◽  
pp. 216
Author(s):  
Jayachandra Reddy Peddappi Reddigari ◽  
Yerikala Ramesh ◽  
Chandrasekhar B. Kothapalli
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Research Work ◽  
Particle Morphology ◽  
Entrapment Efficiency ◽  
Adhesive Force ◽  
Lipid Nanoparticles ◽  
Solid Lipid ◽  
Diffusion Studies

The present research work “Formulation and Evaluation of In-situ gels enriched with Tropicamide loaded solid lipid nanoparticles”. To overcome the problems of side effects and to increase the bioavailability of tropicamide loaded solid lipid nanoparticles are containing with suitable lipids (glycerin trimyristate, Tristearin, Phosphatidylcholine & soyabean lecithin) with stabilizers (poloxamer 188) and surfactant like polysorbate 80. The interaction between drug, lipids & polymer by performing with FTIR no incompatibility with each other. The particle morphology was carried out by SEM & AFM in solid lipid nanoparticle formulation. The particle size was ranges from 213.6 ± 2.16nm to 538.0 ± 6.53 nm. The zeta potential ranges form -18.3mV to 25.6mV. The entrapment efficiency of free tropicamide was ranges from 74.13 % to 90.17%. The drug content was ranges from 0.212mg/ml to 0.912mg/ml. The SLN formulations must be transparent white colour and semi solid consistency. The pH 7.0 to 8.0 in all formulation. The gelling strength of gels TSLNGF1 to TSLNGF12 was ranges from 72 ± 1 sec to 117 ± 2 sec. The bio adhesive force was ranges from 10.12 ±1.01 dynes/cm2 to 23.12 ± 1.91 dynes/cm2. The viscosity of prepared formulation ranges from 415 ± 1.94 cps to 652 ± 1.41 cps. The spread ability studies of all formulation were ranges from 09 gms/sec to 18 gms/sec. The Accelerated stability the formulations does not undergo any chemical Changes. In vitro Franz’s diffusion studies of SLN enriched in gels TSLNGF1 to TSLNGF12 among the various formulation best formulations was TSLNGF6; its follows first order kinetics. Keywords: Solid Lipid Nanoparticles; Tropicamide; In- situ gels; In vitro diffusion studies

Preparation, Characterization and Optimization of Irbesartan Loaded Solid Lipid Nanoparticles for Oral Delivery

2021 ◽  
pp. 97-104
Author(s):  
Kumara Swamy S ◽  
Ramesh Alli
Keyword(s):  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Oral Delivery ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Sustained Drug Release ◽  
Bioavailability Enhancement ◽  
Solid Lipid

The purpose of this study was to develop and evaluate irbesartan (IS) loaded solid lipid nanoparticles (SLNs; IS-SLNs) that might enhance the oral bioavailability of IS. IS, an angiotensin-receptor antagonist, used to treat hypertension. However, poor aqueous solubility and poor oral bioavailability has limited therapeutic applications of IS. Components of the SLNs include either of trimyristin/tripalmitin/tristearin/trilaurate/stearic acid/beeswax, and surfactants (Poloxamer 188 and soylecithin). The IS-SLNs were prepared by hot homogenization followed by ultrasonication method and evaluated for particle size, poly dispersity index (PDI), zeta potential (ZP), entrapment efficiency (EE), drug content and in vitro drug release. The physical stability of optimized formulation was studied at refrigerated and room temperature for two months. The optimized IS-SLN formulation (F4) had a mean diameter of about 217.6±3.62 nm, PDI of 0.163±0.032, ZP of -28.5±4.12, assay of 99.8±0.51 and EE of 93.68±2.47%. The formulation showed sustained drug release compared with control formulation over 24 h. Optimized formulation was found to be stable over two months. IS-SLN showed nearly spherical in shape using and converted to amorphous form by DSC. Thus, the results conclusively demonstrated SLNs could be considered as an alternative delivery system for the oral bioavailability enhancement of IS.

scholarly journals Formulation and Evaluation of Solid Lipid Nanoparticles of Bifonazole

2020 ◽  
pp. 105-120
Author(s):  
Botre P.P ◽  
Maniyar M.G.
Keyword(s):  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Fungal Infections ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Gelling Agent ◽  
Rheological Parameters ◽  
Scanning Calorimetry ◽  
Solid Lipid

The objective of this study was to develop suitable solid lipid nanoparticles for topical delivery of Bifonazole. Bifonazole is an imidazole antifungal drug used in form of ointments. It was patented in 1974 and approved for medical use in 1983. Bifonazole having broad spectrum activity against dermatophytes, moulds, yeasts, fungi and some gram positive bacteria. BFZ SLNs systems were developed by melt emulsification followed by solvent evaporation technique using Compritol 888ATO (Glyceryl behenate) as a solid lipid and Tween 80 as a surfactant. Developed SLNs were evaluated for particle size, polydispersity index (PI), entrapment efficiency (EE) and drug release profiles. Process and formulation parameters were optimized. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) studies were carried out on SLNs to mark the changes in the drug and lipid modifications. The BFZ SLNs based gels were prepared using Carbopol 940 as a gelling agent. The SLNs based gels were evaluated for rheological parameters, in vitro drug release and permeation studies. In vitro antifungal study suggested that the SLNs based gel was more effective in inhibiting growth of Candida albicans. Thus the study concludes that SLNs based gel of BFZ gives a sustained release profile of BFZ and has the potential for treatment of topical fungal infections.

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 Preparation, Characterization and Evaluation of Elvitegravir-Loaded Solid Lipid Nanoparticles for Enhanced Solubility and Dissolution Rate

2015 ◽  
Vol 14 (9) ◽  
pp. 1549-1556
Author(s):  
P Kommavarapu ◽  
A Maruthapillai ◽  
K Palanisamy
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
Solid Lipid Nanoparticles ◽  
Entrapment Efficiency ◽  
Aqueous Solubility ◽  
Lipid Nanoparticles ◽  
Solvent Injection ◽  
Injection Method ◽  
Solid Lipid ◽  
Enhanced Solubility

Purpose: To enhance the aqueous solubility and dissolution rate of elvitegravir (EVG) by formulating the drug as solid lipid nanoparticles (SLNs) using solvent injection method.Methods: EVG-loaded SLNs were prepared by solvent injection method. Four different formulations of SLN were prepared using gelucire - 44/14 as lipid core in ethanol, soya lecithin as emulsifier, and polysorbate 80 as surfactant in the aqueous phase. The SLNs were characterized for various physical properties, including particle size, zeta potential, polydispersity, release profile and entrapment efficiency.Results: The yield of SLNs was in the range 151.0 ± 2.4 to 199.1 ± 2.7 nm. Significant changes were observed in mean particle size (nm), Z - potential (mV) and polydispersity index (PDI) of the SLNs by varying the  concentration of cryoprotectant. EVG – SLNs demonstrated a 800 – 1030-fold enhancement in aqueous solubility compared with plain EVG. The dissolution efficiency (DE) for SLNs was > 63 % in all cases and increased up to 83 % with increasing lipid load.Conclusion: Successful preparation and characterization of elvitegravir–loaded solid lipid nanoparticles by solvent injection method has been accomplished in this study.Keywords: Elvitegravir, Solid lipid nanoparticles, Cryoprotectant, Lipid load, Entrapment efficiency

scholarly journals Formulation and In-Vitro Evaluation of Solid Lipid Nanoparticles Containing Levosulpiride

2017 ◽  
Vol 4 (1) ◽  
pp. 17-29 ◽  
Author(s):  
Sukhwinder Singh ◽  
Sukhmeet Singh Kamal ◽  
Amit Sharma ◽  
Daljit Kaur ◽  
Manoj Kumar Katual ◽  
...  
Keyword(s):  
Drug Release ◽  
Stearic Acid ◽  
Calibration Curve ◽  
Solid Lipid Nanoparticles ◽  
Release Kinetics ◽  
Lipid Nanoparticles ◽  
Lipid Phase ◽  
Solid Lipid ◽  
Bioavailable Fraction

Objectives: The present study aims on preparing Levosulpiride loaded solid lipid nanoparticles (SLNs) to reduce the dose, frequency of dosing, reduce side effects and to increase the bioavailable fraction of drug (<30% orally in general). Methods: Levosulpiride was characterized by preformulation studies like physical appearance, melting point, assay, calibration curve, FTIR analysis and DSC analysis. The calibration curve of the drug was prepared in pH 6.8 phosphate buffer. Two lipids (Stearic acid and Palmitic acid) were used as lipid phase to prepare SLNs. Factorial design (23) was applied to formulate 16 formulations (8 for each lipid i.e. SF1-SF8 and PF1-PF8). Levosulpiride SLNs were prepared by solvent evaporation method followed by homogenization. Results: The optimized formulations were characterized by particle size analysis, zeta potential analysis, in vitro drug release and drug release kinetics. Drug-excipient interaction in optimized formulation was characterized by FTIR, DSC and TEM analysis. Conclusion: On the basis of evaluation parameters, the formulation SF1 (containing Stearic acid) and PF1 (containing Palimitic acid) found to be better formulations amongst their groups with a controlled drug release after a period of 24 hrs.

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