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.

Development of Solid Lipid Nanoparticles of Lamivudine for Brain Targeting

2009 ◽  
Vol 1 (1) ◽  
Author(s):  
Pravin Patil ◽  
Anil Sharma ◽  
Subhash Dadarwal ◽  
Vijay Sharma
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Rotation Speed ◽  
Lipid Nanoparticles ◽  
Brain Targeting ◽  
Brain Penetration ◽  
Solid Lipid ◽  
Diffusion Technique

The objective of present investigation was to enhance brain penetration of Lamivudine, one of the most widely used drugs for the treatment of AIDS. This was achieved through incorporating the drug into solid lipid nanoparticles (SLN) prepared by using emulsion solvent diffusion technique. The formulations were characterized for surface morphology, size and size distribution, percent drug entrapment and drug release. The optimum rotation speed, resulting into better drug entrapment and percent yield, was in the range of 1000-1250 r/min. In vitro cumulative % drug release from optimized SLN formulation was found 40-50 % in PBS (pH-7.4) and SGF (pH-1.2) respectively for 10 h. After 24 h more than 65 % of the drug was released from all formulations in both mediums meeting the requirement for drug delivery for prolong period of time.

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

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 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.

Methotrexate Loaded Solid Lipid Nanoparticles (SLN) for Effective Treatment of Carcinoma

2006 ◽  
Vol 6 (9) ◽  
pp. 2991-2995 ◽  
Author(s):  
K. Ruckmani ◽  
M. Sivakumar ◽  
P. A. Ganeshkumar
Keyword(s):  
Stearic Acid ◽  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Solid Lipid ◽  
Soya Lecithin ◽  
Release Drug ◽  
Antitumour Drugs ◽  
Sodium Taurodeoxycholate ◽  
Average Size

Solid Lipid Nanoparticles (SLN) containing Methotrexate (MTX), an anticancer drug for intravenous administration was formulated and characterized. The SLN dispersions with MTX, stearic acid, and soya lecithin in the ratio of 1:4:1, 1:4:1.5, and 1:4:2, sodium taurodeoxycholate and distilled water were prepared by micro emulsification solidification method. The results show that the prepared MTX-SLN particles (with MTX–Stearic acid–Soya lecithin—1:4:2) have an average size of 270 nm with 51.3% drug entrapment. The in vitro-release was attained up to 15th h. The pharmacokinetic studyreveals that the half-life and MRT of SLNs were higher than MTX solution. The life span of EAC (Ehrlich Ascite Carcinoma) bearing mice was increased when treated with MTX-SLNs (Methotrexate nanoparticles). These results clearly indicate that SLNs are a promising sustained release drug targeting system for lipophilic antitumour drugs.

Effect of Acyclovir Solid Lipid Nanoparticles for the Treatment of Herpes Simplex Virus (HSV) Infection in an Animal Model of HSV-1 Infection

2019 ◽  
Vol 7 (5) ◽  
pp. 389-403 ◽  
Author(s):  
Ritika Kondel ◽  
Nusrat Shafiq ◽  
Indu P. Kaur ◽  
Mini P. Singh ◽  
Avaneesh K. Pandey ◽  
...  
Keyword(s):  
Particle Size ◽  
Single Dose ◽  
Drug Release ◽  
Mouse Model ◽  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Proof Of Concept ◽  
In Vitro Drug Release ◽  
Solid Lipid

Background: Acyclovir use is limited by a high frequency of administration of five times a day and low bioavailability. This leads to poor patient compliance. Objectives: To overcome the problem of frequent dosing, we used nanotechnology platform to evaluate the proof of concept of substituting multiple daily doses of acyclovir with a single dose. Methods: Acyclovir was formulated as solid lipid nanoparticles (SLN). The nanoparticles were characterized for particle size, surface charge and morphology and in vitro drug release. The pharmacokinetic and pharmacodynamic of SLN acyclovir were compared with conventional acyclovir in a mouse model. Results: SLN showed drug loading of 90.22% with 67.44% encapsulation efficiency. Particle size was found to be of 131 ± 41.41 nm. In vitro drug release showed 100% release in SIF in 7 days. AUC0-∞ (119.43 ± 28.74 μg/ml h), AUMC0-∞ (14469 ± 4261.16 μg/ml h) and MRT (120.10 ± 9.21 h) were significantly higher for ACV SLN as compared to ACV AUC0-∞ (12.22 ± 2.47 μg/ml h), AUMC0-∞ (28.78 ± 30.16 μg/ml h) and MRT (2.07 ± 1.77 h), respectively (p<0.05). In mouse model, a single dose of ACV SLN was found to be equivalent to ACV administered as 400mg TID for 5 days in respect to lesion score and time of healing. Conclusion: The proof of concept of sustained-release acyclovir enabling administration as a single dose was thus demonstrated.

Sign in / Sign up

Export Citation Format

Share Document