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International Journal of Pharmaceutical and Applied Sciences/1 (1)/2010 Advances In Novel Drug Delivery Carriers: Formulation And In
Vitro Evaluation of Solid Lipid Nanoparticles of Nateglinide
P. Khemariya1*, A. Jain2, R. Goswami3, M. Bhargava4,
S. Goswami4 ,S. K. Singhal4, M. Nagar4
2Dept. of Pharmaceutical Science, Dr. H.S.Gour University Sagar, MP. 3Sardar Patel University, Anand, Gujrat.
*Corresponding Author email: tinku_pharma@yahoo.co.in
Abstract:
1. Introduction:
The development of new chemical entities is expensive, time consuming and unspecified investigation was to formulative study for the in action1,2. Therefore more attention is being paid in the development of novel drug delivery carriers that can be used to improve for Nateglinide.Method and characterization- molecule3,4. So, current research in drug Solid lipid nanoparticles (SLNPs) based on therapeutic efficacy of drug5 and minimizing morphology, zeta potential, particle size, and delivery science7. It offers a suitable means drug release. Morphology and dimensional of delivering small molecular weight drugs as well as macromolecules such as proteins, electron microscopy and Photon Correlation peptides, or genes by either localized or demonstrate that SLNPs exhibit no toxicity. Spherical SLNPs with an average particle formulating suitable dosage forms which are size of ~173 nm were formulated. Delivery biocompatible, and reduce dosing frequency significantly higher accumulation by the endothelial cell monolayer as compared to the drug in aqueous solution. In vitro release is having particles ranging from 50-400 nm demonstrated that Nateglinide was released in a prolonged fashion for 24 h. Both free Potency, no use of organic solvents, suitable spent on the blocks in the bar test, although delivery and use of biodegradable lipids are the action of encapsulated Nateglinide was more rapid in onset and prolonged than free drug. These data suggest that SLNPs would Keywords: Solid lipid nanoparticles, Nategli
diffusion, water-in oil- in-water (w/o/w) double-emulsion method, high speed stirring International Journal of Pharmaceutical and Applied Sciences/1 (1)/2010 situation in which the human body either definite time this resulted in the formation of lipid suspension This mixture was further specified time period to obtain definite I and Type II16.Type I – condition when body fail to produce sufficient insulin. Type II - were formed and free drug was removed by condition when body doesn’t use the Insulin or by insulin resistance. Nateglinide is a anti- diabetic drug used to lower blood sugar in Charecterization
patients with type 2 diabetes mellitus. It is Particle size measurement
diabetes. It is also helpful for stimulation of Nateglinide is available in 60mg & 120mg frequency, leser side effect and increased stationary angle of 90 and fixed temperature at 25°C. The aqueous SLN dispersions were 2. Materials and Methods:
Transmission Electron microscopy
microscope (Philips, CM 200, acceleration voltage 200kV, resolution 0.23 nm). Fig-I (MWCO 10-12kD) was purchased from
Himedia, Mumbai, India. All other reagents
and solvents were of analytical grade and
were purchased from local suppliers unless
stated otherwise. Deionized water was used
throughout the study. All ingredients were
used as analytical grade.

3. Method of preparation:

The solvent injection method reported by
Stevens et al., (2004) was used to prepare
SLNPs. The lipid tristearin, soya lecithin &
drug nataglenide were dissolved in ethanol Fig: 1 TEM of Nateglinide Loaded SLNPs
maintained in another water bath. Alcoholic solution of lipid & drug was added as small Zeta potential measurement
surfactant solution and the whole mixture To find out the average particle charge Zeta was stirred using a mechanical stirrer (Remi Instrument, India) for specified time at specified speed of rotation. Stirring for kept stationary at 25°C. Before measuring, each sample of solid Lipid nanoparticles was International Journal of Pharmaceutical and Applied Sciences/1 (1)/2010 intervals samples were analyzed for drug content by measuring absorbance at 210 nm was performed at least four times. The pH Spectrophotometer (Shimadzu,1600 Japan). Differential scanning calorimetry22
in Table1,and graphically shown in fig.3 Differential Scanning Calorimetry (DSC) was performed with a Mettler DSC 822e (Mettler Toledo, Greifensee, Switzerland). S.No. Time (in hrs.) % Drug release Samples containing cooling rate of 5°C/min. The samples were further cooled from 85 to 25°C under liquid Table 1: In vitro % Drug Release
nitrogen. Enthalpies were calculated using
Fig: 3 % Drug release
Fig: 2 DSC of Nateglinide Loaded SLNPs
Drug loading Capacity
4. Results:
nanoparticles was performed by dissolving Transmission Electron microscopy
methanol and analyzing obtained solution by Solid lipid Nanoparticles (SLNPs) are the carriers which are attracting major attention as novel colloidal drug carriers for topical Drug Release
10 mL of optimized SLNPs formulation free Differential scanning calorimetery
from any unentrapped drug was taken in the cooling scan is the most common technique. maintained at 37±1°C throughout the study. peak at 55.2°C which can be attributed to International Journal of Pharmaceutical and Applied Sciences/1 (1)/2010 Average diameter and zeta potential
Richardson, J. Salsman, D.Top, R. Antueno, allows predictions about the storage stability of colloidal dispersion. In general, particle [7] J.I. MacGregor and V.C. Jordan, Basic charged particles (high zeta potential) due to electric repulsion. The mean zeta potential method had gained a relatively good stability Mehnert, Solid Lipid Nanoparticles (SLN) for Drug Loading
controlled drug delivery-Drug release and By HPLC technique it was observed that 90- Drug Release
characterization. Int. J. Pharmacol., 4: 1-4, 5. Conclusion:
[10] F.Q Hu, S.P. Jiang, Y.Z. Du, H. Yuan, Solid lipid nanoparticles (SLNPs) as Drug carriers have unique characteristics that can nanostructured lipid carriers, Int. J Pharm., enhance performance in a variety of dosage other colloidal or polymeric material due to [11] S.K. Katiyar, F. Afaq, K. Azizuddin, the higher drug incorporation and improved Toxicology and Appl. Pharm. Vol. 176, 110, 6. Acknowledgements:
Tyrrelll:FEBS Letters. Vol. 439, 253, (1998). [13] R.H. Muller, K. Mader, S. Gohla, Eur. J. 7. References:
[14] R. Lander, W. Manger, M. Scouloudis, [1] R.H. Muller, K. Mader, S. Gohla, Eur. J. Pharm. Biopharm., 51, 161-177. (2000). [2] Mehnert and K. Mader, Adv. Drug.Del. [15] F.Q. Hu, S.P. Jiang, Y.Z. Du, H. Yuan, stearic acid nanostructured lipid carriers by [3] S.P.Vyas and R.K. Khar, Targeted and sunscreens: In vitro release and in vivo skin penetration. J. Control Release, 81: 225- International Journal of Pharmaceutical and Applied Sciences/1 (1)/2010 Mehnert, Solid Lipid Nanoparticles (SLN) for controlled drug delivery-Drug release and determination. Pharm. Pharmacol. Lett., 3: [23] F. Wan, J. You, Y. Sun, Z. Xing-Guo [18] S. Liedtke, S. Wissing, R.H. Müller and homogenization equipment on Preparation and evaluation in vitro, I. Int. J. nanodispersions characteristics. Int. J. Pharm., 196: 183-185, (2000). [19] A. Miglietta, R. Cavalli, C. Bocca, L. Gabriel and M.R. Gasco, Cellular uptake and cytotoxicity of Solid Lipid Nanospheres (SLN) incorporating doxorubicin or paclitaxel. Int. J. Pharm., 210: 61-67, (2000). [20] N. AL-Haj, A. Rasedee, Solid lipid nanoparticles preparation and characterization. Int. J. Pharmacol., 4: 1-4, (2008). [21] A. Lippacher, R.H. Muller and K. Mader, Semisolid SLN™ dispersions for topical application: Influence of formulation and production parameters on viscoelastic properties. Eur. J. Pharm. Biopharm., 53: 155-160, (2002)

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