Abstract
Non-steroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen (IBP) are among the most prescribed drugs across the globe. However, most NSAIDs are insoluble in water leading them to have poor bioavailability and erratic absorption. Moreover, NSAIDs such as IBP and ketoprofen (KP) have to be administered very frequently due to their short plasma half-life leading to side effects. Controlled release formulations of IBP, KP and nabumetone (NBT) based on solid lipid nanoparticles (SLNs) were successfully synthesised in the present study to solve the above-mentioned challenges that are associated with NSAIDs. SLNs were prepared in two steps; hot-melt homogenization followed by sonication to formulate SLNs with spherical morphology. While capmul® GMS-50K (capmul) was used as the lipid due to the high solubility of the studied drugs in it, gelucire® 50/13 (gelucire) was used as the surfactant. It was found that particle size was directly proportional to drug concentration and inversely proportional to surfactant concentration, volume of water added and temperature of water. Ultrasonication in a pulse mode with optimum duration of 15 min was essential to obtain smaller nanoparticles through the formation of a nanoemulsion. Drug loaded SLNs with small particle size and narrow size distribution with good solid loading, encapsulation efficiency and drug loading percentage could be prepared using the optimised conditions. SLNs prepared at the optimised condition were characterized thoroughly by using different techniques such as dynamic light scattering (DLS), field emission scanning electron microscopy (FESEM), transmission electron microscopy (TEM), atomic force microscopy (AFM), X-ray diffraction (XRD), differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). The cytotoxicity results showed that the prepared SLNs are non-toxic to Raw cell line. The drugs IBP, KP and NBT showed 53, 74 and 69% of percentage entrapment efficiency with drug loading of 6, 2 and 7% respectively. Slow, steady and sustained drug release was observed from the SLNs for over 6 days.
| Original language | English |
|---|---|
| Pages (from-to) | 686-696 |
| Number of pages | 11 |
| Journal | Ultrasonics Sonochemistry |
| Volume | 40 |
| DOIs | |
| State | Published - Jan 2018 |
Bibliographical note
Funding Information:Thanks are due to IIT Mandi for providing laboratory facilities. Financial assistance from ARMREB, DRDO (ARMREB/CDSW/2012/149) and research fellowship to Mr. Raj Kumar and Mr. Ashutosh Singh from UGC are gratefully acknowledged. Dr. Neha Garg acknowledges the financial support from Department of Science and Technology , India under INSPIRE faculty scheme ( DST/INSPIRE/04/2015/000958 ). Assistance from Dr. Sacheen Kumar and Dr. Jaspreet Kaur Randhawa in nanoemulsion preparation is also acknowledged here by.
Publisher Copyright:
© 2017
Keywords
- Controlled drug release
- Dissolution rate
- NSAIDs
- Nanoemulsions
- Solid lipid nanoparticles