Single-step and low-energy method to prepare solid lipid nanoparticles and nanostructured lipid carriers using biocompatible solvents
Abhijit A. Date, Mangal S. Nagarsenker ✽
Eur. J. Pharm. Res., Volume 1, Issue 1, pp. 12-19 (2019) Available online March 13rd 2019
Abstract:
Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLCs) are widely being explored for improving dermal/transdermal and oral delivery of drugs, neutraceuticals and cosmeceuticals. High-pressure homogenization (HPH) is the most commonly used preparation method for SLN/NLCs. SLN/NLCs preparation by the HPH requires high energy input and longer duration. Here, we describe a simple yet innovative low-energy method to prepare SLN/NLCs in a single-step using biocompatible solvents. We first show that biocompatible solvents such as Transcutol P, Soluphor P, N-methyl pyrrolidone, and glycofurol can solubilize glyceryl monostearate, glyceryl behenate, and glyceryl distearate to a variable degree. Our pre-formulation studies showed that only GMS could be transformed into SLN or NLCs despite high solubility of the lipids investigated indicating the importance of solvent-lipid interaction parameter in our preparation method. Finally, we show that SLN and NLCs of glyceryl monostearate with size < 150 nm and acceptable polydispersity index can be easily developed using Transcutol P as a biocompatible solvent and polyoxyl-40-stearate (MYS-40) as a stabilizer. As the Transcutol P has excellent acceptability for dermal/transdermal and oral route, there is no need to remove the residual Transcutol P (5% v/v) from the prepared glyceryl monostearate SLN/NLCs. Thus, our method offers a simple yet innovative way to prepare GMS SLN/NLCs suitable for dermal/transdermal and oral applications.