Development and evaluation of nanostructured lipid carriers-based gel of isotretinoin

作者：Patwekar Shailesh L; Pedewad Snehal R^*; Gattani Surendra

来源：Particulate Science and Technology, 2018, 36(7): 832-843.

DOI：10.1080/02726351.2017.1305026

• Hot homogenization technique
• isotretinoin
• NLC
• photostabilty
• skin irritation

In the present work attempts have been made to prepare the nanostructured lipid carriers (NLC) gel, by using the poorly water-soluble drug isotretinoin (IT), which is preferably used in the case of acne. The four different formulations of IT-NLC (NLC 1-NLC 4) were prepared using solid and liquid lipid with Tween 80 in different ratios by the hot homogenization method. Properties of entrapment efficiency and drug release behavior were investigated for all formulations from this NLC 4 formulation and optimized. Evaluation of NLC 4 such as particle size, zeta potential, differential scanning calorimetry (DSC), scanning electron microscopy (SEM), transmission electron microscopy (TEM), x-ray diffraction (XRD), and photostabilty study was performed. The nanoparticles were suitably gelled and evaluated for drug content, pH, spreadability, extrudability, rheology, and drug release. Safety to gel was assessed using primary skin irritation studies. The formulated NLC 4 was spherical in shape, with average particle size 154.1nm, zeta potential -26.9mV, and entrapment efficiency 91.85%+/- 0.10%. The results showed that entrapment of IT into NLCs reduced its photo degradation. IT-NLC gel showed a faster onset of action and elicited prolonged activity. The IT-NLC gel was less irritating, which shows improving ability for skin tolerability and being a carrier for topical delivery.

• 出版日期2018