Nanostructured lipid carriers (NLC) based controlled release topical gel of clobetasol propionate: design and in vivo characterization

Abstract

Nanostructured lipid carrier (NLC)-based gel was developed as a potential topical system for clobetasol propionate (CP) topical delivery for the treatment of eczema. The characterizations of the prepared NLC formulation for topical application on the skin were assessed by means of morphology (SEM), particle size distribution, zeta potential analysis, drug entrapment efficiency, and in vitro drug release studies to select the optimized NLC formulation. The optimized NLC formulation encompasses particle size of 137.9 nm with -20.5 mV zeta potential and 0.224 polydispersity index which indicates good stability of NLC dispersion. NLC formulation showed a good entrapment efficiency of 78.5 % ± 0.03 with cumulative in vitro release 85.42 % up to 24 h. The optimized NLC formulation was suitably gelled and characterized for rheology, drug content, ex vivo drug permeation studies, and drug release kinetics studies. The permeation study revealed that the permeability parameters like steady-state flux (Jss), permeability coefficient (Kp), and enhancement ratio were significantly higher for NLC-based gel formulation as compared to marketed formulation of clobetasol propionate. The value of r (2) (Korsmeyer-Peppas equation) indicated good linearity showing anomalous (non-Fickian) diffusion viz. drug release is controlled by more than one process, i.e., superposition of both phenomenon, the diffusion controlled as well as swelling controlled release. The anti-inflammatory activity of NLC gel via paw oedema technique showed a rapid onset of action, as well as a prolonged duration of action as compared with the marketed gel.

Encapsulation of Oleuropein in Nanostructured Lipid Carriers: Biocompatibility and Antioxidant Efficacy in Lung Epithelial Cells

“…In this work, Korsmeyer-Peppas showed the highest r 2 for all nanoparticle formulations with r 2 = 0.977 (NLC-OLE30), r 2 = 0.998 (NLC-OLE40), and r 2 = 0.999 (NLC-OLE50), respectively. This type of release has been reported before for some nanostructured lipid carriers [59][60][61]. In addition, the diffusional exponent 'n' of the Korsmeyer-Peppas model also described the OLE release mechanism, which in this case was in the range 0.46 to 0.59, indicating that OLE was released by an anomalous transport mechanism [58].…”

<p>Use of transethosomes for enhancing the transdermal delivery of olmesartan medoxomil: in vitro, ex vivo, and in vivo evaluation</p>

“…On the other hand, nonionic SAAs have more profound effect on extending the diffuse layer which generates lower ZP while anionic SAAs are held up more tightly around the particle and consequently have lesser effect on the thickness of the diffuse layer, retaining higher ZP values. 49 With respect to PC:SAA ratio (X 2 ), vesicles with the greatest amount of PC exhibited the highest ZP. Although PC heads are zwitterionic and thus theoretically uncharged at neutral pH, they give rise to negative ZP value in water.…”

Development and Characterization of Precirol Ato 88 Base in Nanostructured Lipid Carriers (Nlc) Formulation With the Probe Sonication Method

“…Campervan surfactant with a water phase using magnetic-stirrer (IKA® C-Mag H54) (Phase B). Phase B is added to phase A, then stirred using a high-shear homogenizer (Ultra Thurrax IKA® T25) to form pre-emulsions [17][18][19] step is to reduce particle size using a sonicator probe (Ivymen Ultrasonic Homogenizers CY-500) [20].…”