Clobetasol propionate loaded nanostructured lipid carrier gel: formulation strategy and in vitro performance evaluation

Impact of liquid lipid on development and stability of trimyristin nanostructured lipid carriers for oral delivery of resveratrol

This work aims to develop nanostructured lipid carriers (NLCs) to improve the oral bioavailability of febuxostat (FEB). High shear homogenization, a well-known technique, followed by bath sonication with slight modifications was used to prepare FEB-loaded NLCs using oleic acid as liquid lipid and stearic acid as solid lipid. A total of 3² full factorial design was utilized to examine the effect of 2 independent variables, namely, X1 (liquid to solid lipid ratio) and X2 (surfactant concentration) on the Y1 (particle size) and Y2 (% entrapment efficiency) of the drug. The prepared NLCs were evaluated for particle size, polydispersity index, zeta potential, and (%) entrapment efficiency. The drug's highest solubility was found in the stearic (solid lipid) and oleic acid (liquid lipid), which were further chosen for NLC preparation. Result of the present study showed an increase in entrapment efficiency and a decrease in particle size with the increase in liquid lipid to solid lipid ratio. With increased surfactant concentration, a small particle size is observed. The optimized formulation's particle size and (%) entrapment efficiency was found to be 99 nm and 80%, respectively. The formulations' zeta potential and polydispersity index were found within the range. Compared to plain drug suspension, the optimized formulation showed higher drug release, which may be due to the presence of the higher amount of liquid lipid. The particles shown in the transmission electron microscopy were round in shape and have smooth surface. Stability studies showed that the NLC formulation can be stored for a longer time period under room condition. FEB-loaded NLC were successfully prepared using full 3² factorial design, and can be further used for oral delivery of FEB for gout treatment.

Objectives This work aims to develop nanostructured lipid carriers (NLCs) to improve the oral bioavailability of febuxostat (FEB). Materials and Methods High shear homogenization, a well-known technique, followed by bath sonication with slight modifications was used to prepare FEB-loaded NLCs using oleic acid as liquid lipid and stearic acid as solid lipid. A total of 3² full factorial design was utilized to examine the effect of 2 independent variables, namely, X1 (liquid to solid lipid ratio) and X2 (surfactant concentration) on the Y1 (particle size) and Y2 (% entrapment efficiency) of the drug. The prepared NLCs were evaluated for particle size, polydispersity index, zeta potential, and (%) entrapment efficiency. Results The drug's highest solubility was found in the stearic (solid lipid) and oleic acid (liquid lipid), which were further chosen for NLC preparation. Result of the present study showed an increase in entrapment efficiency and a decrease in particle size with the increase in liquid lipid to solid lipid ratio. With increased surfactant concentration, a small particle size is observed. The optimized formulation's particle size and (%) entrapment efficiency was found to be 99 nm and 80%, respectively. The formulations' zeta potential and polydispersity index were found within the range. Compared to plain drug suspension, the optimized formulation showed higher drug release, which may be due to the presence of the higher amount of liquid lipid. The particles shown in the transmission electron microscopy were round in shape and have smooth surface. Stability studies showed that the NLC formulation can be stored for a longer time period under room condition. Conclusion FEB-loaded NLC were successfully prepared using full 3² factorial design, and can be further used for oral delivery of FEB for gout treatment.

Nanostructured lipid carrier loaded with Zingiber officinale oil to enhance transdermal bioactive delivery for topical formulation

Nanostructured lipid carriers (NLCs) are lipid-based nanoparticles composed of a mixture of solid and liquid lipids, which are stabilized by the outer surface of a surfactant. This research aimed to prepare intranasal nanostructured lipid carriers loaded with amisulpride to enhance its dissolution and bioavailability using different formulation compositions. Amisulpride nanostructured lipid carriers were formulated using ultra-sonication methods. Solid lipids like stearic acid, palmitic acid, and glyceryl monostearate were used, while liquid lipids like oleic acid, Imwitor 988, and isopropyl myristate were employed. Surfactants used were cremophor®EL, tween 80, and span 20 with different co-surfactants: Transcutol HP, triacetin, and propylene glycol in different ratios. The key metrics used in this study's evaluation were particle size, polydispersity index, zeta potential, entrapment efficiency, and loading efficiency. The formulations with the best characteristics were also subjected to an in-vitro release test. The results showed a significant shift in some evaluation criteria with a non-significant change in other characterizations upon switching between different types and ratios of compositions. A biphasic release pattern was also observed. The optimum formula F19 was found to have 68.309±0.38 nm, 0.2408±0.004, -20.64±0.11 mV, 95.75±0.26 and 18.07±0.36, respectively. It was safe on the sheep nasal membrane. The right combination of the formulation compositions based on studying the effect of each factor on the main formulation characteristics can serve as the basis for a successful intranasal amisulpride-loaded nanostructured lipid carrier.

Nanostructured lipid carriers (NLCs) are lipid-based drug delivery systems made from a mix of liquid and solid lipids, stabilized by surfactants. Nyamplung (Calophyllum inophyllum L) oil, rich in oleic acid (48.49%), has shown in recent studies to enhance wound healing and dermatological performance when used in formulations like bigels and hydrogels. The present study aimed to formulate and characterize NLC system composed of solid lipids (cetyl palmitate and stearic acid) and a liquid lipid (nyamplung oil) for effective drug delivery. Six different NLC formulations (I-VI) were prepared by varying the concentrations of cetyl palmitate, stearic acid, and nyamplung oil. The NLC formulations were characterized by assessing their pH, viscosity, particle size, and polydispersity index (PDI). The particle size analysis revealed that the majority of formulations had particle sizes below 1000 nm, which is consistent with the nanoscale range needed for NLC systems, while the viscosity values confirmed good consistency and homogeneity. Uniform particle production and stability were suggested by the monodisperse distributions shown by the PDI values. For all evaluations, the physical properties of Formulations I–III generally satisfied the required standards. Meanwhile Formula VI's particle size exceeded 1000 nm, indicating a less stable dispersion at that lipid ratio. Formulations IV–VI also showed acceptable physicochemical stability. Notably, the use of nyamplung oil contributed additional benefits, such as antioxidant and anti-inflammatory properties, enhancing the overall therapeutic potential. The study highlights the use of locally available natural ingredients to innovate lipid-based delivery systems, offering promising applications in cosmeceutical and pharmaceutical formulations.

Objective: To develop coenzyme Q10 (co-Q10) nanostructured lipid carriers (NLCs) using stearic acid (SA) and various liquid lipids with different lipophilicity as well as highlights the use of in silico studies for predicting and elucidating the interaction of drug-lipid used as carries in NLCs, at the molecular level.
 Methods: The co-Q10 NLCs were prepared using SA as solid lipid and oleic acid (OA), isopropyl myristate (IPM), as well as isopropyl palmitate (IPP) as liquid lipids by the high shear homogenization method. Firstly, the formulas were optimized by the appropriate required HLB (rHLB). The optimized NLCs were characterized in the particle size, distribution of particle size, zeta potential, crystallinity behavior, Fourier transform infrared (FT-IR) spectra, morphology, entrapment efficiency (EE), drug loading (DL), and pH value. The interaction of drug-lipids in silico was studied using the AutoDock Vina program.
 Results: The co-Q10 NLCs using SA and the various liquid lipid possessed the mean particle size, polydispersity index (PDI), zeta potential, EE, DL, and pH values were 180 to 350 nm,<0.5,<-30 mV, 83 to 88%, 10 to 11%, and 5.0 to 5.6, respectively. The EE and DL of co-Q10 NLCs increased with decreasing in binding energy (∆G) in silico.
 Conclusion: The co-Q10 NLCs using SA as solid lipid and OA, IPM, as well as IPP as liquid lipids were developed successfully. Furthermore, in silico study by molecular docking is a potential approach in predicting and elucidating the interaction of drug-lipid in the development of NLCs formulation.

Nanostructured lipid carriers (NLC) are produced using a blend of solid and liquid lipids; this blend is solid at room temperature. NLC is a second generation of lipid nanoparticles, which offer the advantage of improved drug-loading capability and release properties. The purpose of this study was to find the optimized proportion of liquid and solid lipids for production of doxorubicin (Dox)-loaded NLC (Dox-NLC) to decrease the cytotoxicity of Dox. Dox-NLC was prepared by the solvent emulsification/evaporation method using stearic acid (SA) and oleic acid (OA) as the solid lipid and liquid lipid, respectively. Poloxamer 188 and lecithin were used to stabilize NLC dispersion. The physicochemical characteristic and cytotoxicity of Dox-NLC were evaluated. The NLC prepared by 0.6% of stearic acid and 0.4% of oleic acid, showed optimum results with particle size of 134.0 ± 2.3 nm, zeta potential of −19.0 ± 3.9 mV, drug-loading efficiency of 9.5%, and entrapment efficiency of 75%. The drug loading after freeze drying and also after 60 days storage at 4 °C did not change. In vitro drug release study showed that Dox was released from the NLC in a slow but time-dependent behavior. The cytotoxicity of Dox-NLC on MCF-7 cell line was increased compared with the Dox solution. These results suggested that the Dox-NLC produced by this method could be utilized as a sustained release drug carrier system for improving the effectiveness of chemotherapy.

Nanostructured lipid carrier (NLC) is a second generation lipid nanoparticle formed by blends of solid and liquid lipids through hot homogenization technique. In this study, arachidic acid (C20) and erucic acid (C22:1) were used as solid lipids while oleic acid as liquid lipid in the preparation of NLC. Five types of NLC were prepared by varying the amount of oleic acid (C18:1) with respect to arachidic acid while maintaining the amount of erucic acid. Physical stability of the prepared NLC was characterized by its size and zeta potential for a period of 28 days. The results showed that the size of NLCs were between 200 to 260 nm with zeta potential of -55 to -40 mV. Differential scanning calorimetry (DSC) data showed that presence of oleic acid reduces the crystallinity of nanoparticle. Apart from that, depending on the compositions, the morphology of NLC examined under transmission electron microscopy’s (TEM) was round to elongate in shape. Then, active ingredients of ascorbic acid, caffeine and lidocaine with varied hydrophilicity were then loaded into the NLC. Lidocaine has an encapsulation efficiency of nearly 78% while caffeine reaches 43%. Surprisingly, ascorbic acid which is hydrophilic gave a comparative amount of encapsulation efficiency as caffeine at low concentration. This might relate to attraction between opposite charge of NLC and ascorbic acid. When the active ingredients loaded NLC was subjected to in vitro release, the active ingredients’ release profile suggested that NLC exhibit sustained release properties whereby the rate of release is concentration dependent.

In this study, the formulation of Orthosiphon stamineus (OS) loaded onto nanostuctured lipid carrier was prepared using melt emulsification homogenisation technique. Glyceryl monostearate and triglyceride were used as solid and liquid lipids respectively. D-optimal mixture design was employed to optimise the formulation of OS loaded into nanostructured lipid carrier. The independent variables were OS extract, solid lipid and liquid lipid, while the dependent variables were particle size, polydispersity index (PDI) and encapsulation efficiency. Multiple correlation coefficient (R2) obtained for particle size, PDI and encapsulation efficiency was 0.9404, 0.9138 and 0.8754. All three models are significant and the lack of fit for all dependent variables was not significant. Solid lipid was the most influential factor for particle size. For PDI, OS was the dominant factor. Meanwhile liquid lipid is the most influential factor toward the encapsulation efficiency. The optimum formulation of OS loaded nanostructured lipid carrier is 4 % of OS, 1 % of solid lipid and 5 % of liquid lipid.

Nanostructured Lipid Carriers (NLC) are lipid-based carrier system that use a matrix combination in the form of solid and liquid which are stabilized with the addition of surfactant. This NLC was developed to facilitate the dispersion of hydrophobic bioactive compound in a hydrophilic system. This research aims to get the right formulation and can develop stable characterization, using solid lipids Poloxamer and Stearic Acid with liquid lipids Soybeans Oil using surfactant Tween 80 and co-surfactant Propyleneglycol.. The to make the formulation of NLC with a ratio of poloxamer and stearic acid as solid lipid: soybeans oil asliquid lipid is 3:3, 4:2, 5:1 ,surfactant tween 80 and co surfactant propyleneglycol. Test the NLC characterization including PH value, viscosity, particle size, and polydispersity index. Data analysis used to evaluate the characteristics of the obtained NLC using descriptive. The result of the research showed that NLC had good characteistics at a solid lipid poloxamer and stearic acid with Soybean oil liquid lipid ,pH in the range 4-6; good viscosity; good particles have a range of 1000nm; and polydispersity index which shows the results of monodispersion. Nanostructured Llipid Carriers with solid lipid poloxamer and stearic acid and liquid lipid soybean oil obtained good characteristics.

The D-optimal mixture design was employed to evaluate the effect of different composition variables on particle size, polydispersity index, zeta potential and encapsulation efficiency for optimization of Zingiber zerumbet oil loaded nanostructured lipid carrier (NLC). The glyceryl monostearate were used as solid lipid, virgin coconut oil as liquid lipid, and Tween 80 as well as soy lecithin were used as surfactant to achieve stable NLC formulation. The hot homogenization and ultrasonication techniques were employed in preparation of NLC. The statistical evaluations by ANOVA revealed that optimum NLC formulation generated as 3.7% Zingiber zerumbet oil, 5% liquid lipid and 1.3% solid lipid. The optimal NLC formulation had an average diameter of 91.002 nm, PDI of 0.172, zeta-potential of -40.88 mV, and encapsulation efficiency of 94.45%. The transmission electron microscopy (TEM) observations exhibited spherical morphology of Zingiber zerumbet oil loaded NLC. Penetration through Strat-M® membrane shown an excellent diffusion coefficient of NLC-Zingiber zerumbet oil. Therefore, D-optimal mixture design has succeeded in generating optimum NLC formulation for encapsulation of Zingiber zerumbet oil. The stable formulation of NLC for encapsulating essential oil give promising future in various applications such as drug delivery, food, textile and cosmetics.

The purpose of this study was to design and optimize a new topical deliverysystem for ocular administration of flurbiprofen (FB), based on lipidnanoparticles. These particles, called nanostructured lipid carriers (NLC), werecomposed of a fatty acid (stearic acid (SA)) as the solid lipid and a mixture ofMiglyol® 812 and castor oil (CO) as the liquid lipids, prepared by the hot high pressurehomogenization method. After selecting the critical variables influencing thephysicochemical characteristics of the NLC (the liquid lipid (i.e. oil) concentration withrespect to the total lipid (cOil/L (wt%)), the surfactant and the flurbiprofenconcentration, on particle size, polydispersity index and encapsulation efficiency), athree-factor five-level central rotatable composite design was employed to plan andperform the experiments. Morphological examination, crystallinity and stabilitystudies were also performed to accomplish the optimization study. The resultsshowed that increasing cOil/L (wt%) was followed by an enhanced tendency toproduce smaller particles, but the liquid to solid lipid proportion should not exceed30 wt% due to destabilization problems. Therefore, a 70:30 ratio of SA to oil (miglyol + CO) was selected to develop an optimal NLC formulation. The smaller particlesobtained when increasing surfactant concentration led to the selection of 3.2 wt% ofTween® 80 (non-ionic surfactant). The positive effect of the increase in FB concentrationon the encapsulation efficiency (EE) and its total solubilization in the lipidmatrix led to the selection of 0.25 wt% of FB in the formulation. The optimalNLC showed an appropriate average size for ophthalmic administration(228.3 nm) with a narrow size distribution (0.156), negatively charged surface (−33.3 mV) andhigh EE (∼90%). The in vitro experiments proved that sustained release FB was achieved using NLC asdrug carriers. Optimal NLC formulation did not show toxicity on ocular tissues.

Nanostructured Lipid Carriers for Intranasal Administration of Olanzapine in the Management of Schizophrenia

Nanostructured lipid carriers for targeting drug delivery to the epidermal layer.