Nanostructured lipid carrier loaded with zingiber officinale and Zingiber zerumbet oil for induction of lipolysis in subcutaneous skin layer

Body weight loss strategies include combination of nutrition consultation, regular exercise, drug prescription, invasive intervention and/or non-invasive intervention. A non-invasive intervention such as transdermal administration of active ingredients helps in reducing localized subcutaneous adipose tissue through lipolysis. Zingiber officinale (ZO) and Zingiber zerumbet (ZZ) belong to the Zingiberaceae family and both have been discovered to possess lipolysis activity. An efficient drug delivery system is required to encapsulate ZO and ZZ, and deliver these substances up to the subcutaneous skin layer. In this study, ZO and ZZ oil were successfully encapsulated in nanostructured lipid carrier (NLC) using hot homogenization technique followed by ultrasonication. D-optimal mixture design was used to optimize the NLC in which the composition of ZO and ZZ oil, solid lipid, and liquid lipid were the independent variables, while particle size, polydispersity index (PDI), zeta potential, and encapsulation efficiency were the dependent variables. From the study, the optimum formulation for NLC-ZO was 3.6% ZO oil, 1.4% glyceryl monostearate, and 5.0% virgin coconut oil, and the NLC-ZO obtained had the following properties: 90.7 nm particle size, 0.15 PDI, -45.7 mV zeta potential and 88.8% encapsulation efficiency. The optimum NLC-ZZ formulation was 3.7% ZZ oil, 1.3% glyceryl monostearate, and 5.0% virgin coconut oil, and the NLC-ZZ obtained had the following properties: 91.0 nm particle size, 0.17 PDI, -40.9 mV zeta potential and 94.4% encapsulation efficiency. Morphology study revealed the spherical shape of NLC-ZO and NLC-ZZ, and the particle size obtained through transmission electron microscope conformed with the size measured through dynamic light scattering technique. Thermogram profile of NLC showed incorporation of ZO and ZZ into NLC lowered the melting temperature of lipid mixture, thus producing a less ordered crystalline structure of NLC to accommodate the active ingredients. Fourier transform infrared spectroscopy analysis demonstrated an interaction existed between ZO/ZZ and the NLC system. In vitro penetration study using Strat-M® membrane and freshly excised rat skin showed NLC-ZO and NLC-ZZ had higher penetration flux compared to free ZO and ZZ. The release of ZO from NLC-ZO followed Korsmeyer-Peppas model, and the release of ZZ from NLC-ZZ followed zero order kinetic model. 90-day storage stability study showed no significant changes for both NLC-ZO and NLC-ZZ in terms of particle size, PDI and zeta potential. In vitro lipolysis study revealed the potential of NLC-ZO and NLC-ZZ as anti-obesity agents as they stimulated the release of glycerol in 3T3-L1 adipocytes cells. In vivo NLC distribution in female Sprague- Dawley rats showed penetration deep into the dermis layer after 12 h of application. Free fatty acid release was detected when the rats were treated with NLC-ZO and NLC-ZZ for 3 h. This study demonstrated that ZO and ZZ were successfully encapsulated in NLC and the nanoparticles were effectively utilized to enhance dermis penetration and induce lipolysis activity via in vitro and in vivo

Incorporation of Nanoparticles Based on Zingiber Officinale Essential Oil into Alginate Films for Sustained Release

This research focused on the formulation of Ca2+ cross-linked alginate (Alg) gels containing Zingiber officinale oil extract (ZOE) loaded into a nanostructured lipid carrier (NLC). The NLC is intended to protect the Zingiber officinale oil against physical and chemical degradation during topical administration to sustain the drug release and reduce drug leakage during storage. The NLC was prepared using hot homogenisation and ultrasonication of glyceryl monostearate. Virgin coconut oil was used as the liquid lipid. The NLC-ZOE had a mean size diameter of 100 nm and a zeta potential value of −40 mV. The ZOE released from NLC followed the Korsmeyer-Peppas model case I (Fickian diffusion). The NLC-ZOE formulation was then incorporated into Alg. The gels were prepared via ionotropic gelation in the presence of calcium. Scanning electron microscopy (SEM) images of Alg films revealed successful intercalation of NLC within the Alg matrix. The in vitro ZOE release from NLC-ZOEAlg occurred in a sustained manner from the cross-linked Alg hydrogels compared to the free NLC. The profiles of NLC-ZOE released from the Alg films depended on the nanoparticles amount. The results demonstrated the importance of designing a local delivery system to entrap and control the release of the bioactive components of ZOE from within the Alg matrix. Ca2+ cross-linked Alg gels containing ZOE loaded into NLC was found to be suitable for topical delivery applications, as shown by the sustained release of ZOE from calcium cross-linked Alg films containing NLC that was demonstrated in this study.Fil: Rosli, Nur Ayshah. Universiti Sains Malaysia; MalasiaFil: Islan, German Abel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata. Centro de Investigación y Desarrollo en Fermentaciones Industriales. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Centro de Investigación y Desarrollo en Fermentaciones Industriales; ArgentinaFil: Hasham, Rosnani. Universiti Teknologi Malaysia; MalasiaFil: Castro, Guillermo Raul. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata. Centro de Investigación y Desarrollo en Fermentaciones Industriales. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Centro de Investigación y Desarrollo en Fermentaciones Industriales; Argentina. Universidad Federal do Abc; BrasilFil: Aziz, Azila Abdul. Universiti Teknologi Malaysia; Malasi

Formulation and characterization of [6]-gingerol loaded nanostructured lipid carrier (NLC)

Nanostructured lipid carrier (NLC) is the blend of solid lipid, liquid lipid and suitable surfactant for the purpose of encapsulated poorly water soluble drugs. [6]-gingerol is the main bioactive compound in Zingiber officinale, widely known as ginger in Malaysia. Zingiber officinale extract has been discovered to have anti-oxidant, anti-inflammatory, and anti-microbial effects to human body. The aim of this study is to develop NLC formulation for [6]-gingerol and to estimate the potential of NLC as a delivery system for these water insoluble drugs. In this work, the preparation of ginger oil loaded onto nanostructured lipid carrier (GO-NLC) was done by using ultrasonication method. The GO-NLCs were assessed by evaluating the morphology and its entrapment efficiency. The morphological study was performed by using Zetasizer Nano S and the entrapment efficiency analysis of NLC was performed using HPLC by detecting [6]-gingerol as active biomarker. The average particle size for GO-NLCs ranged from size 100 to 250 nm and the average encapsulation efficiency was 92.7± 3.03%.Based on analysis, it is proved that nanostructured lipid carriers has high potential to be nanocarriers for [6]-gingerol

Effects of formulation parameters on particle size and polydispersity index of orthosiphon stamineus loaded nanostructured lipid carrier

This study was conducted to investigate the effect of particle size and polydispersity index (PDI) by changing the concentration of active ingredient and solid lipid in the Orthosiphon stamineus (O. stamineus) loaded nanostructured lipid carrier (NLC) formulation. O. stamineus extract was prepared by maceration method. From the HPLC analysis, the O. stamineus extract contains 38% sinensetin and 62% rosmarinic acid. The method used to prepare the formulation of O. Stamineus loaded NLC is melt emulsification homogenization technique. Solid and liquid lipid used were glyceryl monostearate and triglyceride respectively. It was found that the size of particles increased as increasing in concentration of active and solid lipid in the formulation. The best range for concentration of active and solid lipid are 1-4% and 1-3% respectively since the particle size and PDI needed are below 200 d.nm and 0.2. Collectively, based on particle size and PDI results show that the NLC system is highly potential to be a carrier of transdermal delivery for O. stamineus

Formulation and characterization of nanostructured lipid carrier encapsulated zingiber zerumbet oil using ultrasonication technique

This study presents the formulation of nanostructured lipid carrier encapsulated Zingiber zerumbet oil (NLC-ZZ) using ultrasonication technique. NLC is the blend of solid lipid, liquid lipid and surfactant for encapsulation of poor water soluble actives. The NLC-ZZ formulation was characterized with respect to particle size, polydispersity index (PDI), zeta-potential, encapsulation efficiency and physical morphology. The NLC-ZZ formulation had an average diameter of 96.59 nm, PDI of 0.192, zeta-potential of -39.88 mV, and encapsulation efficiency of 90%, respectively. The NLC formulation for Zingiber zerumbet oil encapsulation has been successfully developed and is suitable for transdermal delivery system due to their nano-size and stability

Effect of high pressure homogenizer on the formation of zingiber officinale- loaded nanostructured lipid carrier

Nowadays, nanostructured lipid carrier has been employed in pharmaceutics, nutraceuticals and biomedical formulations also other purposes. The aim of this study was to estimates the effect of high pressure homogenizer on the properties of zingiber officinale loaded nanostructured lipid carrier especially on size of particle and polydispersity index. Experiments were constructed using high pressure homogenizer by applying certain homogenizing pressure and cycle. The independent variables were homogenization pressure (0–2000 bar) and cycle (1-9) and the analysed responses were particles size and polydispersity index. The increase in the homogenization pressure up to 1300 bar and six cycle decreased the emulsion droplet size. However, the use of pressures above that pressure and cycle resulted in the formation of droplets with larger size

Preparation of zingiber officinale loaded nanostructured lipid carrier (NLC) using ultrasonication and microfluidizer: a comparison

Nanostructured lipid cemer (NLC) is the blend of solid lipid. liquid lipid and suitable surfactant foe the purpose of encapsulated poorly water soluble drugs. Zingiber officinale (ginger) extract has been discovered to have anti-oxidant,anti-inflammatory. and anti-microbial effects to the human body. The aim of this study is to develop NLC formulation for encapsulation of Zingiber officinale (ZO) oil and to compare the charecteristic of NLC prepared using different. methods, ultrasonication and microfluidizer. ln this work, the prepared ZO-NLCs were evaluated in terms of particle size zeta potential, entrapment efficiency and drug loading capacity. The morphological study was performed by using Zetasizer Nano S and entrapment efficiency analysis of NLC was performed using HPLC by detecting (6}-gingerol as active biomarker. Based on the study, NLC prepared by ultrasonication and microfluidizer has an evereqe particle size of 100-250 nm and So-l OO nm, respectively, for same formulation. NLC prepared using mlcrofluidirer also exhibit superior entrapment efficiency and drug loading capacity compared to ultrasonication. Based on the analyses, both ultrasonication and microfluidizer method able to prepare NLC for ZO encapsulation, and microfluidizer appeared to have the pctential to produce more stable and desirable properties of NLC

Skin improvement using Labisia Pumila and Ficus Deltoidea cosmetic formulations

In the tropic, continuous exposure to ultraviolet (UV) light is known to cause photoageing. UV generated reactive oxygen species leading to collagen deficiency and eventually skin wrinkling. Our in vitro study indicated that Labisia pumila (LP) and Ficus deltoidea (FD) could protect fibroblast from UVB irradiation damage. The purpose of this study was to determine the effectiveness of the cosmetic formulation based on LP and FD extracts in reducing the effect of skin ageing due to exposure to UVB irradiation. The evaluation of the active serum and placebo was carried out on 78 volunteers for two months and conducted using noninvasive bioengineering methods including melanin index, erythema index, skin moisture content, skin sebum content and skin surface pH measurement. The cutaneous hydration was increased after 8 weeks application of cosmetic formulation and this is highly related to a decrease of restoration of normal skin surface pH. Besides, the formulation application also caused a significant decrease in skin melanin, erythema content and casual sebum level after 8 weeks application. The formulations prepared from LP and FD were able to exhibit anti-ageing effects. Further study on LP and FD based formulations must be carried out for future natural regenerative anti-ageing cosmetic in the tropic region such as Asia and Middle East market