The activity of candlenut oil in the nanostructured lipid carrier system on hair growth in rats.

Background: Candlenut oil (Aleurites moluccana L. Willd), which is also called Aleurites moluccana Seed (AMS) oil, is empirically effective as a hair growth agent, it is an unstable substance. Nanostructured Lipid Carrier (NLC) is a delivery system that is proven to increase the effectiveness and stability of the material, and the usage of solid lipid combination: beeswax-oleum cacao can produce good NLC characteristics. Objective: To determine the effectiveness of NLC_AMS oil with different combination of beeswax-oleum cacao (100:0; 50:50; 25:75; and 0:100) as a hair growth agent, using rats as subjects. Methods: NLC-AMS oil was made using 20% of total lipid with 5% AMS oil as liquid lipid and 15% solid lipid; combinations of beeswax-oleum cacao were of different ratios (100:0; 50:50; 25:75; and 0:100). NLC was made by High Shear Homogenization (HPH) method. Hair growth activity test carried out on male white rats using the research methods of Yoon (2010). Results: The addition of oleum cacao as a solid lipid did not affect the pH, but increased the consistency and decreased the particle size of NLC- AMS oil. There was a relationship between the characteristic of NLC and the hair growth activity test: the small particle size and low viscosity had greater hair growth activity. Conclusion: The usage of solid lipid combination: beeswaxoleum cacao can produce better NLC characteristics and had higher hair growth activity than the formulas that used single lipid.

The effect of peppermint oil addition on the physical stability, irritability, and penetration of nanostructured lipid carrier coenzyme Q10.

Background: Coenzyme Q10 is formulated into Nanostructured Lipid Carrier (NLC) added with peppermint oil (PO) 0% (F1), 1% (F2), 1.5% (F3) and 2% (F4) to increase its penetration. Objective: This study aims to determine the effect of PO addition on the irritability, stability, and penetration of Coenzyme Q10 in the NLC. Methods: Coenzyme Q10 NLC was prepared using the High Shear Homogenization method. Furthermore, physical characterization was carried out. Physical stability testing was carried out for 90 days at a temperature of 25±5oC and an RH of 60±10%. The in vivo irritation test was observed for mice's back skin after 24 hours while the penetration study was further evaluated at 2 hours of the sample application. Results: Increasing the PO amount into Coenzyme Q10 NLC reduced the viscosity which was 329.1±15.5 cps for PO 0% to 219.9±2.9 cps for 2% addition. The observation of particle morphology showed that all NLC Coenzyme Q10 has a spherical particle shape with particle size between 188.25±13.22 to 197.80±14.19 nm. All formulas had high entrapment efficiency (>80%). PO addition did not cause changes in physical characteristics during 90 days of storage. The 24 hours' irritation test showed that F2 and F3 are non-irritating. By PO addition skin penetration improved at 2 hours' penetration study. Conclusion: PO addition up to 2% reduced viscosity, but did not affect particle size and morphology of Coenzyme Q10 NLC. Addition of PO up to 1.5% increased entrapment efficiency, did not irritate and increased the penetration of Coenzyme Q10 NLC.

The effect of 1,2-dioleoyl-3-trimethylammonium propane (DOTAP) Addition on the physical characteristics of ß-ionone liposomes.

ß-ionone (ION) is a cyclic terpenoid compound that demonstrates considerable potential for the prevention and treatment of cancer. However, the water solubility of ß-ionone is poor and the compound demonstrates low permeability. Liposomes have been reported as increasing both qualities. In this study, the development of ß-ionone liposomes was initiated by adding 1,2-dioleoyl-3-trimethylammonium propane (DOTAP) to produce cationic liposomes as a means of enhancing binding to cancer cells. Liposomes composed of ß-ionone, HSPC, cholesterol, and DSPE-mPEG2000 were prepared using the thin layer hydration method. Cellular uptake studies were carried out with HeLa cells incubated with ß-ionone liposomes for two hours. The results indicated that the addition of DOTAP increased particle size and affected the spectroscopical and thermogram profiles of the liposomes, thereby confirming reduction in liposome crystallinity, while the zeta potential became positive. Moreover, the calcein release profile further showed that additional DOTAP increased both membrane fluidity and cellular uptake in HeLa cells In conclusion, adding DOTAP affected the physicochemical cationic properties of liposome and improved cellular uptake in HeLa cells.

The effect of surfactant type on characteristics, skin penetration and anti-aging effectiveness of transfersomes containing amniotic mesenchymal stem cells metabolite products in UV-aging induced mice.

Transfersome has been developed to enhance dermal delivery of amniotic mesenchymal stem cell metabolite products (AMSC-MP). AMSC-MP contains many growth factors for managing skin aging, thus improving the quality of an adjusted life year. This study aims to determine the effect of surfactant types acting as the edge activator on transfersome-loading AMSC-MP. Transfersome was prepared by thin-layer hydration method and composed of l-α-phosphatidylcholine as a phospholipid and three types of surfactants, namely; cationic (stearylamine), anionic (sodium cholate), and nonionic surfactant (Tween 80) at a weight ratio of 85:15, respectively. Transfersomes were evaluated for physical characteristics, penetration, effectiveness, and safety. The results showed that sodium cholate, an anionic surfactant, produced the smallest transfersome particle size, i.e., 144.2 ± 3.2 nm, among all formulas. Trans-SA containing stearylamine had a positive charge of 41.53 ± 6.03 mV compared to Trans-SC and Trans-TW, whose respective charges were -56.9 ± 0.55 mV and -41.73 ± 0.86 mV. The small particle size and low negative value of zeta potential enabled high dermal penetration by transfersomes containing AMSC-MP, while the positive charge of stearylamine hindered its penetration of deeper skin layers. Trans-SC and Trans-TW produced higher collagen density values at 77.11 ± of 4.15% and 70.05 ± of 6.95%, than that of Trans-SA. All the AMSC-MP transfersomes were relatively safe with 0.5-1.0 macrophage cell numbers invaded the dermis per field of view. In conclusion, sodium cholate, an anionic surfactant, demonstrated considerable capacity as the edge activator of transfersome-loading AMSC-MP for skin anti-aging therapy.

Penetration study of p-methoxycinnamic acid (PMCA) in nanostructured lipid carrier, solid lipid nanoparticles, and simple cream into the rat skin.

This study compared the ability of Nanostructured Lipid Carrier (NLC), Solid Lipid Nanoparticles (SLN), and Cream systems in delivering para Methoxycinnamic Acid (PMCA) to the dermis layer of the skin. Wistar rats were used as research subjects. NLC and SLN were made by applying the high shear homogenization method. Nile red was used as a penetration indicator based on its fluorescence. The interaction between fluorescence labeled NLC, SLN, or Cream and rat skin was visualized by fluorescence microscopy. Observations were made after 2 and 4.5 h of smearing the test sample. From the observations, it was known that the system/lipid base could penetrate the stratum corneum for delivering drugs. Penetration speed differs among systems as does the number of PMCAs that can be delivered. In this study, it can be concluded that the NLC system is able to deliver PMCA more quickly and in greater quantities to the dermis than SLN and Cream.

Characterization and in vitro release of inhalation quercetin solid lipid microparticles: Effect of lipid.

This study purposes to develop solid lipid microparticles (SLM) inhalation delivery system for respiratory diseases with Quercetin as the active agent. Quercetin has various functions, such as for antioxidant, anti-inflammatory, immunomodulator, and antivirus. SLM is formed from a mixture of lipids and surfactants, namely, Glyceryl Behenate as solid lipid, Poloxamer 188 as the surfactant, and production of SLM using the melt o/w emulsification technique and was dried using freeze dryer. The effect of lipid concentration was studied in this research. Quercetin SLM was characterized by moisture content, Fourier transform infrared, particle size, yield, drug loading, and encapsulation efficiency. The SLM particles produced were spherical in shape and had a smooth surface with sizes of F1, F2, and F3 were 1.79 µm, 1.88 µm, and 1.91 µm, respectively. According to the target particle size of inhalation, Quercetin SLM had good flowability according to Carr's Index (F1 = 12.73% ± 0.38, F2 = 14.28% ± 0.65, F3 = 14.65% ± 0.62), in which the highest drug loading and EE of F3 were 10.94% and 88.48%, respectively. In vitro release study showed that in 630 min about 31%-33% Quercetin released indicated sustained release following Higuchi kinetics and quercetin release rate was not affected by the amount of lipid. To sum up, quercetin SLM demonstrates its potential as an inhalation delivery system and it is recommended to study its stability.

The thermodynamic study of p-methoxycinnamic acid inclusion complex formation, using ß-cyclodextrin and hydroxypropyl-ß-cyclodextrin.

OBJECTIVES: Cyclodextrin's ability to form an inclusion complex with a guest molecule is a function of two factors. The first is steric and depends on the relative size of cyclodextrin cavity to the guest molecule, while the second is the thermodynamic interaction between the different system components. This study therefore aims to determine the effect of ß-cyclodextrin and hydroxypropyl-ß-cyclodextrin as complex formers, on thermodynamic parameter values (ΔH, ΔG, and ΔS) in the formation of inclusion complex with p-methoxycinnamic acid (pMCA). METHODS: The pMCA complex formation with ß-cyclodextrin or hydroxypropyl-ß-cyclodextrin was determined in 0.02 pH 4.0 M acetate buffer and 0.02 M pH 7.0 phosphate buffer, with a 0.2 µ value at 32, 37, and 42 ± 0.5 °C. This experiment was carried out in a waterbath shaker until a saturated solution was obtained. Subsequently, pMCA concentration was determined using UV spectrophotometer at the maximum pMCA wavelength, at each pH. RESULTS: The result showed pMCA formed inclusion complex with ß-cyclodextrin or hydroxypropyl-ß-cyclodextrin and exhibited increased solubility with increase in ß-cyclodextrin or hydroxypropyl-ß-cyclodextrin concentration. This temperature rise led to a decrease in the complex's constant stability (K). Furthermore, the interaction showed a negative enthalpy (∆H<0) and is a spontaneous processes (∆G<0). At pH 4.0, an increase in the system's entropy occurred (∆S>0), however, at pH 7.0, the system's entropy decreased (∆S<0). CONCLUSIONS: The rise in pMCA solubility with increase in cyclodextrin solution concentration indicates an inclusion complex has been formed, and is supported by thermodynamic data.

Interactions of primaquine and chloroquine with PEGylated phosphatidylcholine liposomes.

This study aimed to analyze the interaction of primaquine (PQ), chloroquine (CQ), and liposomes to support the design of optimal liposomal delivery for hepatic stage malaria infectious disease. The liposomes were composed of hydrogenated soybean phosphatidylcholine, cholesterol, and distearoyl-sn-glycero-3-phosphoethanolamine-N-(methoxy[polyethyleneglycol]-2000), prepared by thin film method, then evaluated for physicochemical and spectrospic characteristics. The calcein release was further evaluated to determine the effect of drug co-loading on liposomal membrane integrity. The results showed that loading PQ and CQ into liposomes produced changes in the infrared spectra of the diester phosphate and carbonyl ester located in the polar part of the phospholipid, in addition to the alkyl group (CH2) in the nonpolar portion. Moreover, the thermogram revealed the loss of the endothermic peak of liposomes dually loaded with PQ and CQ at 186.6 °C, which is identical to that of the phospholipid. However, no crystallinity changes were detected through powder X-ray diffraction analysis. Moreover, PQ, with either single or dual loading, produced the higher calcein release profiles from the liposomes than that of CQ. The dual loading of PQ and CQ tends to interact with the polar head group of the phosphatidylcholine bilayer membrane resulted in an increase in water permeability of the liposomes.

Peel-off emulgel mask of Cocos nucifera L. Extract using gelling agent carbomer 940 as antiacne against Propionibacterium acnes ATCC 11827.

Cocos nucifera Linn., which contain lauric acid has been known had antibacterial activity against Propionibacterium acnes that usually improve severe of pimple. Current study investigated optimum formula of emulgel mask based on the C. nucifera L. Extract from Kopyor coconut. Extract were tested for antibacterial against P. acnes ATCC 11827. In this research, C. nucifera L. extract of 1 and 5% were formulated as an active agent of peel off antiacne emulgel mask-containing carbomer 940 in various concentration (1% and 1.5%). The peel-off emulgel mask of C. nucifera L extract was then evaluated in terms of viscosity, pH, drying time, spreadability, and antibacterial activity. The selected formula was formula containing 5% of extract and 1% of carbomer 940. This formula had pH that suitable with skin pH 4.5-6.5, had good spreadability, and also produced highest antibacterial activity against P. acnes.

Enhancing skin penetration of epigallocatechin gallate by modifying partition coefficient using reverse micelle method.

Aim: (-)-Epigallocatechin gallate (EGCG) has been reported as inducing apoptosis in cervical cancer. However, EGCG demonstrates low skin permeability. In order to develop topical delivery of EGCG, the partition coefficient, log P, was modified using a reverse micelle method. Results & methodology: During this study, Tween 80 and Span 80 were added to EGCG at hydrophilic-lipophilic balance (HLB) values of 4.3, 6 and 8. The results showed that lowering the HLB value increases the log P value of EGCG and results in higher IC50 values in Henrietta Lacks (HeLa) cancer cells than that of EGCG. Surfactant-modified EGCG-HLB 6 produced faster and deeper skin penetration than EGCG. Conclusion: Modification of log P value using a combination of Tween 80 and Span 80 improved cytotoxicity and topical delivery of EGCG.