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Fulltext Development of nanoemulsion for efficient brain parenteral delivery of cefuroxime: designs, characterizations, and pharmacokinetics

Harun SN, Nordin SA, Gani SSA, Shamsuddin AF, Basri M, Basri HB

Int J Nanomedicine, 2018;13:2571-2584.
PMID: 29731632 DOI: 10.2147/IJN.S151788

Background and aim: Drugs that are effective against diseases in the central nervous system and reach the brain via blood must pass through the blood-brain barrier (BBB), a unique interface that protects against potential harmful molecules. This presents a major challenge in neuro-drug delivery. This study attempts to fabricate the cefuroxime-loaded nanoemulsion (CLN) to increase drug penetration into the brain when parenterally administered.
Methods: The nanoemulsions were formulated using a high-pressure homogenization technique and were characterized for their physicochemical properties.
Results: The characterizations revealed a particle size of 100.32±0.75 nm, polydispersity index of 0.18±0.01, zeta potential of -46.9±1.39 mV, viscosity of 1.24±0.34 cps, and osmolality of 285.33±0.58 mOsm/kg, indicating that the nanoemulsion has compatibility for parenteral application. CLN was physicochemically stable within 6 months of storage at 4°C, and the transmission electron microscopy revealed that the CLN droplets were almost spherical in shape. The in vitro release of CLN profile followed a sustained release pattern. The pharmacokinetic profile of CLN showed a significantly higher Cmax, area under the curve (AUC)0-
t
, prolonged half-life, and lower total plasma clearance, indicating that the systemic concentration of cefuroxime was higher in CLN-treated rats as compared to cefuroxime-free treated rats. A similar profile was obtained for the biodistribution of cefuroxime in the brain, in which CLN showed a significantly higher Cmax, AUC0-
t
, prolonged half-life, and lower clearance as compared to free cefuroxime solution.
Conclusion: Overall, CLN showed excellent physicochemical properties, fulfilled the requirements for parenteral administration, and presented improved in vivo pharmacokinetic profile, which reflected its practical approach to enhance cefuroxime delivery to the brain.

Matched MeSH terms: Emulsions/administration & dosage*; Emulsions/chemistry
Enhancing biopharmaceutical performance of an anticancer drug by long chain PUFA based self-nanoemulsifying lipidic nanomicellar systems

Khurana RK, Beg S, Burrow AJ, Vashishta RK, Katare OP, Kaur S, et al.

Eur J Pharm Biopharm, 2017 Dec;121:42-60.
PMID: 28887099 DOI: 10.1016/j.ejpb.2017.09.001

The aim of this study was to develop polyunsaturated fatty acid (PUFA) long chain glyceride (LCG) enriched self-nanoemulsifying lipidic nanomicelles systems (SNELS) for augmenting lymphatic uptake and enhancing oral bioavailability of docetaxel and compare its biopharmaceutical performance with a medium-chain fatty acid glyceride (MCG) SNELS. Equilibrium solubility and pseudo ternary phase studies facilitated the selection of suitable LCG and MCG. The critical material attributes (CMAs) and critical process parameters (CPPs) were earmarked using Placket-Burman Design (PBD) and Fractional Factorial Design (FFD) for LCG- and MCG-SNELS respectively, and nano micelles were subsequently optimized using I- and D-optimal designs. Desirability function unearthed the optimized SNELS with Temul <5min, Dnm <100nm, Rel15min >85% and Perm45min >75%. The SNELS demonstrated efficient biocompatibility and energy dependent cellular uptake, reduced P-gp efflux and increased permeability using bi-directional Caco-2 model. Optimal PUFA enriched LCG-SNELS exhibited distinctly superior permeability and absorption parameters during ex vivo permeation, in situ single pass intestinal perfusion, lymphatic uptake and in vivo pharmacokinetic studies over MCG-SNELS.

Matched MeSH terms: Emulsions/pharmacokinetics*; Emulsions/chemistry*
Fulltext A comparative study of the physicochemical properties of a virgin coconut oil emulsion and commercial food supplement emulsions

Khor YP, Koh SP, Long K, Long S, Ahmad SZ, Tan CP

Molecules, 2014 Jul 01;19(7):9187-202.
PMID: 24988188 DOI: 10.3390/molecules19079187

Food manufacturers are interested in developing emulsion-based products into nutritional foods by using beneficial oils, such as fish oil and virgin coconut oil (VCO). In this study, the physicochemical properties of a VCO oil-in-water emulsion was investigated and compared to other commercial oil-in-water emulsion products (C1, C2, C3, and C4). C3 exhibited the smallest droplet size of 3.25 µm. The pH for the emulsion samples ranged from 2.52 to 4.38 and thus were categorised as acidic. In a texture analysis, C2 was described as the most firm, very adhesive and cohesive, as well as having high compressibility properties. From a rheological viewpoint, all the emulsion samples exhibited non-Newtonian behaviour, which manifested as a shear-thinning property. The G'G'' crossover illustrated by the VCO emulsion in the amplitude sweep graph but not the other commercial samples illustrated that the VCO emulsion had a better mouthfeel. In this context, the VCO emulsion yielded the highest zeta potential (64.86 mV), which was attributed to its strong repulsive forces, leading to a good dispersion system. C2 comprised the highest percentage of fat among all emulsion samples, followed by the VCO emulsion, with 18.44% and 6.59%, respectively.

Matched MeSH terms: Emulsions
Fulltext The bioaccessibility of eicosapentaenoic acid was higher from phospholipid food products than from mono- and triacylglycerol food products in a dynamic gastrointestinal model

Domoto N, Koenen ME, Havenaar R, Mikajiri A, Chu BS

Food Sci Nutr, 2013 Nov;1(6):409-15.
PMID: 24804049 DOI: 10.1002/fsn3.58

The bioaccessibility of eicosapentaenoic acid (EPA) in the forms of monoacylglycerol (EPA-MAG), triacylglycerol (EPA-TAG), and phospholipid (EPA-PL) during gastrointestinal passage was compared in this study using a dynamic gastrointestinal model (TIM system). The TIM system simulated the average upper gastrointestinal tract conditions of healthy human adults after intake of a meal (fed state conditions). In this study, the three EPA-rich oils were separately homogenized with full fat milk to obtain oil-in-water emulsions. Plain yogurt was added into the mixture at an emulsion/yogurt ratio of 4:1 (w/w) as the food matrix of the test products. The results show that the test meals containing EPA-PL left the stomach compartment most efficiently in comparison with the gastric emptying of EPA-MAG and EPA-TAG. The PLs also showed a significantly (P < 0.05) higher bioaccessibility of EPA (75-80%) in comparison with MAG (30%) and TAG (38%). The better gastric emptying of EPA-PL was likely related to the more stable emulsion of EPA-PL in the test meal. EPA-PL was delivered within the meal matrix into the duodenum instead of floating on the top of the test meal matrix. EPA-MAG had the highest amount of EPA that did not leave the stomach (68% of the test meal). The results from this work indicate that EPA-PL is a more effective form of EPA for a higher lipid bioaccessibility than MAG and TAG under the test conditions.

Matched MeSH terms: Emulsions
Cavitation technology - a greener processing technique for the generation of pharmaceutical nanoemulsions

Sivakumar M, Tang SY, Tan KW

Ultrason Sonochem, 2014 Nov;21(6):2069-83.
PMID: 24755340 DOI: 10.1016/j.ultsonch.2014.03.025

Novel nanoemulsion-based drug delivery systems (DDS) have been proposed as alternative and effective approach for the delivery of various types of poorly water-soluble drugs in the last decade. This nanoformulation strategy significantly improves the cell uptake and bioavailability of numerous hydrophobic drugs by increasing their solubility and dissolution rate, maintaining drug concentration within the therapeutic range by controlling the drug release rate, and reducing systemic side effects by targeting to specific disease site, thus offering a better patient compliance. To date, cavitation technology has emerged to be an energy-efficient and promising technique to generate such nanoscale emulsions encapsulating a variety of highly potent pharmaceutical agents that are water-insoluble. The micro-turbulent implosions of cavitation bubbles tear-off primary giant oily emulsion droplets to nano-scale, spontaneously leading to the formation of highly uniform drug contained nanodroplets. A substantial body of recent literatures in the field of nanoemulsions suggests that cavitation is a facile, cost-reducing yet safer generation tool, remarkably highlighting its industrial commercial viability in the development of designing novel nanocarriers or enhancing the properties of existing pharmaceutical products. In this review, the fundamentals of nanoemulsion and the principles involved in their formation are presented. The underlying mechanisms in the generation of pharmaceutical nanoemulsion under acoustic field as well as the advantages of using cavitation compared to the conventional techniques are also highlighted. This review focuses on recent nanoemulsion-based DDS development and how cavitation through ultrasound and hydrodynamic means is useful to generate the pharmaceutical grade nanoemulsions including the complex double or submicron multiple emulsions.

Matched MeSH terms: Emulsions
Impact of process parameters in the generation of novel aspirin nanoemulsions--comparative studies between ultrasound cavitation and microfluidizer

Tang SY, Shridharan P, Sivakumar M

Ultrason Sonochem, 2013 Jan;20(1):485-97.
PMID: 22633626 DOI: 10.1016/j.ultsonch.2012.04.005

In the present investigation, the operating efficiency of a bench-top air-driven microfluidizer has been compared to that of a bench-top high power ultrasound horn in the production of pharmaceutical grade nanoemulsions using aspirin as a model drug. The influence of important process variables as well as the pre-homogenization and drug loading on the resultant mean droplet diameter and size distribution of emulsion droplets was studied in an oil-in-water nanoemulsion incorporated with a model drug aspirin. Results obtained show that both the emulsification methods were capable of producing very fine nanoemulsions containing aspirin with the minimum droplet size ranging from 150 to 170 nm. In case of using the microfluidizer, it has been observed that the size of the emulsion droplets obtained was almost independent of the applied microfluidization pressure (200-600 bar) and the number of passes (up to 10 passes) while the pre-homogenization and drug loading had a marginal effect in increasing the droplet size. Whereas, in the case of ultrasound emulsification, the droplet size was generally decreased with an increase in sonication amplitude (50-70%) and period of sonication but the resultant emulsion was found to be dependent on the pre-homogenization and drug loading. The STEM microscopic observations illustrated that the optimized formulations obtained using ultrasound cavitation technique are comparable to microfluidized emulsions. These comparative results demonstrated that ultrasound cavitation is a relatively energy-efficient yet promising method of pharmaceutical nanoemulsions as compared to microfluidizer although the means used to generate the nanoemulsions are different.

Matched MeSH terms: Emulsions
Fulltext Effect of surfactant and surfactant blends on pseudoternary phase diagram behavior of newly synthesized palm kernel oil esters

Mahdi ES, Sakeena MH, Abdulkarim MF, Abdullah GZ, Sattar MA, Noor AM

Drug Des Devel Ther, 2011;5:311-23.
PMID: 21792294 DOI: 10.2147/DDDT.S15698

The purpose of this study was to select appropriate surfactants or blends of surfactants to study the ternary phase diagram behavior of newly introduced palm kernel oil esters.

Matched MeSH terms: Emulsions
Anti-inflammatory and analgesic effects of ketoprofen in palm oil esters nanoemulsion

Sakeena MH, Yam MF, Elrashid SM, Munavvar AS, Azmin MN

J Oleo Sci, 2010;59(12):667-71.
PMID: 21099145

Ketoprofen is a potent non-steroidal anti-inflammatory drug has been used in the treatment of various kinds of pains, inflammation and arthritis. However, oral administration of ketoprofen produces serious gastrointestinal adverse effects. One of the promising methods to overcome these adverse effects is to administer the drug through the skin. The aim of the present work is to evaluate the anti-inflammatory and analgesic effects from topically applied ketoprofen entrapped palm oil esters (POEs) based nanoemulsion and to compare with market ketoprofen product, Fastum(®) gel. The novelty of this study is, use of POEs for the oil phase of nanoemulsion. The anti-inflammatory and analgesic studies were performed on rats by carrageenan-induced rat hind paw edema test and carrageenan-induced hyperalgesia pain threshold test to compare the ketoprofen entrapped POEs based nanoemulsion formulation and market formulation. Results indicated that there are no significant different between ketoprofen entrapped POEs nanoemulsion and market formulation in carrageenan-induced rat hind paw edema study and carrageenan-induced hyperalgesia pain threshold study. However, it shows a significant different between POEs nanoemulsion formulation and control group in these studies at p<0.05. From these results it was concluded that the developed nanoemulsion have great potential for topical application of ketoprofen.

Matched MeSH terms: Emulsions/chemical synthesis; Emulsions/pharmacology; Emulsions/chemistry
Polysaccharide with antioxidant, α-amylase inhibitory and ACE inhibitory activities from Momordica charantia

Tan HF, Gan CY

Int J Biol Macromol, 2016 Apr;85:487-96.
PMID: 26778156 DOI: 10.1016/j.ijbiomac.2016.01.023

Functional polysaccharide was isolated from Momordica charantia, with a yield of 36% (w/w). M. charantia bioactive polysaccharide (MCBP) was an acidic and branched heteropolysaccharide with a molecular weight of 92 kDa. Fourier transform infrared spectroscopic analysis indicated that MCBP was a pectin-like polysaccharide with an esterification degree of 53% and it contains numerous monosaccharides, predominantly glucose, galactose, and galaturonic acid. The results also showed that MCBP exhibited free radical scavenging activity (31.9%), ferric reducing antioxidant power (0.95 mM), α-amylase inhibition (89.1%), and angiotensin-converting enzyme inhibition (94.1%). In the terms of functionality, MCBP showed a lower water-holding capacity but higher in oil-holding capacity, emulsifying activity and foaming capacity compared to citrus pectin. Scanning electron microscopy images demonstrated that MCBP formed gels with a porous structure, and flow analysis showed that the gel solution exhibited pseudoplastic shear-thinning behavior. These findings indicated that MCBP is a promising functional macromolecular carbohydrate for the food and nutraceutical industries.

Matched MeSH terms: Emulsions
Fulltext Characterization of flaxseed oil emulsions

Lee PE, Choo WS

J Food Sci Technol, 2015 Jul;52(7):4378-86.
PMID: 26139903 DOI: 10.1007/s13197-014-1495-3

The emulsifying capacity of surfactants (polysorbate 20, polysorbate 80 and soy lecithin) and proteins (soy protein isolate and whey protein isolate) in flaxseed oil was measured based on 1 % (w/w) of emulsifier. Surfactants showed significantly higher emulsifying capacity compared to the proteins (soy protein isolate and whey protein isolate) in flaxseed oil. The emulsion stability of the flaxseed oil emulsions with whey protein isolate (10 % w/w) prepared using a mixer was ranked in the following order: 1,000 rpm (58 min) ≈ 1,000 rpm (29 min) ≈ 2,000 rpm (35 min) >2,000 rpm (17.5 min). The emulsion stability of the flaxseed oil emulsions with whey protein isolate (10 % w/w) prepared using a homogenizer (Ultra Turrax) was independent of the speed and mixing time. The mean particle size of the flaxseed oil emulsions prepared using the two mixing devices ranged from 23.99 ± 1.34 μm to 47.22 ± 1.99 μm where else the particle size distribution and microstructure of the flaxseed oil emulsions demonstrated using microscopic imaging were quite similar. The flaxseed oil emulsions had a similar apparent viscosity and exhibited shear thinning (pseudoplastic) behavior. The flaxseed oil emulsions had L* value above 70 and was in the red-yellow color region (positive a* and b* values).

Matched MeSH terms: Emulsions
Magnetic cellulose nanocrystal stabilized Pickering emulsions for enhanced bioactive release and human colon cancer therapy

Low LE, Tan LT, Goh BH, Tey BT, Ong BH, Tang SY

Int J Biol Macromol, 2019 Apr 15;127:76-84.
PMID: 30639596 DOI: 10.1016/j.ijbiomac.2019.01.037

Stimuli-responsive drug release and controlled delivery play crucial roles in enhancing the therapeutic efficacy and lowering over-dosage induced side effects. In this paper, we report magnetically-triggered drug release and in-vitro anti-colon cancer efficacy of Fe3O4@cellulose nanocrystal (MCNC)-stabilized Pickering emulsions containing curcumin (CUR). The loading efficiency of CUR in the micron-sized (≈7 μm) MCNC-stabilized Pickering emulsions (MCNC-PE) template was found to be 99.35%. The drug release profiles showed that the exposure of MCNC-PE to external magnetic field (EMF) (0.7 T) stimulated the release of bioactive from MCNC-PE achieving 53.30 ± 5.08% of the initial loading over a 4-day period. The MTT assay demonstrated that the CUR-loaded MCNC-PE can effectively inhibits the human colon cancer cells growth down to 18% in the presence of EMF. The formulation also resulted in 2-fold reduction on the volume of the 3-D multicellular spheroids of HCT116 as compared to the control sample. The MCNC particle was found to be non-toxic to brine shrimp up to a concentration of 100 μg/mL. Our findings suggested that the palm-based MCNC-PE could be a promising yet effective colloidal drug delivery system for magnetic-triggered release of bioactive and therapeutics.

Matched MeSH terms: Emulsions
Fulltext Development of Polyvinylidene Fluoride Membrane via Assembly of Tannic Acid and Polyvinylpyrrolidone for Filtration of Oil/Water Emulsion

Nawi NIM, Ong Amat S, Bilad MR, Nordin NAHM, Shamsuddin N, Prayogi S, et al.

Polymers (Basel), 2021 Mar 22;13(6).
PMID: 33810126 DOI: 10.3390/polym13060976

Wastewater containing oil/water emulsion has a serious ecological impact and threatens human health. The impact worsens as its volume increases. Oil/water emulsion needs to be treated before it is discharged or reused again for processing. A membrane-based process is considered attractive in effectively treating oil/water emulsion, but progress has been dampened by the membrane fouling issue. The objective of this study is to develop polyvinylidene fluoride (PVDF) membranes customized for oil/water emulsion separation by incorporating assembly of tannic acid (TA) and polyvinylpyrrolidone (PVP) in the polymer matrix. The results show that the assembly of TA/PVP complexation was achieved as observed from the change in colour during the phase inversion and as also proven from the characterization analyses. Incorporation of the TA/PVP assembly leads to enhanced surface hydrophilicity by lowering the contact angle from 82° to 47°. In situ assembly of the TA/PVP complex also leads to enhanced clean water permeability by a factor of four as a result of enhanced mean flow pore size from 0.2 to 0.9 µm. Owing to enhanced surface chemistry and structural advantages, the optimum hydrophilic PVDF/TA/PVP membrane poses permeability of 540.18 L/(m2 h bar) for oil/water emulsion filtration, three times higher than the pristine PVDF membrane used as the reference.

Matched MeSH terms: Emulsions
Fulltext The Impact of Ethylene Glycol on Droplet Growth Inhibition in Ethylene Vinyl Acetate Emulsions

Rosdi MRH, Ahmad Razali MA, Ku Ishak KM, Ariffin A

ACS Omega, 2020 Jun 23;5(24):14473-14480.
PMID: 32596585 DOI: 10.1021/acsomega.0c01114

Pour point depressant (PPD) emulsion has been gaining attention in crude oil transportation owing to its potential to solve solidification issues that arise in cold climate environments. An emulsion system provides a wide range of temperature application that combines good shelf life and tunable thermal properties to tackle this problem. These features can be achieved by incorporating an antifreeze agent into the emulsion. One of the most commonly used antifreeze agents is ethylene glycol (EG). Hence, this study focuses on the thermal properties and droplet size growth of PPD emulsions that were aged in variable concentrations of EG solution. EG50 exhibited the lowest freezing temperature of -44 °C, while EG25 demonstrated the lowest vitrification temperature of -68.7 °C. The particle size of the emulsions underwent a significant reduction from 332.3 to 228.9 nm upon the stepwise EG concentration increment to EG50. However, when the concentration was increased to EG75, a slight increase in the emulsion particle size was observed with a recorded value of 237.8 nm. Thus, it is concluded that EG50 represents the optimum concentration for delivering the best freezing protection and producing a smaller droplet particle size.

Matched MeSH terms: Emulsions
Safety against nephrotoxicity in paclitaxel treatment: Oral nanocarrier as an effective tool in preclinical evaluation with marked in vivo antitumor activity

Choudhury H, Gorain B, Tekade RK, Pandey M, Karmakar S, Pal TK

Regul Toxicol Pharmacol, 2017 Dec;91:179-189.
PMID: 29080846 DOI: 10.1016/j.yrtph.2017.10.023

Oral paclitaxel (PTXL) formulations freed from cremophor® EL (CrEL) is always in utmost demand by the cancerous patients due to toxicities associated with the currently marketed formulation. In our previous investigation [Int. J. Pharm. 2014; 460:131], we have developed an oral oil based nanocarrier for the lipophilic drug, PTXL to target bioavailability issue and patient compliance. Here, we report in vivo antitumor activity and 28-day sub-chronic toxicity of the developed PTXL nanoemulsion. It was observed that the apoptotic potential of oral PTXL nanoemulsion significantly inhibited the growth of solid tumor (59.2 ± 7.17%; p

Matched MeSH terms: Emulsions/adverse effects; Emulsions/pharmacology; Emulsions/chemistry
Fulltext physicochemical properties of undulated surf clam (Paphia undulata) HYDROLYSATE AS AFFECTED BY DEGREE OF HYDROLYSIS

YAP JAA YEE, AMIZA MAT AMIN

UMT Journal of Undergraduate Research, 2020;2(3):15-26.
MyJurnal

This study aimed to determine the physicochemical properties of undulated surf clam (Paphia undulata) hydrolysate as affected by the degree of hydrolysis (DH). Three levels of DH of undulated surf clam hydrolysate were prepared which were DH 36.57% (without any enzymatic hydrolysis), DH 58.25% (0.5% Alcalase®; 5 min; pH 7.5; 60ºC) and DH 91.26% (1% Alcalase®; 30 min; pH 7.5; 60ºC). After protein hydrolysis, the undulated surf clam hydrolysates were centrifuged, and their supernatants were freeze-dried. This study found that the protein hydrolysate with lower DH (DH 36.57%) gave lower protein content and higher ash and fat contents compared to other samples (DH 58.25% and DH 91.26%). However, the carbohydrate content is similar in all samples (16.56-20.04%). This study also found that foaming properties (29.43-67.50%), emulsifying capacity (11.94-110.52%) and peptide solubility (57.61-94.08%) were affected by the DH. As DH increased, the emulsifying capacity decreased, while peptide solubility increased. While the foaming capacity increased with increasing DH until it reached a maximum value and level off afterwards. For colour parameters, although there were differences between L*, a* and b* values for all three samples, a fluctuating pattern was noted with DH. DH also did not affect the water-holding and oil-holding capacity of undulated surf clam hydrolysate. This study shows that certain physicochemical properties of undulated surf clam hydrolysate can be tailored by adjusting the degree of hydrolysis.

Matched MeSH terms: Emulsions
Antipsychotic Potential and Safety Profile of TPGS-Based Mucoadhesive Aripiprazole Nanoemulsion: Development and Optimization for Nose-To-Brain Delivery

Kumbhar SA, Kokare CR, Shrivastava B, Gorain B, Choudhury H

J Pharm Sci, 2021 04;110(4):1761-1778.
PMID: 33515583 DOI: 10.1016/j.xphs.2021.01.021

Delivering therapeutics to the brain using conventional dosage forms is always a challenge, thus the present study was aimed to formulate mucoadhesive nanoemulsion (MNE) of aripiprazole (ARP) for intranasal delivery to transport the drug directly to the brain. Therefore, a TPGS based ARP-MNE was formulated and optimized using the Box-Behnken statistical design. The improved in vitro release profile of the formulation was in agreement to enhanced ex vivo permeation through sheep mucous membranes with a maximum rate of permeation co-efficient (62.87 cm h-1 × 103) and flux (31.43 μg cm-2.h-1). The pharmacokinetic profile following single-dose administration showed the maximum concentration of drug in the brain (Cmax) of 15.19 ± 2.51 μg mL-1 and Tmax of 1 h in animals with ARP-MNE as compared to 10.57 ± 1.88 μg mL-1 and 1 h, and 2.52 ± 0.38 μg mL-1 and 3 h upon intranasal and intravenous administration of ARP-NE, respectively. Further, higher values of % drug targeting efficiency (96.9%) and % drug targeting potential (89.73%) of ARP-MNE through intranasal administration were investigated. The studies in Wistar rats showed no existence of extrapyramidal symptoms through the catalepsy test and forelimb retraction results. No ex vivo ciliotoxicity on nasal mucosa reflects the safety of the components and delivery tool. Further, findings on locomotor activity and hind-limb retraction test in ARP-MNE treated animals established its antipsychotic efficacy. Thus, it can be inferred that the developed ARP-MNE could effectively be explored as brain delivery cargo in the effective treatment of schizophrenia without producing any toxic manifestation.

Matched MeSH terms: Emulsions
Fulltext Efficacy of Insecticide and Bioinsecticide Ground Sprays to Control Metisa plana Walker (Lepidoptera: Psychidae) in Oil Palm Plantations, Malaysia

Salim H, Rawi CS, Ahmad AH, Al-Shami SA

Trop Life Sci Res, 2015 Dec;26(2):73-83.
PMID: 26868711 MyJurnal

The effectiveness of the synthetic insecticides trichlorfon, lambda-cyhalothrin, cypermethrin emulsion concentrated (EC) and cypermethrin emulsion water based (EW) and a bio-insecticide, Bacillus thuringiensis subsp. kurstaki (Btk), was evaluated at 3, 7, 14 and 30 days after treatment (DAT) for the control of Metisa plana larvae in an oil palm (Elaeis guineensis) plantation in Malaysia. Although all synthetic insecticides effectively reduced the larval population of M. plana, trichlorfon, lambda-cyhalothrin and cypermethrin EC were the fastest-acting. The larval population dropped below the economic threshold level (ETL) 30 days after a single application of the synthetic insecticides. Application of Btk, however, gave poor results, with the larval population remaining above the ETL post treatment. In terms of operational productivity, ground spraying using power spray equipment was time-consuming and resulted in poor coverage. Power spraying may not be appropriate for controlling M. plana infestations in large fields. Using a power sprayer, one man could cover 2-3 ha per day. Hence, power spraying is recommended during outbreaks of infestation in areas smaller than 50 ha.

Matched MeSH terms: Emulsions
Targeted drug delivery to the brain via intranasal nanoemulsion: Available proof of concept and existing challenges

Chatterjee B, Gorain B, Mohananaidu K, Sengupta P, Mandal UK, Choudhury H

Int J Pharm, 2019 Jun 30;565:258-268.
PMID: 31095983 DOI: 10.1016/j.ijpharm.2019.05.032

Intranasal delivery has shown to circumvent blood-brain-barrier (BBB) and deliver the drugs into the CNS at a higher rate and extent than other conventional routes. The mechanism of drug transport from nose-to-brain is not fully understood yet, but several neuronal pathways are considered to be involved. Intranasal nanoemulsion for brain targeting is investigated extensively. Higher brain distribution of drug after administering intranasal nanoemulsion was established by many researchers. Issues with nasomucosal clearance are solved by formulating modified nanoemulsion; for instance, mucoadhesive nanoemulsion or in situ nanoemulgel. However, no intranasal nanoemulsion for brain targeted drug delivery has been able to cross the way from 'benches to bed-side' of patients. Possibilities of toxicity by repeated administration, irregular nasal absorption during the diseased condition, use of a high amount of surfactants are few of the persisting challenges that need to overcome in coming days. Understanding the ways how current developments has solved some challenges is necessary. At the same time, the future direction of the research on intranasal nanoemulsion should be figured out based on existing challenges. This review is focused on the current developments of intranasal nanoemulsion with special emphasis on the existing challenges that would help to set future research direction.

Matched MeSH terms: Emulsions
Influence of lipolysis and droplet size on tocotrienol absorption from self-emulsifying formulations

Yap SP, Yuen KH

Int J Pharm, 2004 Aug 20;281(1-2):67-78.
PMID: 15288344

A single dose comparative bioavailability study was conducted to evaluate the bioavailability of tocotrienols from two self-emulsifying formulations, one of which produced an emulsion that readily lipolysed under in vitro condition (SES-A), while the other produced a finer dispersion with negligible lipolysis (SES-B) in comparison with that of a non-self-emulsifying formulation in soya oil. The study was conducted according to a three-way crossover design using six healthy human volunteers. Statistically significant differences were observed between the logarithmic transformed peak plasma concentration (Cmax) and total area under the plasma concentration-time curve (AUC(0-infinity)) values of both SES-A and -B compared to NSES-C indicating that SES-A and -B achieved a higher extent of absorption compared to NSES-C. Moreover, the 90% confidence interval of the AUC(0-infinity) values of both SES-A and -B over those of NSES-C were between 2-3 suggesting an increase in bioavailability of about two-three times compared to NSES-C. Both SES-A and -B also achieved a faster onset of absorption. However, both SES-A and -B had comparable bioavailability, despite the fact that SES-B was able to form emulsions with smaller droplet size. Thus, it appeared that both droplet sizes as well as the rate and extent of lipolysis of the emulsion products formed were important for enhancing the bioavailability of the tocotrienols from the self-emulsifying systems.

Matched MeSH terms: Emulsions/administration & dosage; Emulsions/pharmacokinetics; Emulsions/chemistry
Fulltext Effect of chitosan-palm stearin edible coating on the post harvest life of star fruits (Averrhoa carambola L.) stored at room temperature

Nurul Hanani, M.Z., Halimahton Zahrah, M.S., Zaibunnisa, A.H.

International Food Research Journal, 2012;19(4):1433-1438.
MyJurnal

This study was conducted to develop an edible coating containing combined hydrophilic (chitosan) and hydrophobic (palm stearin) components which demonstrated gas barrier and moisture barrier properties, respectively, to prolong the post harvest life of star fruits (Averrhoa carambola L.). The emulsions of chitosan (C) and palm stearin (S) were prepared by using different ratios of C:S which were 1:0, 1:1, 1;2, 1:3, 2:1, 3:1 and 0:1. Viscosity of emulsions was studied. The physicochemical properties of coated star fruits were also evaluated in terms of weight loss, firmness, visual appearance, oxygen concentration, carbon dioxide concentration and ethylene concentration during storage at room temperature (26-28˚C) for 18 days. The results obtained showed that coating reduced weight loss, maintained firmness and appearance, slowed down the production of respiratory gases and reduced ethylene production. The most recommended coating for star fruits was C:S of 1:1 ratio as it showed good water barrier and gas barrier properties and could extend the post harvest life of star fruits up to 20 days as compared to the control samples which had a post harvest life of 12 days.

Matched MeSH terms: Emulsions

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