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Advanced nanoscale carrier-based approaches to overcome biopharmaceutical issues associated with anticancer drug 'Etoposide'

Choudhury H, Maheshwari R, Pandey M, Tekade M, Gorain B, Tekade RK

Mater Sci Eng C Mater Biol Appl, 2020 Jan;106:110275.
PMID: 31753398 DOI: 10.1016/j.msec.2019.110275

Etoposide (ETS), topoisomerase-II inhibitor, is a first-line anticancer therapeutics used in diverse cancer types. However, the therapeutic potential of this molecule has mainly impeded due to its detrimental toxicity profile, unfavorable rejection by the cancer cells due to P-glycoprotein (P-gp) efflux activity, and rapid hepatic clearance through extensive metabolism by Cytochrome-P450. To increase the therapeutic potency without significant adverse effects, the implication of novel ETS-nanoformulation strategies have recommended mainly. Nanomedicine based nanoformulation approaches based on nanoparticles (NPs), dendrimers, carbon-nanotubes (CNTs), liposomes, polymeric micelles, emulsions, dendrimers, solid-lipid NPs, etc offers immense potential opportunities to improve the therapeutic potential of pharmaceutically problematic drugs. This review provides an up-to-date argument on the work done in the field of nanomedicine to resolve pharmacokinetic and pharmacodynamic issues associated with ETS. The review also expounds the progress in regards to the regulatory, patenting and clinical trials related to the innovative formulation aspects of ETS.

Matched MeSH terms: Solubility
Processing and analysis of chitosan nanocomposites reinforced with chitin whiskers and tannic acid as a crosslinker

Rubentheren V, Ward TA, Chee CY, Tang CK

Carbohydr Polym, 2015 Jan 22;115:379-87.
PMID: 25439908 DOI: 10.1016/j.carbpol.2014.09.007

Chitosan film reinforced with nano-sized chitin whiskers and crosslinked using tannic acid was synthesized by the casting-vaporation method. The mechanical and physicochemical properties of several film samples (consisting of different ratio of chitin and tannic acid) were compared with neat chitosan. Tensile tests show that the addition of chitin improves the nanocomposite films mechanical properties up to 137% compared to neat chitosan, but this is slightly degraded when tannic acid is introduced. However, tannic acid and chitin whisker content greatly reduced moisture content by 294% and water solubility by 13%. Transmission electron microscopy (TEM) and Fourier-transform-infrared spectroscopy (FTIR) were used to investigate the morphology and molecular interaction of film. X-ray diffraction results indicated that the samples with chitin whiskers had a more rigid structure. The addition of tannic acid changed the structure into an anhydrous crystalline conformation when compared to neat chitosan film.

Matched MeSH terms: Solubility
Solubilization of beclomethasone dipropionate in sterically stabilized phospholipid nanomicelles (SSMs): physicochemical and in vitro evaluations

Sahib MN, Abdulameer SA, Darwis Y, Peh KK, Tan YT

Drug Des Devel Ther, 2012;6:29-42.
PMID: 22393583

The local treatment of lung disorders such as asthma and chronic obstructive pulmonary disease via pulmonary drug delivery offers many advantages over oral or intravenous routes of administration. This is because direct deposition of a drug at the diseased site increases local drug concentrations, which improves the pulmonary receptor occupancy and reduces the overall dose required, therefore reducing the side effects that result from high drug doses. From a clinical point of view, although jet nebulizers have been used for aerosol delivery of water-soluble compounds and micronized suspensions, their use with hydrophobic drugs has been inadequate.

Matched MeSH terms: Solubility
Fulltext Rehydrated sterically stabilized phospholipid nanomicelles of budesonide for nebulization: physicochemical characterization and in vitro, in vivo evaluations

Sahib MN, Darwis Y, Peh KK, Abdulameer SA, Tan YT

Int J Nanomedicine, 2011;6:2351-66.
PMID: 22072872 DOI: 10.2147/IJN.S25363

Inhaled corticosteroids provide unique systems for local treatment of asthma or chronic obstructive pulmonary disease. However, the use of poorly soluble drugs for nebulization has been inadequate, and many patients rely on large doses to achieve optimal control of their disease. Theoretically, nanotechnology with a sustained-release formulation may provide a favorable therapeutic index. The aim of this study was to determine the feasibility of using sterically stabilized phospholipid nanomicelles of budesonide for pulmonary delivery via nebulization.

Matched MeSH terms: Solubility
Fulltext Exploring the potential of a highly compressible microcrystalline cellulose as novel tabletting excipient in the compaction of extended-release coated pellets containing an extremely water-soluble model drug

Zeeshan F, Peh KK, Tan YT

AAPS PharmSciTech, 2009;10(3):850-7.
PMID: 19554454 DOI: 10.1208/s12249-009-9278-2

Compaction of controlled-release coated pellets into tablets is challenging because of the fusion of pellets and the rupturing of coated film. The difficulty in compaction intensifies with the use of extremely water-soluble drugs. Therefore, the present study was conducted to prepare and compact pellets containing pseudoephedrine hydrochloride as an extremely water-soluble model drug. The pellets were produced using an extrusion-spheronization technique. The drug-loaded pellets were coated to extend the drug release up to 12-h employing various polymers, and then they were compressed into tablets using microcrystalline cellulose Ceolus KG-801 as a novel tabletting excipient. The in vitro drug release studies of coated pellets and tablets were undertaken using the USP basket method in dissolution test apparatus I. The amount of drug released was analyzed at a wavelength of 215 nm. The combined coatings of hydroxypropyl methylcellulose and Kollicoat SR-30D yielded 12-h extended-release pellets with drug release independent of pH of dissolution medium following zero-order kinetics. The drug release from the tablets prepared using inert Celous KG-801 granules as tabletting excipient was found faster than that of coated pellets. However, a modification in drug release rate occurred with the incorporation of inert Ceolus KG-801 pellets. The drug dissolution profile from tablets containing 40% w/w each of coated pellets and inert granules along with 20% w/w inert pellets was found to be closely similar to that of coated pellets. Furthermore, the friability, tensile strength, and disintegration time of the tablets were within the USP specifications.

Matched MeSH terms: Solubility
Design of a 24-hour controlled porosity osmotic pump system containing PVP: formulation variables

Yakubu R, Peh KK, Tan YT

Drug Dev Ind Pharm, 2009 Dec;35(12):1430-8.
PMID: 19929202 DOI: 10.3109/03639040902988566

The purpose of this study was to design a 24-hour controlled porosity osmotic pump system that utilizes polyvinyl pyrrolidone (PVP) as an osmotic-suspending/release retarding agent of drugs.

Matched MeSH terms: Solubility
Solubility of core materials in aqueous polymeric solution effect on microencapsulation of curcumin

Aziz HA, Peh KK, Tan YT

Drug Dev Ind Pharm, 2007 Nov;33(11):1263-72.
PMID: 18058323

Curcumin, the main active constituent of turmeric herb (Curcuma longa L.) have been reported to possess many medicinal values. The application of curcumin in dermatological preparations is limited by their intense yellow color property, which stains the fabric and skin. The objectives of this study were to reduce the color staining effect and enhance the stability of curcumin via microencapsulation using gelatin simple coacervation method. As for curcumin, ethanol and acetone were used as coacervating solvents. Curcumin was dispersed in ethanol while dissolved in acetone. Irrespective of the types of coacervating solvents used, microencapsulation resolved the color-staining problem and enhanced the flow properties and photo-stability of curcumin. Nevertheless, it was found that more spherical curcumin microcapsules with higher yield, higher curcumin loading, and higher entrapment efficiency were obtained with acetone than ethanol. The in vitro release of curcumin after microencapsulation was slightly prolonged. Further evaluation of the effects of solubility of core materials in coacervating solvent or polymeric aqueous solution using six different drug compounds, namely, ketoconazole, ketoprofen, magnesium stearate, pseudoephedrine HCl, diclofenac sodium, and paracetamol, suggested that the solubility of core materials in aqueous polymeric solution determined the successful formation of microcapsules. Microcapsules could only be formed if the core materials were not dissolved in the aqueous polymeric solution while the core materials could either be dissolved or dispersed in the coacervating solvent. In summary, microencapsulation not only circumvents the color-staining problem but also improved the stability and flowability of curcumin. The solubility of core material in aqueous polymeric solution plays a pivotal role in determining the successful formation of microcapsules.

Matched MeSH terms: Solubility
Functional properties and utilization of Artocarpus heterophyllus Lam seed starch from new species in China

Zhang Y, Hu M, Zhu K, Wu G, Tan L

Int J Biol Macromol, 2018 Feb;107(Pt B):1395-1405.
PMID: 29017887 DOI: 10.1016/j.ijbiomac.2017.10.001

Jackfruit is now receiving extensive attention as a new source of starch. However, jackfruit seeds are discarded as waste, although they are rich in starch. The functional properties of the starches were investigated from new Chinese jackfruit species. All the starches have a high amylose (26.56-38.34%) with a potential to become functional foods rich in resistant starch. The jackfruit starches varied from trigonal and tetragonal, round to semi-oval/bell shapes and showed significant variations in particle sizes (5.53-14.46μm). These variations led to significant differences in their functional properties, and significant correlations were found in their pasting, thermal, crystal and texture parameters. Hierarchical cluster analysis sorted the samples into three groups of 1) Malaysia 8 (M8) and ZhenZhu (ZZ); 2) Malaysia 2, Malaysia 3 and Malaysia 4, (M2, M3, M4); and 3) Xiangyinsuo 11, Xiangyinsuo 4, Xiangyinsuo 3 and Xiangyinsuo 2 (X11, X4, X3, X2). The first group could be used as food thickening or gelling agents. The second group could be applied in glutinous foods. The third group make them suitable for fillings in confectionery or weaning foods.

Matched MeSH terms: Solubility
Fulltext Production of spray-dried honey jackfruit (Artocarpus heterophyllus) powder from enzymatic liquefied puree

Wong CW, Tan HH

J Food Sci Technol, 2017 Feb;54(2):564-571.
PMID: 28242955 DOI: 10.1007/s13197-017-2501-3

This paper presents the enzymatic liquefaction process for honey jackfruit optimized with Pectinex® Ultra SP-L and Celluclast® 1.5 L individually or in combinations at different concentrations (0-2.5% v/w) and incubation time (0-2.5 h). Treatment with combinations of enzymes showed a greater effect in the reduction of viscosity (83.9-98.8%) as compared to single enzyme treatment (64.8-87.3%). The best parameter for enzymatic liquefaction was obtained with 1.0% (v/w) Pectinex® Ultra SP-L and 0.5% (v/w) Celluclast® 1.5 L for 1.5 h. Spray drying process was carried out using different inlet temperatures (140-180 °C) and maltodextrin concentrations (10-30% w/w). Results indicated that the spray-dried honey jackfruit powder produced at 160 °C with 30% w/w maltodextrin gave the highest product yield (66.90%) with good powder qualities in terms of water activity, solubility, moisture content, hygroscopicity, color and bulk density. The spray-dried honey jackfruit powder could potentially be incorporated into various food products.

Matched MeSH terms: Solubility
Optimization of processing parameters for the preparation of phytosterol microemulsions by the solvent displacement method

Leong WF, Che Man YB, Lai OM, Long K, Misran M, Tan CP

J Agric Food Chem, 2009 Sep 23;57(18):8426-33.
PMID: 19694442 DOI: 10.1021/jf901853y

The purpose of this study was to optimize the parameters involved in the production of water-soluble phytosterol microemulsions for use in the food industry. In this study, response surface methodology (RSM) was employed to model and optimize four of the processing parameters, namely, the number of cycles of high-pressure homogenization (1-9 cycles), the pressure used for high-pressure homogenization (100-500 bar), the evaporation temperature (30-70 degrees C), and the concentration ratio of microemulsions (1-5). All responses-particle size (PS), polydispersity index (PDI), and percent ethanol residual (%ER)-were well fit by a reduced cubic model obtained by multiple regression after manual elimination. The coefficient of determination (R(2)) and absolute average deviation (AAD) value for PS, PDI, and %ER were 0.9628 and 0.5398%, 0.9953 and 0.7077%, and 0.9989 and 1.0457%, respectively. The optimized processing parameters were 4.88 (approximately 5) homogenization cycles, homogenization pressure of 400 bar, evaporation temperature of 44.5 degrees C, and concentration ratio of microemulsions of 2.34 cycles (approximately 2 cycles) of high-pressure homogenization. The corresponding responses for the optimized preparation condition were a minimal particle size of 328 nm, minimal polydispersity index of 0.159, and <0.1% of ethanol residual. The chi-square test verified the model, whereby the experimental values of PS, PDI, and %ER agreed with the predicted values at a 0.05 level of significance.

Matched MeSH terms: Solubility
Fulltext Impact of Quercetin Encapsulation with Added Phytosterols on Bilayer Membrane and Photothermal-Alteration of Novel Mixed Soy Lecithin-Based Liposome

Toopkanloo SP, Tan TB, Abas F, Alharthi FA, Nehdi IA, Tan CP

Nanomaterials (Basel), 2020 Dec 05;10(12).
PMID: 33291386 DOI: 10.3390/nano10122432

This study used highly lipophilic agents with an aim to increase the oxidant inhibitory activity and enhance photothermal stability of a novel mixed soy lecithin (ML)-based liposome by changing the composition of formulation within the membrane. Specifically, the development and optimization of the liposome intended for improving Trolox equivalent antioxidant capacity (TEAC) value and %TEAC loss was carried out by incorporating a natural antioxidant, quercetin (QU). In this context, a focus was set on QU encapsulation in ML-based liposomes and the concentration-dependent solubility of QU was investigated and calculated as encapsulation efficiency (EE). To explore the combined effects of the incorporation of plant sterols on the integrity and entrapment capacity of mixed phospholipid vesicles, conjugation of two types of phytosterols (PSs), namely β-sitosterol (βS) and stigmasterol (ST), to mixed membranes at different ratios was also performed. The EE measurement revealed that QU could be efficiently encapsulated in the stable ML-based liposome using 0.15 and 0.1 g/100 mL of βS and ST, respectively. The aforementioned liposome complex exhibited a considerable TEAC (197.23%) and enhanced TEAC loss (30.81%) when exposed to ultraviolet (UV) light (280-320 nm) over a 6 h duration. It appeared that the presence and type of PSs affect the membrane-integration characteristics as well as photodamage transformation of the ML-based liposome. The association of QU with either βS or ST in the formulation was justified by their synergistic effects on the enhancement of the EE of liposomes. Parallel to this, it was demonstrated that synergistic PS effects could be in effect in the maintenance of membrane order of the ML-based liposome. The findings presented in this study provided useful information for the development and production of stable QU-loaded ML-based liposomes for food and nutraceutical applications and could serve as a potential mixed lipids-based delivery system in the disease management using antioxidant therapy.

Matched MeSH terms: Solubility
Fulltext Emulsion formulation optimization and characterization of spray-dried κ-carrageenan microparticles for the encapsulation of CoQ10

Chan SW, Mirhosseini H, Taip FS, Ling TC, Nehdi IA, Tan CP

Food Sci Biotechnol, 2016;25(Suppl 1):53-62.
PMID: 30263486 DOI: 10.1007/s10068-016-0098-3

The present study is aimed to prepare κ-carrageenan microparticles for the encapsulation of model drug, coenzyme Q10 (CoQ10). A face-centered central composite design was employed to study the effects of three different formulation variables (κ-carrageenan, emulsifier, and oil). The powder yield was found inversely affected by the κ-carrageenan and oil concentration. The encapsulation efficiency was maximized in the region of the middle level κ-carrageenan concentration, the high level emulsifier concentration, and the low level oil concentration. The emulsifier concentration was the most influential variable on the particle size of powder. The optimal formulation was reported as 0.91% (w/v) κ-carrageenan concentration, 0.64% (w/v) emulsifier, and 1.0% (w/w) oil. Both differential scanning colorimeter and X-ray diffraction analyses proved that incorporation of CoQ10 into κ- carrageenan microcapsules resulted in amorphous powder with significantly (p<0.05) higher water solubility compared to pure CoQ10 and physical mixture in the crystalline form.

Matched MeSH terms: Solubility
Producing a lycopene nanodispersion: Formulation development and the effects of high pressure homogenization

Shariffa YN, Tan TB, Uthumporn U, Abas F, Mirhosseini H, Nehdi IA, et al.

Food Res Int, 2017 11;101:165-172.
PMID: 28941679 DOI: 10.1016/j.foodres.2017.09.005

The aim of this study was to develop formulations to produce lycopene nanodispersions and to investigate the effects of the homogenization pressure on the physicochemical properties of the lycopene nanodispersion. The samples were prepared by using emulsification-evaporation technique. The best formulation was achieved by dispersing an organic phase (0.3% w/v lycopene dissolved in dichloromethane) in an aqueous phase (0.3% w/v Tween 20 dissolved in deionized water) at a ratio of 1:9 by using homogenization process. The increased level of homogenization pressure to 500bar reduced the particle size and lycopene concentration significantly (p<0.05). Excessive homogenization pressure (700-900bar) resulted in large particle sizes with high dispersibility. The zeta potential and turbidity of the lycopene nanodispersion were significantly influenced by the homogenization pressure. The results from this study provided useful information for producing small-sized lycopene nanodispersions with a narrow PDI and good stability for application in beverage products.

Matched MeSH terms: Solubility
Relating in vitro/in vivo data of two controlled-release metformin formulations

Yuen KH, Peh KK, Tan BL

Drug Dev Ind Pharm, 1999 May;25(5):613-8.
PMID: 10219530

This study was conducted to compare the bioavailability of two controlled-release metformin preparations (Diabetmin Retard and Glucophage Retard) and also to correlate the in vitro and in vivo data obtained with the two preparations. Twelve healthy volunteers participated in the study, conducted according to a completely randomized, two-way crossover design. The preparations were compared using area under the plasma concentration-time curve AUC0-infinity, time to reach peak plasma concentration Tmax, and peak plasma concentration Cmax, while correlation was determined between in vitro release and in vivo absorption. Diabetmin Retard demonstrated a slower rate of in vitro release, but a faster rate of in vivo absorption than Glucophage Retard. However, the in vivo absorption of both products was found to be slower than that of drug released in vitro. A satisfactory relationship could be established between the in vitro and in vivo results, but there was no rank order correlation. No statistically significant difference was observed between the two preparations in the parameters AUC0-infinity and Cmax. However, a slight but statistically significant difference was observed between the Tmax values, but it may not be therapeutically significant. Moreover, the 90% confidence interval for the ratio of the logarithmic transformed AUC0-infinity values, as well as the logarithmic transformed Cmax values, of Diabetmin Retard over those of Glucophage Retard was within the acceptance criteria of 0.80-1.25.

Matched MeSH terms: Solubility
Microwave modified non-crosslinked pectin films with modulated drug release

Anuar NK, Wong TW, Taib MN

Pharm Dev Technol, 2012 Jan-Feb;17(1):110-7.
PMID: 20958167 DOI: 10.3109/10837450.2010.522584

The effects of microwave on drug release properties of pectin films carrying sulfanilamide (SN-P), sulfathiazole (ST-P) and sulfamerazine (SM-P) of high to low aqueous solubilities were investigated. These films were prepared by solvent evaporation technique and treated by microwave at 80 W for 5-40 min. Their profiles of drug dissolution, drug content, matrix interaction and matrix crystallinity were determined by drug dissolution testing, drug content assay, differential scanning calorimetry, X-ray diffractometry and scanning electron microscopy techniques. Microwave induced an increase in matrix amorphousness but lower drug release propensity with a greater retardation extent in SN-P films, following a rise in strength of matrix interaction. A gain in amorphous structure does not necessarily increase the drug release of film. Microwave can possibly retard drug release of pectin film carrying water-soluble drug through modulating its state of matrix interaction.

Matched MeSH terms: Solubility
Fulltext Bioavailability of Eurycomanone in Its Pure Form and in a Standardised Eurycoma longifolia Water Extract

Ahmad N, Samiulla DS, Teh BP, Zainol M, Zolkifli NA, Muhammad A, et al.

Pharmaceutics, 2018 Jul 11;10(3).
PMID: 29997335 DOI: 10.3390/pharmaceutics10030090

Eurycoma longifolia is one of the commonly consumed herbal preparations and its major chemical compound, eurycomanone, has been described to have antimalarial, antipyretic, aphrodisiac, and cytotoxic activities. Today, the consumption of E. longifolia is popular through the incorporation of its extract in food items, most frequently in drinks such as tea and coffee. In the current study, the characterisation of the physicochemical and pharmacokinetic (PK) attributes of eurycomanone were conducted via a series of in vitro and in vivo studies in rats and mice. The solubility and chemical stability of eurycomanone under the conditions of the gastrointestinal tract environment were determined. The permeability of eurycomanone was investigated by determining its distribution coefficient in aqueous and organic environments and its permeability using the parallel artificial membrane permeability assay system and Caco-2 cultured cells. Eurycomanone's stability in plasma and its protein-binding ability were measured by using an equilibrium dialysis method. Its stability in liver microsomes across species (mice, rat, dog, monkey, and human) and rat liver hepatocytes was also investigated. Along with the PK evaluations of eurycomanone in mice and rats, the PK parameters for the Malaysian Standard (MS: 2409:201) standardised water extract of E. longifolia were also evaluated in rats. Both rodent models showed that eurycomanone in both the compound form and extract form had a half-life of 0.30 h. The differences in the bioavailability of eurycomanone in the compound form between the rats (11.8%) and mice (54.9%) suggests that the PK parameters cannot be directly extrapolated to humans. The results also suggest that eurycomanone is not readily absorbed across biological membranes. However, once absorbed, the compound is not easily metabolised (is stable), hence retaining its bioactive properties, which may be responsible for the various reported biological activities.

Matched MeSH terms: Solubility
Fulltext Determining the Effect of Centrifugal Force on the Desired Growth and Properties of PCPDTBT as p-Type Nanowires

Doris M, Aziz F, Alhummiany H, Bawazeer T, Alsenany N, Mahmoud A, et al.

Nanoscale Res Lett, 2017 Dec;12(1):67.
PMID: 28116608 DOI: 10.1186/s11671-017-1851-0

In this study, low-bandgap polymer poly{[4,4-bis(2-ethylhexyl)-cyclopenta-(2,1-b;3,4-b')dithiophen]-2,6-diyl-alt-(2,1,3-benzothiadiazole)-4,7-diyl} (PCPDTBT) nanostructures have been synthesized via a hard nanoporous alumina template of centrifugal process. Centrifuge has been used to infiltrate the PCPDTBT solution into the nanoporous alumina by varying the rotational speeds. The rotational speed of centrifuge is directly proportional to the infiltration force that penetrates into the nanochannels of the template. By varying the rotational speed of centrifuge, different types of PCPDTBT nanostructures are procured. Infiltration force created during the centrifugal process has been found a dominant factor in tuning the morphological, optical, and structural properties of PCPDTBT nanostructures. The field emission scanning electron microscopy (FESEM) images proved the formation of nanotubes and nanowires. The energy-dispersive X-ray spectroscope (EDX) analysis showed that the nanostructures were composed of PCPDTBT with complete dissolution of the template.

Matched MeSH terms: Solubility
Targeted drug delivery systems: synthesis and in vitro bioactivity and apoptosis studies of gemcitabine-carbon dot conjugates

Yunus U, Zulfiqar MA, Ajmal M, Bhatti MH, Chaudhry GE, Muhammad TST, et al.

Biomed Mater, 2020 09 26;15(6):065004.
PMID: 32442994 DOI: 10.1088/1748-605X/ab95e1

Gemcitabine (GEM) is used to treat various cancers such as breast, pancreatic, non-small lung, ovarian, bladder, and cervical cancers. GEM, however, has the problem of non-selectivity. Water-soluble, fluorescent, and mono-dispersed carbon dots (CDs) were fabricated by ultrasonication of sucrose. The CDs were further conjugated with GEM through amide linkage. The physical and morphological properties of these carbon dot-gemcitabine (CD-GEM) conjugates were determined using different analytical techniques. In vitro cytotoxicity and apoptosis studies of CD-GEM conjugates were evaluated by various bioactivity assays on human cell lines, MCF-7 (human breast adenocarcinoma), and HeLa (cervical cancer) cell lines. The results of kinetic studies have shown a maximum drug loading efficacy of 17.0 mg of GEM per 50.0 mg of CDs. The CDs were found biocompatible, and the CD-GEM conjugates exhibited excellent bioactivity and exerted potent cytotoxicity against tumor cells with an IC50 value of 19.50 μg ml-1 in HeLa cells, which is lower than the IC50 value of pure GEM (∼20.10 μg ml-1). In vitro studies on CD-GEM conjugates demonstrated the potential to replace the conventional administration of GEM. CD-GEM conjugates are more stable, have a higher aqueous solubility, and are more cytotoxic as compared to GEM alone. The CD-GEM conjugates show reduced side effects in the normal cells along with excellent cellular uptake. Hence, CD-GEM conjugates are more selective toward cancerous cell lines as compared to non-cancerous cells. Also, the CD-GEM conjugates successfully induced early and late apoptosis in cancer cell lines and might be effective and safe to use for in vivo applications.

Matched MeSH terms: Solubility
Improving oral bioavailability of medicinal herbal compounds through lipid-based formulations - A Scoping Review

Tan OJ, Loo HL, Thiagarajah G, Palanisamy UD, Sundralingam U

Phytomedicine, 2021 Sep;90:153651.
PMID: 34340903 DOI: 10.1016/j.phymed.2021.153651

BACKGROUND: Although numerous medicinal herbal compounds demonstrate promising therapeutic potential, their clinical application is often limited by their poor oral bioavailability. To circumvent this barrier, various lipid-based herbal formulations have been developed and trialled with promising experimental results.
PURPOSE: This scoping review aims to describe the effect of lipid-based formulations on the oral bioavailability of herbal compounds.
METHODS: A systematic search was conducted across three electronic databases (Medline, Embase and Cochrane Library) between January 2010 and January 2021 to identify relevant studies. The articles were rigorously screened for eligibility. Data from eligible studies were then extracted and collated for synthesis and descriptive analysis using Covidence.
RESULTS: A total of 109 studies were included in the present review: 105 animal studies and four clinical trials. Among the formulations investigated, 50% were emulsions, 34% lipid particulate systems, 12% vesicular systems, and 4% were other types of lipid-based formulations. Within the emulsion system classification, self-emulsifying drug delivery systems were observed to produce the best improvements in oral bioavailability, followed by mixed micellar formulations. The introduction of composite lipid-based formulations and the use of uncommon surfactants such as sodium oleate in emulsion preparation was shown to consistently enhance the bioavailability of herbal compounds with poor oral absorption. Interestingly, the lipid-based formulations of magnesium lithospermate B and Pulsatilla chinensis produced an absolute bioavailability greater than 100% indicating the possibility of prolonged systemic circulation. With respect to chemical conjugation, D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) was the most frequently used and significantly improved the bioavailability of its phytoconstituents.
CONCLUSION: Our findings suggest that there is no distinct lipid-based formulation superior to the other. Bioavailability improvements were largely dependent on the nature of the phytoconstituents. This scoping review, however, provided a detailed summary of the most up-to-date evidence on phytoconstituents formulated into lipid preparations and their oral bioavailability. We conclude that a systematic review and meta-analysis between bioavailability improvements of individual phytoconstituents (such as kaempferol, morin and myricetin) in various lipid-based formulations will provide a more detailed association. Such a review will be highly beneficial for both researchers and herbal manufacturers.

Matched MeSH terms: Solubility
Synthesis and anticancer activity of novel water soluble benzimidazole carbamates

Cheong JE, Zaffagni M, Chung I, Xu Y, Wang Y, Jernigan FE, et al.

Eur J Med Chem, 2018 Jan 20;144:372-385.
PMID: 29288939 DOI: 10.1016/j.ejmech.2017.11.037

Metastases account for more than 90% of all cancer deaths and respond poorly to most therapies. There remains an urgent need for new therapeutic modalities for the treatment of advanced metastatic cancers. The benzimidazole methylcarbamate drugs, commonly used as anti-helmitics, have been suggested to have anticancer activity, but progress has been stalled by their poor water solubility and poor suitability for systemic delivery to disseminated cancers. We synthesized and characterized the anticancer activity of novel benzimidazoles containing an oxetane or an amine group to enhance solubility. Among them, the novel oxetanyl substituted compound 18 demonstrated significant cytotoxicity toward a variety of cancer cell types including prostate, lung, and ovarian cancers with strong activity toward highly aggressive cancer lines (IC50: 0.9-3.8 μM). Compound 18 achieved aqueous solubility of 361 μM. In a mouse xenograft model of a highly metastatic human prostate cancer, compound 18 (30 mg/kg) significantly inhibited the growth of established tumors (T/C: 0.36) without noticeable toxicity.

Matched MeSH terms: Solubility

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