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Disposition and tissue distribution of imatinib in a liposome formulation after intravenous bolus dose to mice

Moo KS, Radhakrishnan S, Teoh M, Narayanan P, Bukhari NI, Segarra I

Yao Xue Xue Bao, 2010 Jul;45(7):901-8.
PMID: 20931790

Imatinib is an efficacious anticancer drug with a spectrum of potential antitumour applications limited by poor biodistribution at therapeutic concentrations to the tissues of interest. We assess the pharmacokinetic and tissue distribution profile of imatinib in a liposome formulation. Its single dose (6.25 mg x kg(-1)) in a liposome formulation was administered iv to male mice. Imatinib concentration was measured in plasma, spleen, liver, kidney and brain using a HPLC assay. Non-compartmental pharmacokinetic approach was used to assess the disposition parameters. The plasma disposition profile was biphasic with a plateau-like second phase. The AUC(0-->infinity) was 11.24 microg x h x mL(-1), the elimination rate constant (k(el)) was 0.348 h(-1) and the elimination half life (t(1/2)) was 2.0 h. The mean residence time (MRT) was 2.59 h, V(SS) was 1.44 L x kg(-1) and clearance was 0.56 L x h x kg(-1). Liver achieved the highest tissue exposure: CMAX = 18.72 microg x mL(-1); AUC(0-->infinity)= 58.18 microg x h x mL(-1) and longest t(1/2) (4.29 h) and MRT (5.31 h). Kidney and spleen AUC(0-->infinity) were 47.98 microg x h x mL(-1) and 23.46 microg x h x mL(-1), respectively. Half-life was 1.83 h for the kidney and 3.37 h for the spleen. Imatinib penetrated into the brain reaching approximately 1 microg x g(-1). Upon correction by organ blood flow the spleen showed the largest uptake efficiency. Liposomal imatinib presented extensive biodistribution. The drug uptake kinetics showed mechanism differences amongst the tissues. These findings encourage the development of novel imatinib formulations to treat other cancers.

Matched MeSH terms: Liposomes/administration & dosage; Liposomes/chemistry*
Renal ultrastructural alterations induced by various preparations of mefenamic acid

Jarrar QB, Hakim MN, Zakaria ZA, Cheema MS, Moshawih S

Ultrastruct Pathol, 2020 Jan 02;44(1):130-140.
PMID: 31967489 DOI: 10.1080/01913123.2020.1717705

Mefenamic acid (MFA) treatment is associated with a number of cellular effects that potentiate the incidence of renal toxicity. The aim of this study is to investigate the potential ultrastructural alterations induced by various preparations of MFA (free MFA, MFA-Tween 80 liposomes, and MFA-DDC liposomes) on the renal tissues. Sprague-Dawley rats were subjected to a daily dose of MFA preparations for 28 days. Renal biopsies from all groups of rats under study were processed for transmission electron microscopic examination. The findings revealed that MFA preparations induced various ultrastructural alterations including mitochondrial injury, nuclear and lysosomal alterations, tubular cells steatosis, apoptotic activity, autophagy, and nucleophagy. These alterations were more clear in rats received free MFA, and MFA-Tween 80 liposomes than those received MFA-DDC liposomes. It is concluded that MFA-DDC liposomes are less potential to induce renal damage than free MFA and MFA-Tween 80 liposomes. Thus, MFA-DDC liposomes may offer an advantage of safe drug delivery.

Matched MeSH terms: Liposomes
Comparative ultrastructural hepatic alterations induced by free and liposome-encapsulated mefenamic acid

Jarrar QB, Hakim MN, Cheema MS, Zakaria ZA

Ultrastruct Pathol, 2017 8 23;41(5):335-345.
PMID: 28829237 DOI: 10.1080/01913123.2017.1349850

Mefenamic acid (MFA) is used as an anti-inflammatory, antinociceptive, and antipyretic agent for treatment of a wide range of pathological disorders. While the uncertainty of its safety and the poor oral bioavailability constitute the major limiting factors of its medical use, considerable efforts including liposomal encapsulation are needed to achieve maximum therapeutic advantages. The current work was conducted to investigate the ultrastructural alterations in the liver induced by free MFA and its liposomal preparation. Female Sprague-Dawley rats were treated with daily oral doses of either free MFA or MFA entrapped in Tween 80 inoculated liposomes at the concentration of 80 mg/kg for 28 days. Ultrathin sections were prepared from biopsies taken from the liver of each member of all animals under study and subjected to examination by transmission electron microscopy. The liver of rats that were exposed to liposomal MFA showed more ultrastructural alterations than the rats treated with the free drug. While both groups of rats demonstrated sinusoidal dilatation, Kupffer cell hyperplasia, mitochondrial damage, and nuclear alterations, rats treated with liposome-encapsulated MFA induced an increase in the multiple lysosomes formation, hepatocytic steatosis, and apoptotic activity than free MFA-treated rats. The ultrastructural findings of the present study indicate that the use of liposomal MFA induces more hepatic damage than the use of free MFA.

Matched MeSH terms: Liposomes/pharmacology*
Nano-drug delivery system: a promising approach against breast cancer

Malik JA, Ansari JA, Ahmed S, Khan A, Ahemad N, Anwar S

Ther Deliv, 2023 May;14(5):357-381.
PMID: 37431741 DOI: 10.4155/tde-2023-0020

Breast cancer (BC) is among the most frequent malignancies women face around the globe. Nanotherapeutics are constantly evolving to overcome the limitations of conventional diagnostic and therapeutic approaches. Nanotechnology-based nanocarriers have a higher entrapment efficiency, low cytotoxicity, greater stability and improved half-life than conventional therapy. Nano-drug delivery systems have improved pharmacokinetics and pharmacodynamics parameters because of nanomeric size. Currently, various nano-formulations are in preclinical and clinical settings for breast cancer, like polymeric nanoparticles, micelles, nanobodies, magnetic nanoparticles, liposomes, niosomes, gold-nanoparticles, dendrimers and carbon-nanotubes. This review highlights the recent advancement in developing nano-drug delivery systems for BC treatment. This review will open the gateway to researchers to understand the current approaches to developing nano-formulation and improving problems associated with conventional therapy.

Matched MeSH terms: Liposomes
Oral bioavailability enhancement of a hydrophilic drug delivered via folic acid-coupled liposomes in rats

Ling SS, Yuen KH, Magosso E, Barker SA

J Pharm Pharmacol, 2009 Apr;61(4):445-9.
PMID: 19298690 DOI: 10.1211/jpp/61.04.0005

A liposome preparation that is amenable to receptor-mediated endocytosis has been developed to enhance the oral bioavailability of poorly absorbable peptidomimetic drugs by use of folic acid as the mediator of liposomal uptake.

Matched MeSH terms: Liposomes*
In vivo studies of nanostructure-based photosensitizers for photodynamic cancer therapy

Voon SH, Kiew LV, Lee HB, Lim SH, Noordin MI, Kamkaew A, et al.

Small, 2014 Dec 29;10(24):4993-5013.
PMID: 25164105 DOI: 10.1002/smll.201401416

Animal models, particularly rodents, are major translational models for evaluating novel anticancer therapeutics. In this review, different types of nanostructure-based photosensitizers that have advanced into the in vivo evaluation stage for the photodynamic therapy (PDT) of cancer are described. This article focuses on the in vivo efficacies of the nanostructures as delivery agents and as energy transducers for photosensitizers in animal models. These materials are useful in overcoming solubility issues, lack of tumor specificity, and access to tumors deep in healthy tissue. At the end of this article, the opportunities made possible by these multiplexed nanostructure-based systems are summarized, as well as the considerable challenges associated with obtaining regulatory approval for such materials. The following questions are also addressed: (1) Is there a pressing demand for more nanoparticle materials? (2) What is the prognosis for regulatory approval of nanoparticles to be used in the clinic?

Matched MeSH terms: Liposomes
Fulltext The major allergen Der p 2 is a cholesterol binding protein

Reginald K, Chew FT

Sci Rep, 2019 02 07;9(1):1556.
PMID: 30733527 DOI: 10.1038/s41598-018-38313-9

Der p 2 is a major dust mite allergen and >80% of mite allergic individuals have specific IgE to this allergen. Although it is well characterized in terms of allergenicity, there is still some ambiguity in terms of its biological function. Three-dimensional structural analysis of Der p 2 and its close homologues indicate the presence of a hydrophobic cavity which can potentially bind to lipid molecules. In this study, we aimed to identify the potential ligand of Der p 2. Using a liposome pulldown assay, we show that recombinant Der p 2 binds to liposomes prepared with exogenous cholesterol in a dose dependent fashion. Next, an ELISA based assay using immobilized lipids was used to study binding specificities of other lipid molecules. Cholesterol was the preferred ligand of Der p 2 among 11 different lipids tested. Two homologues of Der p 2, Der f 2 and Der f 22 also bound to cholesterol. Further, using liquid chromatography-mass spectrometry (LC-MS), we confirmed that cholesterol is the natural ligand of Der p 2. Three amino acid residues of Der p 2, V104, V106 and V110 are possible cholesterol binding sites, as alanine mutations of these residues showed a significant decrease in binding (p

Matched MeSH terms: Liposomes/metabolism; Liposomes/chemistry
Effect of gamma irradiation on the physical stability of dppc liposomes

Liyana Mohd Ali Napia, Faizal Mohamed, Hur Munawar Kabir Mohd, Intan Syakeela Ahmad Bastamam, Shamellia Sharin, Norsyahidah Mohd Hidzir, et al.

Sains Malaysiana, 2018;47:1235-1240.

Unilamellar liposomes composed of dipalmitoylphosphatidylcholine (DPPC) were prepared by the reverse-phase
evaporation method and extrusion through a polycarbonate membrane filter. Liposomes at 0.7 mg/mL lipid concentration
in deionized water were exposed to gamma irradiation at a dose in the range 0.5 to 25 kGy. Gamma irradiation of
liposomes resulted in the degradation of DPPC lipids into free fatty acids, lysophosphatidylcholine and 1,2-palmitoylphosphatidic
acid (DPPA). The effect of gamma irradiation towards the physical stability of liposomes was investigated
by means of dynamic light scattering (DLS), transmission electron microscopy (TEM) and zeta potential analysis. From
the DLS analysis, no significant changes were observed in the hydrodynamic size of liposomes. TEM images indicate that
the liposomes surface became smoother and rounder as higher irradiation doses were applied. Zeta potential analysis
showed that gamma irradiation of DPPC liposomes at radiation doses as low as 0.5 kGy resulted in a drastic rise in the
magnitude of the zeta potential. The results also demonstrate that gamma irradiation of liposomes suspension enhanced
the overall stability of liposomes. Hence, it can be concluded that gamma irradiation on DPPC liposomes may potentially
produce liposomes with higher stability.

Matched MeSH terms: Unilamellar Liposomes
Fulltext Targeted Therapy for Acute Autoimmune Myocarditis with Nano-Sized Liposomal FK506 in Rats

Okuda K, Fu HY, Matsuzaki T, Araki R, Tsuchida S, Thanikachalam PV, et al.

PLoS One, 2016;11(8):e0160944.
PMID: 27501378 DOI: 10.1371/journal.pone.0160944

Immunosuppressive agents are used for the treatment of immune-mediated myocarditis; however, the need to develop a more effective therapeutic approach remains. Nano-sized liposomes may accumulate in and selectively deliver drugs to an inflammatory lesion with enhanced vascular permeability. The aims of this study were to investigate the distribution of liposomal FK506, an immunosuppressive drug encapsulated within liposomes, and the drug's effects on cardiac function in a rat experimental autoimmune myocarditis (EAM) model. We prepared polyethylene glycol-modified liposomal FK506 (mean diameter: 109.5 ± 4.4 nm). We induced EAM by immunization with porcine myosin and assessed the tissue distribution of the nano-sized beads and liposomal FK506 in this model. After liposomal or free FK506 was administered on days 14 and 17 after immunization, the cytokine expression in the rat hearts along with the histological findings and hemodynamic parameters were determined on day 21. Ex vivo fluorescent imaging revealed that intravenously administered fluorescent-labeled nano-sized beads had accumulated in myocarditic but not normal hearts on day 14 after immunization and thereafter. Compared to the administration of free FK506, FK506 levels were increased in both the plasma and hearts of EAM rats when liposomal FK506 was administered. The administration of liposomal FK506 markedly suppressed the expression of cytokines, such as interferon-γ and tumor necrosis factor-α, and reduced inflammation and fibrosis in the myocardium on day 21 compared to free FK506. The administration of liposomal FK506 also markedly ameliorated cardiac dysfunction on day 21 compared to free FK506. Nano-sized liposomes may be a promising drug delivery system for targeting myocarditic hearts with cardioprotective agents.

Matched MeSH terms: Liposomes/administration & dosage*; Liposomes/chemistry
Prospects and challenges of synergistic effect of fluorescent carbon dots, liposomes and nanoliposomes for theragnostic applications

Faghihi H, Mozafari MR, Bumrungpert A, Parsaei H, Taheri SV, Mardani P, et al.

Photodiagnosis Photodyn Ther, 2023 Jun;42:103614.
PMID: 37201772 DOI: 10.1016/j.pdpdt.2023.103614

The future of molecular-level therapy, efficient medical diagnosis, and drug delivery relies on the effective theragnostic function which can be achieved by the synergistic effect of fluorescent carbon dots (FCDs) liposomes (L) and nanoliposomes. FCDs act as the excipient navigation agent while liposomes play the role of the problem-solving agent, thus the term "theragnostic" would describe the effect of LFCDs properly. Liposomes and FCDs share some excellent at-tributes such as being nontoxic and biodegradable and they can represent a potent delivery system for pharmaceutical compounds. They enhance the therapeutic efficacy of drugs via stabilizing the encapsulated material by circumventing barriers to cellular and tissue uptake. These agents facilitate long-term drug biodistribution to the intended locations of action while eliminating systemic side effects. This manuscript reviews recent progress with liposomes, nanoliposomes (collectively known as lipid vesicles) and fluorescent carbon dots, by exploring their key characteristics, applications, characterization, performance, and challenges. An extensive and intensive understanding of the synergistic interaction between liposomes and FCDs sets out a new research pathway to an efficient and theragnostic / theranostic drug delivery and targeting diseases such as cancer.

Matched MeSH terms: Liposomes*
Fulltext Optimization of Aceclofenac Proniosomes by Using Different Carriers, Part 1: Development and Characterization

Sammour RMF, Taher M, Chatterjee B, Shahiwala A, Mahmood S

Pharmaceutics, 2019 Jul 18;11(7).
PMID: 31323799 DOI: 10.3390/pharmaceutics11070350

In the contemporary medical model world, the proniosomal system has been serving as a new drug delivery system that is considered to significantly enhance the bioavailability of drugs with low water solubility. The application of this system can improve the bioavailability of aceclofenac that is used for the relief of pain and inflammation in osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis. The present study is intended to develop an optimized proniosomal aceclofenac formula by the use of different carriers. Aceclofenac proniosomes have been prepared by slurry method, and different carriers such as maltodextrin, mannitol, and glucose were tried. Prepared proniosomes characterized by differential scanning calorimetry (DSC) analysis and Fourier transform infrared (FTIR) analysis revealed the compatibility of the drug chosen with the ingredient added, powder X-ray diffractometry (XRD) confirmed the amorphous phase of the prepared proniosomes, and finally, the surfactant layer was observed by scanning electron microscopy (SEM). Aceclofenac physical state transformations were confirmed with all formulas but maltodextrin proniosomes exhibited solubility more than other formulations. HPLC method has been used to analyze the niosomes derived from proniosomes in terms of their entrapment capability and drug content. The obtained results revealed that aceclofenac proniosomes can be successfully prepared by using different carriers.

Matched MeSH terms: Liposomes
Fulltext Influence of the Encapsulation Efficiency and Size of Liposome on the Oral Bioavailability of Griseofulvin-Loaded Liposomes

Ong SG, Ming LC, Lee KS, Yuen KH

Pharmaceutics, 2016;8(3).
PMID: 27571096 DOI: 10.3390/pharmaceutics8030025

The objective of the present study was to investigate the influence of the encapsulation efficiency and size of liposome on the oral bioavailability of griseofulvin-loaded liposomes. Griseofulvin-loaded liposomes with desired characteristics were prepared from pro-liposome using various techniques. To study the effect of encapsulation efficiency, three preparations of griseofulvin, namely, griseofulvin aqueous suspension and two griseofulvin-loaded liposomes with different amounts of griseofulvin encapsulated [i.e., F1 (32%) and F2(98%)], were administered to rats. On the other hand, to study the effect of liposome size, the rats were given three different griseofulvin-loaded liposomes of various sizes, generated via different mechanical dispersion techniques [i.e., FTS (142 nm), MS (357 nm) and NS (813 nm)], but with essentially similar encapsulation efficiencies (about 93%). Results indicated that the extent of bioavailability of griseofulvin was improved 1.7-2.0 times when given in the form of liposomes (F1) compared to griseofulvin suspension. Besides that, there was an approximately two-fold enhancement of the extent of bioavailability following administration of griseofulvin-loaded liposomes with higher encapsulation efficiency (F2), compared to those of F1. Also, the results showed that the extent of bioavailability of liposomal formulations with smaller sizes were higher by approximately three times compared to liposomal formulation of a larger size. Nevertheless, a further size reduction of griseofulvin-loaded liposome (≤400 nm) did not promote the uptake or bioavailability of griseofulvin. In conclusion, high drug encapsulation efficiency and small liposome size could enhance the oral bioavailability of griseofulvin-loaded liposomes and therefore these two parameters deserve careful consideration during formulation.

Matched MeSH terms: Liposomes
Vesicular Systems Containing Curcumin and Their Applications in Respiratory Disorders - A Mini Review

Chellappan DK, Hansbro PM, Dua K, Hsu A, Gupta G, Ng ZY, et al.

Pharm Nanotechnol, 2017;5(4):250-254.
PMID: 28786351 DOI: 10.2174/2211738505666170808094635

BACKGROUND: Vesicular systems like nanotechnology and liposomes are gaining tremendous attention lately in the field of respiratory diseases. These formulations enhance bioavailability of the drug candidate, which could be achieved through a novel drug delivery mechanism. Moreover, the therapeutic potential achieved through these systems is highly controllable over long durations of time providing better efficacy and patient compliance.
OBJECTIVE: The objective of this paper is to review the recent literature on vesicular drug delivery systems containing curcumin.
METHODS: We have collated and summarized various recent attempts made to develop different controlled release drug delivery systems containing curcumin which would be of great interest for herbal, formulation and biological scientists. There are several vesicular nanotechnological techniques involving curcumin which have been studied recently, targeting pulmonary diseases.
RESULTS: Different vesicular systems containing curcumin are being studied for their therapeutic potential in different respiratory diseases. There has been a renewed interest in formulations containing curcumin recently, primarily owing to the broad spectrum therapeutic potential of this miracle substance. Various types of formulations, containing curcumin, targeting different bodily systems have recently emerged and, nevertheless, the search for newer frontiers with this drug goes on.
CONCLUSION: This mini review, in this direction, tries to highlight the key research interventions employing vesicular systems of drug delivery with curcumin.

Matched MeSH terms: Liposomes/chemistry
An evaluation of tocotrienol ethosomes for transdermal delivery using Strat-M® membrane and excised human skin

Nair RS, Billa N, Leong CO, Morris AP

Pharm Dev Technol, 2021 Feb;26(2):243-251.
PMID: 33274672 DOI: 10.1080/10837450.2020.1860087

Tocotrienol (TRF) ethosomes were developed and evaluated in vitro for potential transdermal delivery against melanoma. The optimised TRF ethosomal size ranged between 64.9 ± 2.2 nm to 79.6 ± 3.9 nm and zeta potential (ZP) between -53.3 mV to -62.0 ± 2.6 mV. Characterisation of the ethosomes by ATR-FTIR indicated the successful formation of TRF-ethosomes. Scanning electron microscopy (SEM) images demonstrated the spherical shape of ethosomes, and the entrapment efficiencies of all the formulations were above 66%. In vitro permeation studies using full-thickness human skin showed that the permeation of gamma-T3 from the TRF ethosomal formulations was significantly higher (p

Matched MeSH terms: Liposomes
Carbon nanotubes (CNTs) based advanced dermal therapeutics: current trends and future potential

Kuche K, Maheshwari R, Tambe V, Mak KK, Jogi H, Raval N, et al.

Nanoscale, 2018 May 17;10(19):8911-8937.
PMID: 29722421 DOI: 10.1039/c8nr01383g

The search for effective and non-invasive delivery modules to transport therapeutic molecules across skin has led to the discovery of a number of nanocarriers (viz.: liposomes, ethosomes, dendrimers, etc.) in the last few decades. However, available literature suggests that these delivery modules face several issues including poor stability, low encapsulation efficiency, and scale-up hurdles. Recently, carbon nanotubes (CNTs) emerged as a versatile tool to deliver therapeutics across skin. Superior stability, high loading capacity, well-developed synthesis protocol as well as ease of scale-up are some of the reason for growing interest in CNTs. CNTs have a unique physical architecture and a large surface area with unique surface chemistry that can be tailored for vivid biomedical applications. CNTs have been thus largely engaged in the development of transdermal systems such as tuneable hydrogels, programmable nonporous membranes, electroresponsive skin modalities, protein channel mimetic platforms, reverse iontophoresis, microneedles, and dermal buckypapers. In addition, CNTs were also employed in the development of RNA interference (RNAi) based therapeutics for correcting defective dermal genes. This review expounds the state-of-art synthesis methodologies, skin penetration mechanism, drug liberation profile, loading potential, characterization techniques, and transdermal applications along with a summary on patent/regulatory status and future scope of CNT based skin therapeutics.

Matched MeSH terms: Liposomes
Fulltext Local ablation of gastric cancer by reconstituted apolipoprotein B lipoparticles carrying epigenetic drugs

Yang CL, Chao YJ, Wang HC, Hou YC, Chen CG, Chang CC, et al.

Nanomedicine, 2021 10;37:102450.
PMID: 34332115 DOI: 10.1016/j.nano.2021.102450

Epigenetic inhibitors have shown anticancer effects. Combination chemotherapy with epigenetic inhibitors has shown high effectiveness in gastric cancer clinical trials, but severe side effect and local progression are the causes of treatment failure. Therefore, we sought to develop an acidity-sensitive drug delivery system to release drugs locally to diminish unfavorable outcome of gastric cancer. In this study, we showed that, as compared with single agents, combination treatment with the demethylating agent 5'-aza-2'-deoxycytidine and HDAC inhibitors Trichostatin A or LBH589 decreased cell survival, blocked cell cycle by reducing number of S-phase cells and expression of cyclins, increased cell apoptosis by inducing expression of Bim and cleaved Caspase 3, and reexpressed tumor suppressor genes more effectively in MGCC3I cells. As a carrier, reconstituted apolipoprotein B lipoparticles (rABLs) could release drugs in acidic environments. Orally administrated embedded drugs not only showed inhibitory effects on gastric tumor growth in a syngeneic orthotopic mouse model, but also reduced the hepatic and renal toxicity. In conclusion, we have established rABL-based nanoparticles embedded epigenetic inhibitors for local treatment of gastric cancer, which have good therapeutic effects but do not cause severe side effects.

Matched MeSH terms: Liposomes/pharmacology*; Liposomes/chemistry
Curcumin-loaded niosomes downregulate mRNA expression of pro-inflammatory markers involved in asthma: an in vitro study

Jin-Ying Wong, Yin Ng Z, Mehta M, Shukla SD, Panneerselvam J, Madheswaran T, et al.

Nanomedicine (Lond), 2020 12;15(30):2955-2970.
PMID: 33252322 DOI: 10.2217/nnm-2020-0260

Aim: In this study, curcumin was encapsulated in niosomes (Nio-Curc) to increase its effectiveness for the treatment of asthma. Materials & methods: The formulation underwent various physicochemical characterization experiments, an in vitro release study, molecular simulations and was evaluated for in vitro anti-inflammatory activity. Results: Results showed that Nio-Curc had a mean particle size of 284.93 ± 14.27 nm, zeta potential of -46.93 and encapsulation efficacy of 99.62%, which demonstrates optimized physicochemical characteristics. Curcumin release in vitro could be sustained for up to 24 h. Additionally, Nio-Curc effectively reduced mRNA transcript expression of pro-inflammatory markers; IL-6, IL-8, IL-1β and TNF-α in immortalized human airway basal cell line (BCi-NS1.1). Conclusion: In this study, we have demonstrated that Nio-Curc mitigated the mRNA expression of pro-inflammatory markers in an in vitro study, which could be applied to treatment of asthma with further studies.

Matched MeSH terms: Liposomes
Co-encapsulation of gemcitabine and tocotrienols in nanovesicles enhanced efficacy in pancreatic cancer

Maniam G, Mai CW, Zulkefeli M, Fu JY

Nanomedicine (Lond), 2021 02;16(5):373-389.
PMID: 33543651 DOI: 10.2217/nnm-2020-0374

Aim: To synthesize niosomes co-encapsulating gemcitabine (GEM) and tocotrienols, and physicochemically characterize and evaluate the antipancreatic effects of the nanoformulation on Panc 10.05, SW 1990, AsPC-1 and BxPC-3 cells. Materials & methods: Niosomes-entrapping GEM and tocotrienols composed of Span 60, cholesterol and D-α-tocopheryl polyethylene glycol 1000 succinate were produced by Handjani-Vila and film hydration methods. Results: The film hydration produced vesicles measuring 161.9 ± 0.5 nm, approximately 50% smaller in size than Handjani-Vila method, with maximum entrapment efficiencies of 20.07 ± 0.22% for GEM and 34.52 ± 0.10% for tocotrienols. In Panc 10.05 cells, GEM's antiproliferative effect was enhanced 2.78-fold in combination with tocotrienols. Niosomes produced a significant ninefold enhancement in cytotoxicity of the combination, supported by significantly higher cellular uptake of GEM in the cells. Conclusion: This study is a proof of concept on the synthesis of dual-drug niosomes and their efficacy on pancreatic cancer cells in vitro.

Matched MeSH terms: Liposomes
Tumor regression and modulation of gene expression via tumor-targeted tocotrienol niosomes

Tan DM, Fu JY, Wong FS, Er HM, Chen YS, Nesaretnam K

Nanomedicine (Lond), 2017 Oct;12(20):2487-2502.
PMID: 28972460 DOI: 10.2217/nnm-2017-0182

AIM: To develop 6-O-palmitoyl-ascorbic acid-based niosomes targeted to transferrin receptor for intravenous administration of tocotrienols (T3) in breast cancer.
MATERIALS & METHODS: Niosomes were prepared using film hydration and ultrasonication methods. Transferrin was coupled to the surface of niosomes via chemical linker. Nanovesicles were characterized for size, zeta potential, morphology, stability and biological efficacy.
RESULTS: When evaluated in MDA-MB-231 cells, entrapment of T3 in niosomes caused 1.5-fold reduction in IC50 value compared with nonformulated T3. In vivo, the average tumor volume of mice treated with tumor-targeted niosomes was 12-fold lower than that of untreated group, accompanied by marked downregulation of three genes involved in metastasis.
CONCLUSION: Findings suggested that tumor-targeted niosomes served as promising delivery system for T3 in cancer therapy.

Matched MeSH terms: Liposomes/chemistry*
Molecular insights and therapeutic implications of nanoengineered dietary polyphenols for targeting lung cancer: part II

Das SS, Tambe S, Prasad Verma PR, Amin P, Singh N, Singh SK, et al.

Nanomedicine (Lond), 2022 Oct;17(23):1799-1816.
PMID: 36636965 DOI: 10.2217/nnm-2022-0117

Flavonoids represent a major group of polyphenolic compounds. Their capacity to inhibit tumor proliferation, cell cycle, angiogenesis, migration and invasion is substantially responsible for their chemotherapeutic activity against lung cancer. However, their clinical application is limited due to poor aqueous solubility, low permeability and quick blood clearance, which leads to their low bioavailability. Nanoengineered systems such as liposomes, nanoparticles, micelles, dendrimers and nanotubes can considerably enhance the targeted action of the flavonoids with improved efficacy and pharmacokinetic properties, and flavonoids can be successfully translated from bench to bedside through various nanoengineering approaches. This review addresses the therapeutic potential of various flavonoids and highlights the cutting-edge progress in the nanoengineered systems that incorporate flavonoids for treating lung cancer.

Matched MeSH terms: Liposomes/therapeutic use

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