Reverse Phase Evaporation Technique Research Articles

Enhancement of oral bioavailability of ibrutinib using a liposil nanohybrid delivery system.

Liposils, synthesized via the liposome templating method, offer a promising strategy for enhancing liposome stability by employing a silica coating. This study focuses on the development of nanocarriers utilizing silica-coated nanoliposomes for encapsulating the poorly water-soluble drug, ibrutinib. Ibrutinib-loaded nanoliposomes were meticulously formulated using the reverse-phase evaporation technique, serving as templates for silica coating, resulting in spherical liposils with an average size of approximately 240 nanometers. Comprehensive characterization of the liposil's physical and chemical properties was conducted using various analytical methods, including dynamic light scattering, transmission electron microscopy, Fourier-transform infrared spectroscopy, and X-ray diffraction analysis. Liposils demonstrated superior performance compared to ibrutinib-loaded nanoliposomes, showing sustained drug release profiles in simulated intestinal fluids and resistance to simulated gastric fluid, as confirmed by dissolution studies. Moreover, ibrutinib liposils exhibited a significant increase in half-life (4.08-fold) and notable improvement in bioavailability (3.12-fold) compared to ibrutinib suspensions, as determined by pharmacokinetic studies in rats. These findings underscore the potential of liposils as nanocarriers for orally delivering poorly water-soluble drugs, offering enhanced stability and controlled release profiles, thereby improving bioavailability prospects and therapeutic efficacy. This approach holds promise for addressing challenges associated with the oral administration of drugs with limited solubility, thereby advancing drug delivery technologies and clinical outcomes in pharmaceutical research and development.

Liposomal Drug Delivery against Helicobacter pylori Using Furazolidone and N-Acetyl Cysteine in Augmented Therapy.

Helicobacter pylori (H. pylori) infection is a significant global health concern, affecting approximately 50% of the world's population and leading to gastric ulcers, gastritis, and gastric cancer. The increase in antibiotic resistance has compromised the efficacy of existing therapeutic regimens, necessitating novel approaches for effective eradication. This study aimed to develop a targeted liposomal drug delivery system incorporating furazolidone and N-acetylcysteine (NAC) to enhance mucopenetration and improve Helicobacter pylori eradication. Liposomes were formulated with furazolidone, NAC, and Pluronic F-127 using a modified reverse-phase evaporation technique. The formulations were categorized based on charge as neutral, negative, and positive and tested for mucopenetration using a modified silicon tube method with coumarin-6 as a fluorescent marker. The encapsulation efficiency and particle size were analyzed using HPLC and an Izon q-nano particle size analyzer. The results indicated that charged liposomes showed a higher encapsulation efficiency than neutral liposomes with Pluronic F-127. Notably, combining furazolidone with 1% NAC achieved complete eradication of H. pylori in 2.5 h, compared to six hours without NAC. The findings of this study suggest that incorporating NAC and Pluronic F-127 into liposomal formulations significantly enhances mucopenetration and antimicrobial efficacy.

Toxicity of Carboplatin-Niosomal Nanoparticles in a Brain Cancer Cell Line.

Cancer poses a significant challenge in modern medicine, standing as the primary cause of death in many countries, second only to cardiovascular diseases. Among the various treatments available, carboplatin, a chemotherapy drug, is employed for specific cancer types, including brain carcinoma. The main objective of this investigation is to enhance the therapeutic efficacy of carboplatin by utilizing niosomal nanocarriers. We synthesized nanoniosomal carboplatin using the reverse-phase evaporation technique and conducted an assessment of its particle size, zeta potential, and drug-release properties. Subsequently, we evaluated the cytotoxicity of nanoniosomal carboplatin using the C6 rat glioma cell line. Our research revealed that these niosomal nanoparticles possessed a particle size of 290.5±5.5 nm and a zeta potential of -21.7±7.4 mV. The amount of encapsulated drug and drug loading level were found to be 60.2±2.3% and 2.5±1.1%, respectively. Importantly, the cytotoxic impact of these nanoniosomes on the C6 rat glioma cell line exhibited a significant increase compared to the free drug (P<0.05). Based on our discoveries, it is evident that carboplatin niosomal nanocarriers hold potential as an innovative approach to chemotherapy for brain cancer therapy.

Characteristics and Cytotoxic Effects of Nano-Liposomal Paclitaxel on Gastric Cancer Cells.

Addressing both the initial treatment response and subsequent paclitaxel resistance is a pivotal concern. Nano drug delivery, an emerging approach, presents a cutting-edge alternative to conventional chemotherapy. This investigation synthesized PEGylated nanoparticles (NPs) via the Reverse Phase Evaporation technique for liposomal NPs. Characteristics such as zeta potential, size, drug release and polydispersity index (PDI) were subjected to evaluation. Subsequently, cytotoxicity assays were conducted on gastric cancer cells (AGS) following 24 and 48-hour incubation periods. In this study, the liposomal NPs had a zeta potential of -22 mV and a particle size of 285 nm. The Entrapment efficiency was determined as 41% that occurred physically. Additionally, the liposomal NPs demonstrated a high drug retention rate (39% remained after 72 hours), and they exhibited significantly increased cytotoxicity compared to the free drug, confirming their effectiveness as a suitable carrier for paclitaxel during both incubation periods (P<0.05). These findings collectively advocate the potential of liposomal NPs as promising contenders for effective nano-drug application in propelling chemotherapy forward.

Preparation, Characterization and Cytotoxic Studies of Cisplatin-containing Nanoliposomes on Breast Cancer Cell Lines

Objective: Today, cancer is one the most important challenges in modern medicine. Breast carcinoma is one type of cancer that is treated with cisplatin, a chemotherapy drug. By using liposomal nanocarriers, this study seeks to increase the therapeutic efficiency of cisplatin. Method: The zeta potential, particle size, and drug-release characteristics of nanoliposomal cisplatin were evaluated after it had been synthesized using the reverse phase evaporation technique. The cytotoxicity rate of nanoliposomal cisplatin was then assessed using the T-47D breast cancer cell line. Results: This study’s liposomal nanoparticles (NPs) had a zeta potential of -24.9 mV and a particle size of 342.3 nm. 3.51% and 79.6%, respectively, were found to be the drug loading level and amount of encapsulated drug. A significant improvement over the free drug was seen in this nanoliposome’s cytotoxic effect on the T-47D breast cancer cell line (P&lt;0.05). Conclusion: According to what we have discovered, cisplatin liposomal nanocarriers may prove to be a cutting-edge chemotherapy treatment for breast cancer.

Liposomes encapsulating novel antimicrobial peptide Omiganan: Characterization and its pharmacodynamic evaluation in atopic dermatitis and psoriasis mice model

Omiganan is a novel 12 amino acid synthetic cationic peptide from the cathelicidin family. Omiganan possesses antimicrobial action against a wide range of microbes, including gram-positive and gram-negative bacteria and fungi. Omiganan mainly acts by depolarizing the cytoplasmic membrane, resulting in cellular disruption and death. Apart from its antimicrobial effect, Omiganan also has anti-inflammatory activity. The present investigation aimed to evaluate and compare the efficacy of Omiganan liposomal gel with conventional formulations (Omiganan gel and lotion) in atopic dermatitis (AD) and psoriasis mice animal models. Liposomes encapsulating Omiganan were prepared using the reverse-phase evaporation technique and incorporated into Carbopol 934P gel. The optimized Omiganan liposomes were then characterized for various physicochemical parameters such as vesicle size, shape and surface morphology, zeta-potential, rheological parameters, in-vitro drug release, ex-vivo skin permeation/deposition, in-vitro antimicrobial activity, proteolytic stability, and cellular toxicity and uptake studies. Liposomes exhibited 72 % encapsulation with 7.8 % loading efficacy, a vesicle size, and zeta potential of 120 nm and − 17.2 mv, respectively. Moreover, Omiganan liposomal gel demonstrated controlled release and a better permeation profile than conventional formulations. A substantial reduction in levels of pro-inflammatory cytokines and improvement in AD and psoriatic lesions were achieved by Omiganan liposomal gel compared to Omiganan gel and lotion-based formulations. The present study confirms that Omiganan liposomal formulation can be an effective, safe, and novel alternative treatment approach in atopic dermatitis and psoriasis.

Pentacyclic triterpenes modulate liposome membrane fluidity and permeability depending on membrane cholesterol content

Since the membrane-related processes represent an integral part of the biological activities of drugs, their effect on the membrane dynamics is actually considered. In this study, we investigated the effect of pentacyclic triterpenes (TTPs), oleanolic acid (OA) and erythrodiol (ER), on the fluidity and permeability of liposomes membranes differing by their cholesterol content. All liposomes were prepared by reverse phase evaporation technique (REV). Spin-labeled liposomes exposed or not to TTPs were used for fluidity studies by using 5- and 16-doxyl stearic acids (DSA). TTPs-loaded liposomes (phospholipid:cholesterol of 1:1), and preformed vesicles exposed to TTPs were used for permeability studies by monitoring the release of sulforhodamine B (SRB) at 37 °C. The apparent release constants of SRB were determined by Higuchi model based on a biphasic curve shape (0–10 h; 10–48 h). TTPs-loaded liposomes were characterized for their size and homogeneity. Results showed that ER increased the membrane fluidity at the upper region of the membrane while the both TTPs produced a condensing effect at the deeper region of the membrane. The membrane composition was a critical parameter modulating the effect of TTPs on the membrane permeability. Also, this study consolidated the fact that a fluidizing membrane agent is not necessarily a permeabilizing-membrane compound.

Niosomes-based gene delivery systems for effective transfection of human mesenchymal stem cells

Gene transfer to mesenchymal stem cells (MSCs) has arisen as a powerful approach to increase the therapeutic potential of this effective cell population. Over recent years, niosomes have emerged as self-assembled carriers with promising performance for gene delivery. The aim of our work was to develop effective niosomes-based DNA delivery platforms for targeting MSCs. Niosomes based on 1,2-di-O-octadecenyl-3-trimethylammonium propane (DOTMA; 0, 7 or 15%) as cationic lipid, cholesterol as helper lipid, and polysorbate 60 as non-ionic surfactant, were prepared using a reverse phase evaporation technique. Niosomes dispersions (filtered or not) and their corresponding nioplexes with a lacZ plasmid were characterized in terms of size, charge, protection, and complexation abilities. DOTMA concentration had a large influence on the physicochemical properties of resulting nioplexes. Transfection efficiency and cytotoxic profiles were assessed in two immortalized cell lines of MSCs. Niosomes formulated with 15% DOTMA provided the highest values of β-galactosidase activity, being similar to those achieved with Lipofectamine®, but showed less cytotoxicity. Filtration of niosomes dispersions before adding to the cells resulted in a loss of their biological activities. Storage of niosomes formulations (for 30 days at room temperature) caused minor modification of their physicochemical properties but also attenuated the transfection capability of the nioplexes. Differently, addition of the lysosomotropic agent sucrose into the culture medium during transfection or to the formulation itself improved the transfection performance of non-filtered niosomes. Indeed, steam heat-sterilized niosomes prepared in sucrose medium demonstrated transfection capability.

Formulation, characterization, and evaluation of the anti-tumor activity of nanosized galangin loaded niosomes on chemically induced hepatocellular carcinoma in rats

Galangin (GAL) is a flavonoid with anti-tumor activity. However, its poor solubility results in low bioavailability thus hindering its clinical application. To overcome this challenge, we have prepared niosomal vesicles by reverse-phase evaporation technique using non-ionic surfactant (Span 20, Span 40, and Span 60) and cholesterol in diverse molar ratios with or without charge inducing agents including Dicetylphosphate (DCP) and Stearylamine (STR). The prepared niosomal formulations were evaluated for drug entrapment efficiency (DEE), Drug loading capacity (DL %), size, and cumulative % drug released. DEE ranged between 45.13 ± 0.35 and 77.69 ± 0.45%. DL% ranged from 9.02 ± 0.51 to 16.72 ± 0.39%. The vesicle size ranged between 173.7 ± 12.6 and 355.6 ± 17.9 nm. The optimized niosomal formulation; F8 (prepared from Span 60, cholesterol, and STR in a 1:1: 0.25 M ratios) was selected depending on its highest DEE, DL%, and suitable drug release profile. F8 was subjected to further investigations as FTIR, DSC analysis, zeta potential, scanning electron microscope, stability studies, and estimation of liver biomarkers. Histopathological examination and immunohistochemical assessment of Minichromosome maintenance 3 (MCM3) were done on extracted liver tissue. Significant improvement of liver biomarkers was observed with galangin loaded niosomes. Histopathological and immunohistochemical examination showed that GAL loaded niosomes exhibit marked decline in MCM3 immunostaining hepatocytes and neoplastic hepatic lesions with a small number of hepatic adenomas, thus GAL loaded niosomes are considered as a promising targeted system for improving anti-tumor activity against liver cancer.

Arginine-modified chitosan complexed with liposome systems for plasmid DNA delivery

In order to make more efficient chitosan-based nanoparticles for transfection in physiological condition, chitosomes composed of chitosan modified with arginine and complexed with DOTAP/DOPE lipids are synthesized (named chitosomes) by reverse phase evaporation technique. Structure analyses of chitosomes with or without plasmid DNA (pDNA) are performed by electrophoresis, zeta potential, dynamic light scattering, small angle X-ray scattering and isothermal titration calorimetry, and transfection efficiency and cytotoxicity are performed in HEK293 T cells. Chitosomes have a positive surface charge (X¯= 52 mV) with an average size of 116 nm, and interaction with pDNA are favored thermodynamically and do not suffer aggregation significantly. In our experimental conditions, the transfection efficiency average reaches 86% ± 3, while the Lipofectamine® reaches 87% ± 5 in vitro. Cytotoxicity of chitosomes are tolerable. Structural analyses show that that chitosomes-pDNA complexes appear to have multilamellar vesicle structures hosting pDNA in-between bilayers which favor interaction with cell membrane and delivery of pDNA. Results show that synthesized chitosomes are promising carriers for gene delivery.

Latanoprost niosomes as a sustained release ocular delivery system for the management of glaucoma

Objective: Glaucoma is a leading cause of irreversible blindness worldwide. Whereas latanoprost is one of the most effective drugs in glaucoma treatment, its eye drops need frequent application leading to lack of patient adherence. This study aimed to develop a patient-friendly niosome-in-gel system for the sustained ocular delivery of latanoprost.Methods: Niosomes were prepared by the reverse-phase evaporation technique and optimized for different formulation parameters, such as cholesterol/surfactant and drug/surfactant ratios. Selected niosomal formulations were incorporated into different gels and their viscosity and drug release kinetics were evaluated. Optimal niosomal gel was evaluated in vivo in rabbits’ eyes for irritation potential and ability to reduce intraocular pressure.Results: FT-IR studies showed that there were nonspecific interactions between latanoprost and different niosomal components leading to drug encapsulation efficiency ≥88%. Latanoprost encapsulation efficiency increased with the drug/surfactant ratio and encapsulation efficiency ∼98% was obtained at a ratio of 50%. Pluronic® F127 had the best ability to sustain drug release from the niosomes. In rabbits’ eyes, this gel was free of toxic and irritant effects and reduced intraocular pressure over a period of three days, which was significantly longer than that of commercial latanoprost eye drops.Conclusion: Latanoprost niosomal Pluronic® F127 gel may find applications in glaucoma management.

Gene delivery to the rat retina by non-viral vectors based on chloroquine-containing cationic niosomes

The incorporation of chloroquine within nano formulations, rather than as a co-treatment of the cells, could open a new avenue for in vivo retinal gene delivery. In this manuscript, we evaluated the incorporation of chloroquine diphosphate into the cationic niosome formulation composed of poloxamer 188, polysorbate 80 non-ionic surfactants, and 2,3-di (tetradecyloxy) propan-1-amine (hydrochloride salt) cationic lipid, to transfect rat retina. Niosome formulations without and with chloroquine diphosphate (DPP80, and DPP80-CQ, respectively) were prepared by the reverse phase evaporation technique and characterized in terms of size, PDI, zeta potential, and morphology. After the incorporation of the pCMS-EGFP plasmid, the resultant nioplexes -at different cationic lipid/DNA mass ratios- were further evaluated to compact, liberate, and secure the DNA against enzymatic digestion. In vitro procedures were achieved in ARPE-19 cells to assess transfection efficacy and intracellular transportation. Both nioplexes formulations transfected efficiently ARPE-19 cells, although the cell viability was clearly better in the case of DPP80-CQ nioplexes. After subretinal and intravitreal injections, DPP80 nioplexes were not able to transfect the rat retina. However, chloroquine containing vector showed protein expression in many retinal cells, depending on the administration route. These data provide new insights for retinal gene delivery based on chloroquine-containing niosome non-viral vectors.

Natamycin niosomes as a promising ocular nanosized delivery system with ketorolac tromethamine for dual effects for treatment of candida rabbit keratitis; in vitro/in vivo and histopathological studies

Objectives: This study was aimed to develop dual-purpose natamycin (NAT)-loaded niosomes in ketorolac tromethamine (KT) gels topical ocular drug delivery system to improve the clinical efficacy of natamycin through enhancing its penetration through corneal tissue and reducing inflammation associated with Fungal keratitis (FK).Significance: Nanosized carrier systems, as niosomes would provide great potential for improving NAT ocular bioavailability.NAT niosomal dispersion formulae were prepared and then incorporated in 0.5%KT gels using different mucoadhesive viscosifying polymers.Methods: Niosomes were prepared using the reverse-phase evaporation technique. In vitro experimental, and in vivo clinical evaluations for these formulations were done for assessment of their safety and efficacy for treatment of Candida Keratitis in Rabbits. In vitro release study was carried out by the dialysis method. In vivo and histopathological studies were performed on albino rabbits.Results: NAT niosomes exhibited high entrapment efficiency percentage (E.E%) up to96.43% and particle size diameter ranging from 181.75 ± 0.64 to 498.95 ± 0.64 nm, with negatively charged zeta potential (ZP). NAT niosomal dispersion exhibited prolonged in vitro drug release (40.96–77.49% over 24h). NAT-loaded niosomes/0.5%KT gel formulae revealed retardation in vitro release, compared to marketed-product (NATACYN®) and NAT-loaded niosomes up to57.32% (F8). In vivo experimental studies showed the superiority for F8 in treatment of candida keratitis and better results on corneal infiltration and hypopyon level. These results were consistent with histopathological examination in comparison with F5 and combined marketed products (NATACYN® and Ketoroline®).Conclusions: This study showed that F8 has the best results from all pharmaceutical in vitro evaluations and a better cure percent in experimental application and enhancing the prolonged delivery of NAT and penetrating the cornea tissues.

Gene transfer to rat cerebral cortex mediated by polysorbate 80 and poloxamer 188 nonionic surfactant vesicles.

BackgroundGene therapy can be an intriguing therapeutic option in wide-ranging neurological disorders. Though nonviral gene carriers represent a safer delivery system to their viral counterparts, a thorough design of such vehicles is crucial to enhance their transfection properties.PurposeThis study evaluated the effects of combined use of two nonionic surfactants, poloxamer 188 (P) and polysorbate 80 (P80) into nanovesicles – based on 2,3-di(tetradecyloxy)propan-1-amine cationic lipid (D) – destined for gene delivery to central nervous system cells.MethodsNiosome formulations without and with poloxamer 188 (DP80 and DPP80, respectively) were prepared by the reverse-phase evaporation technique and characterized in terms of size, surface charge, and morphology. After the addition of pCMS-EGFP plasmid, the binding efficiency to the niosomes was evaluated in agarose gel electrophoresis assays. Additionally, transfection efficiency of complexes was also evaluated in in vitro and in vivo conditions.ResultsIn vitro experiments on NT2 cells revealed that the complexes based on a surfactant combination (DPP80) enhanced cellular uptake and viability when compared with the DP80 counterparts. Interestingly, DPP80 complexes showed protein expression in glial cells after administration into the cerebral cortices of rats.ConclusionThese data provide new insights for glia-centered approach for gene therapy of nervous system disorders using cationic nanovesicles, where nonionic surfactants play a pivotal role.

Corticoids modulate liposome membrane fluidity and permeability depending on membrane composition and experimental protocol design

Given that literature data may give inconsistent results on the effect of a drug on lipid membrane properties, this work aims to investigate the impact of the liposome composition and experimental protocol design on glucocorticoids (GRs: cortisol, cortisone, fludrocortisone acetate, methylprednisolone, prednisolone and prednisone)-modulating membrane fluidity and permeability. GRs-loaded liposomes consisting of dipalmitoylphosphatidylcholine (DPPC) and cholesterol (CHOL) were prepared by reverse phase evaporation technique (REV) at DPPC:CHOL:GR molar ratios of 100:100:2.5, and 100:100:10. The formulations were characterized for their size and homogeneity, encapsulation efficiency and loading rates of GRs, incorporation rates and loading rates of DPPC and CHOL. Changes in DPPC membrane fluidity (CHOL% 0, 10, 20, 30 and 100) after exposure to methylprednisolone were monitored by using 5- and 16-doxyl stearic acids (DSA) as spin probes. For permeability studies, the above-mentioned GRs-loaded liposomes and the preformed liposomes exposed to GRs (2.5 mol%) were compared for the leakage of an encapsulated fluorescent dye, sulforhodamine B (SRB), at 37 °C in buffer (pH 7.5) containing NaCl. The SRB release kinetics were analyzed by the Higuchi model for two release phases (from 0 to 10 h, and from 10 to 48 h). All formulations exhibited a monodispersed size distribution of liposomes with a mean particle value close to 0.4 μm, also the DPPC and CHOL were highly incorporated (>95%). High loading rate values of DPPC and CHOL were also obtained. Except for fludrocortisone acetate (51%) and prednisolone (77%), high loading rate values of GRs were obtained (>81%). Fluidity and permeability studies showed that the GR concentration, CHOL content, experimental protocol design including the period of incubation represent critical parameters to be considered in analyzing the effect of drugs on the membrane properties.

Cholesterol modulates the liposome membrane fluidity and permeability for a hydrophilic molecule

The effect of cholesterol (CHOL) content on the permeability and fluidity of dipalmitoylphosphatidylcholine (DPPC) liposome membrane was investigated. Liposomes encapsulating sulforhodamine B (SRB), a fluorescent dye, were prepared by reverse phase evaporation technique (REV) at various DPPC:CHOL molar ratios (from 100:0 to 100:100). The release kinetics of SRB was studied during 48 h in buffer (pH 7.4) containing NaCl at 37 °C. The DPPC:CHOL formulations were also characterized for their size, polydispersity index and morphology. Increasing CHOL concentration induced an increase in the mean liposomes size accompanying with a shape transition from irregular to nanosized, regular and spherical vesicles. The release kinetics of SRB showed a biphasic pattern; the release data was then analyzed using different mathematical models. On the overall, the SRB release was governed by a non-Fickian diffusion during the first period (0–10 h) while it followed a Fickian diffusion between 10 and 48 h. Changes in DPPC liposome membrane fluidity of various batches (CHOL% 0, 10, 20, 30 and 100) were monitored by using 5- and 16 doxyl stearic acids (DSA) as spin labels. CHOL induced a decrease in the bilayer fluidity. Concisely, CHOL represents a critical component in modulating the release of hydrophilic molecules from lipid vesicles.

An in vivo study of Hypericum perforatum in a niosomal topical drug delivery system

The active compounds present in Hypericum perforatum L. (Hypericaceae) include hyperforin, hypericins and flavonoids, which are assumed to be responsible for the activity of the extract in the treatment of wounds and scars. The present study aimed to incorporate H. perforatum extract standardized to a known content of phloroglucinols, naphthodianthrones and polyphenolic compounds into an effective transdermal drug delivery system capable of entrapping both lipophilic and hydrophilic constituents in the form of niosomal gels for wound treatment. An 80% ethanol extract (HE) was prepared on a pilot scale using DIG-MAZ. An HPLC-DAD holistic profile was established for HE and was standardized to contain 3.4 ± 4 rutin, 1.1 ± 3 chlorogenic acid, 0.5 ± 2 quercitrin, 2.8 ± 2 hyperforin, and 0.51 ± 3% w/w total hypericins. Niosomes were prepared using the modified reverse phase evaporation technique (REV). The wound healing effect of the gel was tested on 16 adult mongrel dogs. A significant decrease in the inflammatory cell count (18.4 ± 5.3) was recorded in the niosomal gel 1.5% NaCMC-treated group at the 7th day post wounding. It induced a marked regression in the inflammatory phase and enhanced the early beginning of the proliferative phase of wound healing. After 21 days, it showed complete re-epithelization, formation of new matrix fibers and significant reduction in the wound size, compared to the control and the Panthenol® 2% cream treated groups. This is the first study of H. perforatum in a niosomal topical drug delivery system.

Carboplatin liposomal nanoparticles: Preparation, characterization, and cytotoxicity effects on lung cancer in vitro environment

ABSTRACTThe study aimed to encapsulate anticancer drug carboplatin into liposomal nanoparticles by reverse-phase evaporation technique and evaluate its efficacy on lung cancer in vitro environment. Nanoparticles were characterized in terms of size, drug loading efficiency, drug retention capability, and cytotoxicity effects. Nanoscale particles with 67% drug encapsulation efficiency were prepared. Also, high retention capability (drug release equal to 25% after 72 h) of the nanodrug was confirmed. In addition, results of the nanodrug cytotoxicity indicated nanoparticles increased potency of the drug by approximately 90%. Findings of the study indicated liposome can be used for carboplatin delivery to lung cancer.

Delivery of cisplatin by folic acid-targeted liposomal nanoparticles into liver cancer cell line

ABSTRACTThis study aimed to prepare cisplatin-loaded PEGylated liposomal nanoparticles targeted with folic acid and evaluate their efficacy on liver cancer cell line PLC/PRF/5 (Alexander hepatoma cell line). Nanoparticles were prepared by reverse phase evaporation technique and characterized by dynamic light scattering, scanning electron microscopy, transmission electron microscopy, inductively coupled plasma optical emission spectrometry, Fourier transform infrared spectroscopy, and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide techniques. Nanoscale particles with appropriate drug encapsulation efficiency (13%) were prepared. Cytotoxicity results indicated that the superior potency of targeted cisplatin-loaded nanoparticles compared to the nontargeted counterpart with 23% more cytotoxicity. Findings of this study confirmed the potency of targeted PEGylated liposomal nanoparticles.

Formulation and evaluation of analgesic activity of polysorbate 80-coated loperamide liposomes in mice

Purpose : To deliver loperamide (Lp) into mice brain using polysorbate 80 (PS80)-coated liposomes that inhibits P-glycoprotein (P-gp) efflux. Method : Lp loaded liposomes were prepared by reverse phase evaporation technique using lecithin (Lec) and cholesterol (Ch). The efficacy of PS80-coated Lp liposomes (PLs) in mice was evaluated using central analgesic models (Eddy’s hot plate method and tail immersion test) and peripheral analgesic model (acetic acid-induced writhing). Results : PLs showed maximum possible response (MPR) of 58.33 % at 60 min in Eddy’s hot plate study. In the tail immersion test, PLs showed MPR of 67.64 and 69.24 % at 60 and 90 min, respectively, relative to control group. This confirms the potential of PLs to deliver Lp to the brain by inhibiting P-gp efflux. Dose response study using tail flick method confirmed the minimum Lp dose (25 μg/kg, i.v) required to achieve central analgesic activity using PLs. Conclusion : PS80-coated Lp loaded liposomes (PLs) possess a good potential to inhibit P-gp efflux of Lp from brain, and also exhibit both central and peripheral analgesic activity. Keywords : Loperamide, Polysorbate 80, P-glycoprotein (P-gp), Analgesic activity