Lecithin-Based Novel Cationic Nanocarriers (Leciplex) I: Fabrication, Characterization and Evaluation

Date, Abhijit A.; Srivastava, Deepika; Nagarsenker, Mangal S.; Mulherkar, Rita; Panicker, Lata; Aswal, Vinod K.; Hassan, P. A.; Steiniger, Frank; Thamm, Jana; Fahr, Alfred

doi:10.2217/nnm.11.38

Cited by 34 publications

(36 citation statements)

References 42 publications

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“…LeciPlexes were prepared by a one-step fabrication process using equimolar amounts of PL-90G and CTAB according to previously published procedures [26,27]. Briefly, the drug (10 mg) and PL-90G (0.182 g, 24 mM) were dissolved in Transcutol ® P (0.5 mL) by heating the mixture briefly to 70 • C in a water bath.…”

Section: Preparation Of Drug-loaded Leciplexesmentioning

confidence: 99%

“…Distilled water (9.5 mL maintained at 70 • C) was added to the drug/PL-90G mixture at once under vigorous stirring. The stirring was continued until a uniform dispersion was obtained [26].…”

Section: Preparation Of Drug-loaded Leciplexesmentioning

confidence: 99%

“…Liposomes are able to encapsulate a wide range of drugs, including hydrophilic and hydrophobic ones, and enhance their delivery through the skin. LeciPlex is a fairly new vesicular nanodelivery system based on the combination of negatively charged phospholipids and cationic surfactants [26]. LeciPlexes are prepared by a simple one-step procedure and have a positive surface charge, which facilitates their intimate interaction with the negatively charged skin surface, leading to enhanced drug penetration into the deep skin layers [27].…”

Section: Introductionmentioning

confidence: 99%

“…Cationic surfactants such as cetyltrimethylammonium bromide (CTAB) used in the preparation of LeciPlex systems were reported to be cytotoxic to human skin HaCaT keratinocyte cells at a concentration as low as 10 µM [28]. However, previous studies showed that the association between CTAB and phospholipids in LeciPlex systems greatly limits their cytotoxic effects [26,29]. Moreover, the toxic effect of CTAB was reported to be due to free CTAB in solution, which is usually removed by centrifugation during LeciPlex preparation [28].…”

Section: Introductionmentioning

confidence: 99%

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Spironolactone-Loaded LeciPlexes as Potential Topical Delivery Systems for Female Acne: In Vitro Appraisal and Ex Vivo Skin Permeability Studies

et al. 2019

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Spironolactone (SP), an aldosterone antagonist with anti-androgen properties, has shown promising results in the treatment of female acne. However, its systemic side effects limit its clinical benefits. This study aimed to prepare and evaluate LeciPlexes for SP topical delivery. LeciPlexes were prepared by a one-step procedure and characterized using various techniques. Optimum LeciPlex preparation was incorporated into 1% methylcellulose gel and SP permeability was tested ex vivo in Sprague-Dawley rat skin. The maximum drug encapsulation efficiency obtained was 93.6 ± 6.9% and was dependent on the drug/phospholipid and surfactant/phospholipid ratios. A zeta potential of +49.3 ± 3.5 to +57.7 ± 3.3 mV and a size of 108 ± 25.3 to 668.5 ± 120.3 nm were observed for the LeciPlexes. FT-IR and DSC studies confirmed the incorporation of SP into the LeciPlexes through hydrophobic and hydrogen bonding interactions. SP release from the LeciPlex formulations was significantly slower than from the drug suspension. Cumulative SP permeated through rat skin from LeciPlex gel was about 2-fold higher than SP control gel. Cumulative SP deposited in the stratum corneum and other skin layers from the LeciPlex gel was about 1.8- and 2.6-fold higher than SP control gel, respectively. This new SP LeciPlex formulation is a promising carrier for the treatment of female acne.

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Section: Preparation Of Drug-loaded Leciplexesmentioning

confidence: 99%

Section: Preparation Of Drug-loaded Leciplexesmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Spironolactone-Loaded LeciPlexes as Potential Topical Delivery Systems for Female Acne: In Vitro Appraisal and Ex Vivo Skin Permeability Studies

et al. 2019

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“…Date et al . prepared self‐assembled cationic SLNs by capping negative phosphate groups of soybean lecithin with positively charged cetyl trimethyl ammonium bromide (CTAB) and didodecyldimethylammonium bromide (DDAB) . These formulations were further used in oral administration of quercetin and anticancer drugs .…”

Section: Introductionmentioning

confidence: 99%

Lecithin‐acrylamido‐2‐methylpropane sulfonate based crosslinked phospholipid nanoparticles as drug carrier

Mutlu

Bostan

Bahadorı

et al. 2016

J of Applied Polymer Sci

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In this study, a novel paclitaxel (PTX) loaded and a crosslinked solid phospholipid nanoparticles (SLN-PTX) with negative surface charge was prepared by UV polymerization for drug delivery. Capping of positive charge of zwitterionic lecithin with negative charge of sodium 2-acrylamido-2-methyl-1-propanesulfonate (AMPS-Na) through cation exchange interaction produced a lecithin-AMPS (L-AMPS) complex. The amphiphilic and negative charged lipid complex was emulsified in the presence of emulsifier, paclitaxel, initiator, and methacrylated poly e-caprolacton-diol (PCL-MAC) as a spacer. The colloidal system was subjected to UVirradiation to obtain crosslinked nanoparticles. Completion of the UV-polymerization was monitored with differential scanning calorimetry (DSC), which indicated the disappearance of exothermic peaks of vinyl groups. The nanoparticle system, having an average size of 200 nm, exhibited high drug encapsulation (96%) with negatively charged surface (zeta potential had an average of 270 mV). PTX release profiles of the crosslinked and uncrosslinked SLN-PTXs were studied and their pharmacological properties were compared. The crosslinked nanoparticles exhibited more controlled release behavior with longer release time compared to the uncrosslinked ones. In vitro cytotoxicity test was conducted on MCF-7 human breast adenocarcinoma cell line, which indicated that the crosslinked SLN-PTXs have a potential therapeutic effect for breast cancer treatments. V C 2016 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2016, 133, 44105.

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Functionalized Lipid Particulates in Targeted Drug Delivery

Nagarsenker

Jain

Shah

2014

Advances in Delivery Science and Technology

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Lipids have been of major interest and importance in fi eld of drug delivery systems. Their application in formulation science has been diverse and promising in different ways. The number of reports published each year on lipid based formulations and lipid based formulations in market establish critical role of lipids in drug delivery. Of considerable importance is the application of lipids in design of particulate systems which are amenable to surface modifi cations for improved drug/gene delivery. In the past few years, reports on different lipid based particulate systems have increased tremendously with major focus on liposomes and solid lipid nanoparticles (SLNs) [ 1 -7 ]. Other lipid based particulate systems that are evaluated include nanostructured lipid carriers (NLCs) [ 6 , 8 -11 ], emulsions [ 12 -17 ], lipid-drug conjugates (LDCs) and recently reported lipid nano-particulates in the form of LeciPlex [ 18 , 19 ], and polymer-lipid hybrid nanoparticles (PLN) [ 20 -22 ]. One of the various reasons responsible for success of lipids in formulation of particulate systems is their bio-compatible and biodegradable nature [ 2 , 19 , 23 ]. Thus, lipid based particulate systems can suitably be employed for delivery through not only noninvasive routes, such as oral and topical, but also through parenteral routes which are very demanding with reference to delivery system design.Lipid particulate systems, over the years, have undergone stupendous modifi cations. Initially lipid particulate system of micron size were reported which were followed by lipid particulates in nanosize range. The nanosize range of particles made them capable of targeting tumors better, primarily because of enhanced

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Lecithin-Based Novel Cationic Nanocarriers (Leciplex) I: Fabrication, Characterization and Evaluation

Cited by 34 publications

References 42 publications

Spironolactone-Loaded LeciPlexes as Potential Topical Delivery Systems for Female Acne: In Vitro Appraisal and Ex Vivo Skin Permeability Studies

Spironolactone-Loaded LeciPlexes as Potential Topical Delivery Systems for Female Acne: In Vitro Appraisal and Ex Vivo Skin Permeability Studies

Lecithin‐acrylamido‐2‐methylpropane sulfonate based crosslinked phospholipid nanoparticles as drug carrier

Functionalized Lipid Particulates in Targeted Drug Delivery

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