Targeting potential and anti-HIV activity of lamivudine loaded mannosylated poly (propyleneimine) dendrimer

Dutta, Tathagata; Jain, Narendra Kumar

doi:10.1016/j.bbagen.2006.12.007

Cited by 181 publications

(91 citation statements)

References 25 publications

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“…Lamivudine has a short biological half-life (4-6 hour) and requires frequent administration for a prolonged period of time (lifelong in AIDS and for one year in hepatitis patients). 1,2 Transdermal route is, therefore, a better alternative to achieve constant plasma levels for prolonged periods of time, which additionally could be advantageous because of less frequent dosing regimens.…”

Section: Introductionmentioning

confidence: 99%

Formulation and evaluation of ethosomes for transdermal delivery of lamivudine

et al. 2007

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The purpose of the present research was to investigate the mechanism for improved intercellular and intracellular drug delivery from ethosomes using visualization techniques and cell line study. Ethosomal formulations were prepared using lamivudine as model drug and characterized in vitro, ex vivo and in vivo. Transmission electron microscopy, scanning electron microscopy, and fluorescence microscopy were employed to determine the effect of ethosome on ultrastructure of skin. Cytotoxicity and cellular uptake of ethosome were determined using T-lymphoid cell line (MT-2). The optimized ethosomal formulation showed 25 times higher transdermal flux (68.4 ± 3.5 μg/cm 2 /h) across the rat skin as compared with that of lamivudine solution (2.8 ± 0.2 μg/cm 2 /h). Microscopic studies revealed that ethosomes influenced the ultrastructure of stratum corneum. Distinct regions with lamellar stacks derived from vesicles were observed in intercellular region of deeper skin layers. Results of cellular uptake study showed significantly higher intracellular uptake of ethosomes (85.7% ± 4.5%) as compared with drug solution (24.9% ± 1.9%). The results of the characterization studies indicate that lipid perturbation along with elasticity of ethosomes vesicles seems to be the main contributor for improved skin permeation.

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Section: Introductionmentioning

confidence: 99%

Formulation and evaluation of ethosomes for transdermal delivery of lamivudine

et al. 2007

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“…Thus, protection in physiological environment and increase of residence time of lamivudine inside cells would greatly improve the treatment efficiency. To achieve this aim, lamivudine has been encapsulated into various colloidal carriers such as biodegradable polymer spheres [7] and micelles [8], and conjugated to polysaccharide and dendrimers [9,10].…”

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confidence: 99%

Preparation and cellular uptake of PLGA particles loaded with lamivudine

et al. 2012

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Poly(D,L-lactide-co-glycolide) (PLGA) nanoparticles loaded with lamivudine and coated with bovine serum albumin (BSA) were prepared via a double emulsion method. The influences of experiments parameters such as volume of inner aqueous phase, concentration of organic phase and ultrasonication time on the particle size and drug entrapment efficiency were investigated, obtaining PLGA particles with a diameter of ~260 nm and drug entrapment efficiency of ~35%. The particles were observed by scanning electron microscopy and transmittance electron microscopy, showing a core-shell structure. BCA assay found that 58 mg BSA was present on/in 1 g LPB particles. The loaded lamivudine showed a burst release at beginning and sustained release until 24 h in physiological conditions. Low pH could accelerate the release of lamivudine from PLGA particles, making the PLGA particles potential intelligent intracellular drug carriers. The PLGA particles were readily internalized into the human liver cells within a short time and increased gradually with the prolongation of incubation time regardless of the loading of lamivudine. The particles either resided within lysosomes or transferred to cytoplasm, but could not enter into the cell nucleus. The cell viability was not significantly influenced in the presence of the particles regardless of lamivudine encapsulation, suggesting that this kind of particles may be a good candidate for the intracellular anti-hepatitis B drug delivery.PLGA, lamivudine, cell uptake, intracellular distribution, drug delivery Citation:Wang B, Chen G Q, Mao Z W, et al. Preparation and cellular uptake of PLGA particles loaded with lamivudine.

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“…Consequently, the viral p24 level was reduced 2.6-fold when compared with the free drug. 92 The key limitations of dendrimer-based drug delivery platforms are the variability of their drug-release mechanisms and the short-term of their release kinetics. Drugs encapsulated within dendrimers have a tendency to be released quickly, unloading their payload prematurely before the delivery platforms even reach the targets.…”

Section: Dendrimersmentioning

confidence: 99%

Current approaches to enhance CNS delivery of drugs across the brain barriers

Lu¹,

Zhao²,

Wong³

et al. 2014

IJN

251

150

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Although many agents have therapeutic potentials for central nervous system (CNS) diseases, few of these agents have been clinically used because of the brain barriers. As the protective barrier of the CNS, the blood–brain barrier and the blood–cerebrospinal fluid barrier maintain the brain microenvironment, neuronal activity, and proper functioning of the CNS. Different strategies for efficient CNS delivery have been studied. This article reviews the current approaches to open or facilitate penetration across these barriers for enhanced drug delivery to the CNS. These approaches are summarized into three broad categories: noninvasive, invasive, and miscellaneous techniques. The progresses made using these approaches are reviewed, and the associated mechanisms and problems are discussed.

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Targeting potential and anti-HIV activity of lamivudine loaded mannosylated poly (propyleneimine) dendrimer

Cited by 181 publications

References 25 publications

Formulation and evaluation of ethosomes for transdermal delivery of lamivudine

Formulation and evaluation of ethosomes for transdermal delivery of lamivudine

Preparation and cellular uptake of PLGA particles loaded with lamivudine

Current approaches to enhance CNS delivery of drugs across the brain barriers

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