Solid lipid nanoparticles of diethylcarbamazine citrate for enhanced delivery to the lymphatics:<i>in vitro</i>and<i>in vivo</i>evaluation

Karthik, S.; Chellan, Vijaya Raghavan; Tamilselvan, Natarajan; Balakumar, K; Rahman, Habibur; Karanam, Vamshikrishna; Muthuswamy, Siva Selva Kumar; Ranganathan, Hari Prasad

doi:10.1517/17425247.2014.915310

Cited by 31 publications

(14 citation statements)

References 46 publications

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“…Interestingly, inhibiting phagocytosis using dextran as an adjuvant increased both lymphatic uptake and residence time of PEGylated colloids. 21 PEGylation can be applied in developing various nanoparticulate carriers like dendrimers, 10 PRINT (particle replication in nonwetting templates) hydrogels, 28 magnetic carbon nanotubes with PEG groups, 29 solid lipid nanoparticles, 3 polymeric nanoparticles, 24 liposomes, 25 and so on. Furthermore, a glance at a few of the promising nanopharmaceuticals in clinical use or undergoing trials like Oncaspar (PEGylated l-asperginase for acute lymphoblastic leukemia), Genexol (PEGylated block polymer containing an anticancer drug for metastatic breast cancer), and Lipo-dox and ThermoDox (PEGylated liposomal forms of doxorubicin) highlights the utility of PEGylation.…”

Section: Pegylation: Gateway For Lymphatic Targetingmentioning

confidence: 99%

“…Studies have revealed that although PEGylation improved lymphatic uptake, it reduced the retention time of colloids. 2,3,10,33 The authors hypothesized that the poor retention of the colloids in the lymph nodes is due to the smaller size and extreme hydrophilic nature of PEGylated colloids. These colloids probably escaped through the spaces present between the lymphatic capillary cells because of their smaller size.…”

Section: Size-dependent Retention In Lymphaticsmentioning

confidence: 99%

“…3,33 In spite of the surrounding immune trafficking cells and oxidative free radicals, filarial worms survive in the lymphatics for several years. These worms contain a thick cuticle comprising an internal matrix of collagenous proteins, which allow them to survive in the face of various host immune reactions.…”

Section: Seeds and Leads From Filarial Worms For Lymphatic Targetingmentioning

confidence: 99%

“…Apart from mediating the immune functions and tissue fluid balance, the lymphatics also act as a reservoir for human immunodeficiency virus, filariasis, tuberculosis, and metastatic cancer cells. 3 Hence, lymphatic targeting of molecules, compounds, vaccines, and so on will be useful for diagnosis and therapy and eliciting immune responses. Colloids have emerged as an important class of drug carriers for targeted delivery into the complex lymphatic system.…”

Section: Introductionmentioning

confidence: 99%

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A brief perspective on the diverging theories of lymphatic targeting with colloids

Karthik

Marslin

Raghavan

et al. 2016

IJN

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For targeted delivery of colloids to the lymphatic system, the colloids should efficiently reach and remain in the lymphatics for a considerable period of time. As per the current knowledge, diffusion and phagocytosis are the two mechanisms through which colloids reach the lymphatic system. Several parameters including particle size and charge have been shown to affect the direct uptake of colloids by the lymphatic system. Although many researchers attached ligands on the surface of colloids to promote phagocytosis-mediated lymphatic delivery, another school of thought suggests avoidance of phagocytosis by use of carriers like polyethylene glycol (PEG)ylated colloids to impart stealth attributes and evade phagocytosis. In this perspective, we weigh up the paradoxical theories and approaches available in the literature to draw conclusions on the conditions favorable for achieving efficient lymphatic targeting of colloids.

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Section: Pegylation: Gateway For Lymphatic Targetingmentioning

confidence: 99%

Section: Size-dependent Retention In Lymphaticsmentioning

confidence: 99%

Section: Seeds and Leads From Filarial Worms For Lymphatic Targetingmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

A brief perspective on the diverging theories of lymphatic targeting with colloids

Karthik

Marslin

Raghavan

et al. 2016

IJN

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“…The sustained release phase of the drug is also not prolonged for longer hours because of the smaller diameter of the particles, which provides a larger surface area for the drug-loaded particles. 65,66 stability of slN-DaP and M-slN-DaP…”

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confidence: 99%

Design and statistical modeling of mannose-decorated dapsone-containing nanoparticles as a strategy of targeting intestinal M-cells

Vieira¹,

Chaves²,

Pinheiro³

et al. 2016

IJN

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The aim of the present work was to develop and optimize surface-functionalized solid lipid nanoparticles (SLNs) for improvement of the therapeutic index of dapsone (DAP), with the application of a design of experiments. The formulation was designed to target intestinal microfold (M-cells) as a strategy to increase internalization of the drug by the infected macrophages. DAP-loaded SLNs and mannosylated SLNs (M-SLNs) were successfully developed by hot ultrasonication method employing a three-level, three-factor Box–Behnken design, after the preformulation study was carried out with different lipids. All the formulations were systematically characterized regarding their diameter, polydispersity index (PDI), zeta potential (ZP), entrapment efficiency, and loading capacity. They were also subjected to morphological studies using transmission electron microscopy, in vitro release study, infrared analysis (Fourier transform infrared spectroscopy), calorimetry studies (differential scanning calorimetry), and stability studies. The diameter of SLNs, SLN-DAP, M-SLNs, and M-SLN-DAP was approximately 300 nm and the obtained PDI was <0.2, confirming uniform populations. Entrapment efficiency and loading capacity were approximately 50% and 12%, respectively. Transmission electron microscopy showed spherical shape and nonaggregated nanoparticles. Fourier transform infrared spectroscopy was used to confirm the success of mannose coating process though Schiff’s base formation. The variation of the ZP between uncoated (approximately −30 mV) and mannosylated formulations (approximately +60 mV) also confirmed the successful coating process. A decrease in the enthalpy and broadening of the lipid melting peaks of the differential scanning calorimetry thermograms are consistent with the nanostructure of the SLNs. Moreover, the drug release was pH-sensitive, with a faster drug release at acidic pH than at neutral pH. Storage stability for the formulations for at least 8 weeks is expected, since they maintain the original characteristics of diameter, PDI, and ZP. These results pose a strong argument that the developed formulations can be explored as a promising carrier for treating leprosy with an innovative approach to target DAP directly to M-cells.

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Lymphatic Transport of Drugs after Intestinal Absorption: Impact of Drug Formulation and Physicochemical Properties

et al. 2020

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Solid lipid nanoparticles of diethylcarbamazine citrate for enhanced delivery to the lymphatics:in vitroandin vivoevaluation

Abstract: Targeting of DEC to the lymphatics is possible through SLNs and the retention time in the lymphatics can also be enhanced.

Cited by 31 publications

References 46 publications

A brief perspective on the diverging theories of lymphatic targeting with colloids

A brief perspective on the diverging theories of lymphatic targeting with colloids

Design and statistical modeling of mannose-decorated dapsone-containing nanoparticles as a strategy of targeting intestinal M-cells

Lymphatic Transport of Drugs after Intestinal Absorption: Impact of Drug Formulation and Physicochemical Properties

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