Molecular interactions, internal structure and drug release kinetics of rationally developed polymer–lipid hybrid nanoparticles

In the era of nanoparticulate controlled and site specific drug delivery systems, use of solid lipids to produce first generation lipid nanoparticles, solid lipid nanoparticles (SLN), became a revolutionary approach in the early nineties. The present review is designed to provide an insight into how SLN are finding a niche as promising nanovectors and forms a sound basis to troubleshoot the existing problems associated with traditional systems. Herein, authors had tried to highlight the frontline aspects prominent to SLN. An updated list of lipids, advanced forms of SLN, methods of preparation, characterization parameters, and various routes of administration of SLN are explored in-depth. Stability, toxicity, stealthing, targeting efficiency and other prospectives of SLN are also discussed in detail. The present discussion embodies the potential of SLN, now being looked up by various research groups around the world for their utility in the core areas of pharmaceutical sciences, thereby urging pharmaceutical industries to foster their scale-up.

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“…Interactions among these components play an important role for successful fabrication and performance of PLNs (17).…”

Section: Polymer Lipid Hybrid Nanoparticles (Plns)mentioning

confidence: 99%

Solid lipid based nanocarriers: An overview / Nanonosači na bazi čvrstih lipida: Pregled

Pardeshi¹,

Rajput²,

Belgamwar³

et al. 2012

Acta Pharmaceutica

182

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“…It has been reported that an electrostatic interaction between cationic drug and counterionic polymers or small molecules plays a prominent role in the development of nanocarriers. 17,[22][23][24][25][26][27][28][29] MTO was incorporated into a mixed lipid core because of the strong electrostatic interaction between DS and GcNa. Moreover, a comparative analysis of the zeta potential of the blank NLCs 4), and MTO-TMLGNs (−28.7±0.4) further confirmed the role of the electrostatic interaction between the MTO and GcNa/DS.…”

Section: Results and Discussion Characterization Of Tmlgnsmentioning

confidence: 99%

Synergistic and complete reversal of the multidrug resistance of mitoxantrone hydrochloride by three-in-one multifunctional lipid-sodium glycocholate nanocarriers based on simultaneous BCRP and Bcl-2 inhibition

Ling¹,

Zhang²,

Zhang³

et al. 2016

IJN

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Multidrug resistance (MDR) is a severe obstacle to successful chemotherapy due to its complicated nature that involves multiple mechanisms, such as drug efflux by transporters (P-glycoprotein and breast cancer resistance protein, BCRP) and anti-apoptotic defense (B-cell lymphoma, Bcl-2). To synergistically and completely reverse MDR by simultaneous inhibition of pump and non-pump cellular resistance, three-in-one multifunctional lipid-sodium glycocholate (GcNa) nanocarriers (TMLGNs) have been designed for controlled co-delivery of water-soluble cationic mitoxantrone hydrochloride (MTO), cyclosporine A (CsA – BCRP inhibitor), and GcNa (Bcl-2 inhibitor). GcNa and dextran sulfate were incorporated as anionic compounds to enhance the encapsulation efficiency of MTO (up to 97.8%±1.9%) and sustain the release of cationic MTO by electrostatic interaction. The results of a series of in vitro and in vivo investigations indicated that the TMLGNs were taken up by the resistant cancer cells by an endocytosis pathway that escaped the efflux induced by BCRP, and the simultaneous release of CsA with MTO further efficiently inhibited the efflux of the released MTO by BCRP; meanwhile GcNa induced the apoptosis process, and an associated synergistic antitumor activity and reversion of MDR were achieved because the reversal index was almost 1.0.

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“…The shell has the ability to interact with a wide variety of molecules, either within the membrane or on the surface of the membranes (129). Improved encapsulation of hydrophobic and hydrophilic drugs with therapeutically effective drug entrapment efficiency and drug loading have been reported in CSLPHNPs for a number of drugs compared to liposomes or PNPs (96,99,102). Amphiphilic character of lipids facilitates the adsorption of hydrophilic compounds on the hydrophilic bilayer surface and insertion of hydrophobic molecules into the hydrophobic lamellar region (129)(130)(131)(132).…”

Section: Advantages Of Cslphnpsmentioning

confidence: 99%

“…The macromolecules or proteins shows greatest loading efficiency near its isoelectric point when it has minimum solubility and maximum adsorption (147). For small molecules, the use of ionic interactions between the drug and polymer can be an effective way to increase the drug loading (96). Examples of the factors which may influence the DL and EE are aqueous solubility of the drug, affinity and miscibility of the drug in both polymer and lipid phases (96), amount of lipid (144), drug-lipid charge interactions (141), aqueous phase pH (148), and methods of preparation.…”

Section: Drug Loading and Entrapment Efficiency Of Cslphnpsmentioning

confidence: 99%

“…For small molecules, the use of ionic interactions between the drug and polymer can be an effective way to increase the drug loading (96). Examples of the factors which may influence the DL and EE are aqueous solubility of the drug, affinity and miscibility of the drug in both polymer and lipid phases (96), amount of lipid (144), drug-lipid charge interactions (141), aqueous phase pH (148), and methods of preparation. Often it is required to carry out in-depth physicochemical characterization during preformulation studies to optimize LC and EE (149).…”

Section: Introductionmentioning

confidence: 99%

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Design, Development and Evaluation of Erlotinib-Loaded Hybrid Nanoparticles for Targeted Drug Delivery to NonSmall Cell Lung Cancer

Mandal¹

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Molecular interactions, internal structure and drug release kinetics of rationally developed polymer–lipid hybrid nanoparticles

Cited by 93 publications

References 49 publications

Solid lipid based nanocarriers: An overview / Nanonosači na bazi čvrstih lipida: Pregled

Solid lipid based nanocarriers: An overview / Nanonosači na bazi čvrstih lipida: Pregled

Synergistic and complete reversal of the multidrug resistance of mitoxantrone hydrochloride by three-in-one multifunctional lipid-sodium glycocholate nanocarriers based on simultaneous BCRP and Bcl-2 inhibition

Design, Development and Evaluation of Erlotinib-Loaded Hybrid Nanoparticles for Targeted Drug Delivery to NonSmall Cell Lung Cancer

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