Rapamycin-loaded solid lipid nanoparticles: Morphology and impact of the drug loading on the phase transition between lipid polymorphs

Mazuryk, Jarosław; Deptuła, Tobiasz; Polchi, Alice; Gapiński, Jacek; Giovagnoli, Stefano; Magini, Alessandro; Emiliani, Carla; Kohlbrecher, J.; Patkowski, A.

doi:10.1016/j.colsurfa.2016.05.017

Cited by 25 publications

(8 citation statements)

References 69 publications

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“…When firstly developed, SLN were presented as tiny and spherical particles, made of solid lipids at room temperature, that may be thought as perfect crystal lipid matrices, able to accommodate a drug or other molecules between fatty acid chains (Puri et al, 2009). Nowadays, however, it is known that this is not necessarily true in all cases, since disc-like shape or flat ellipsoidal geometry have also been described (Mazuryk et al, 2016;Shah et al, 2019). Moreover, the loaded drug may be attached mostly to the carrier matrix surface instead of being embedded into the solid core (Pink et al, 2019;Shah et al, 2019).…”

Section: The Tiny Big Universe Of Lipid Nanoparticlesmentioning

confidence: 99%

Solid Lipid Nanoparticles for Drug Delivery: Pharmacological and Biopharmaceutical Aspects

Montoto

Muraca

Ruiz

2020

Front. Mol. Biosci.

338

148

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Section: The Tiny Big Universe Of Lipid Nanoparticlesmentioning

confidence: 99%

Solid Lipid Nanoparticles for Drug Delivery: Pharmacological and Biopharmaceutical Aspects

Montoto

Muraca

Ruiz

2020

Front. Mol. Biosci.

338

148

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“…In the particular case of lipid NPs, AFM observation is considered a complementary method, particularly useful for observing the shape of the particles ( Peixoto et al, 2005 ). On the other hand, the technique is less relevant for the quantification of dimensions, since particles’ deformation usually occurs ( Dubes et al, 2003 ; Mazuryk et al, 2016 ).…”

Section: Resultsmentioning

confidence: 99%

Novel Phenobarbital-Loaded Nanostructured Lipid Carriers for Epilepsy Treatment: From QbD to In Vivo Evaluation

et al. 2022

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Pharmacological treatments of central nervous system diseases are always challenging due to the restrictions imposed by the blood–brain barrier: while some drugs can effectively cross it, many others, some antiepileptic drugs among them, display permeability issues to reach the site of action and exert their pharmacological effects. The development of last-generation therapeutic nanosystems capable of enhancing drug biodistribution has gained ground in the past few years. Lipid-based nanoparticles are promising systems aimed to improve or facilitate the passage of drugs through biological barriers, which have demonstrated their effectiveness in various therapeutic fields, without signs of associated toxicity. In the present work, nanostructured lipid carriers (NLCs) containing the antiepileptic drug phenobarbital were designed and optimized by a quality by design approach (QbD). The optimized formulation was characterized by its entrapment efficiency, particle size, polydispersity index, and Z potential. Thermal properties were analyzed by DSC and TGA, and morphology and crystal properties were analyzed by AFM, TEM, and XRD. Drug localization and possible interactions between the drug and the formulation components were evaluated using FTIR. In vitro release kinetic, cytotoxicity on non-tumoral mouse fibroblasts L929, and in vivo anticonvulsant activity in an animal model of acute seizures were studied as well. The optimized formulation resulted in spherical particles with a mean size of ca. 178 nm and 98.2% of entrapment efficiency, physically stable for more than a month. Results obtained from the physicochemical and in vitro release characterization suggested that the drug was incorporated into the lipid matrix losing its crystalline structure after the synthesis process and was then released following a slower kinetic in comparison with the conventional immediate-release formulation. The NLC was non-toxic against the selected cell line and capable of delivering the drug to the site of action in an adequate amount and time for therapeutic effects, with no appreciable neurotoxicity. Therefore, the developed system represents a promising alternative for the treatment of one of the most prevalent neurological diseases, epilepsy.

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“…The investigational data also revealed that the efficiency was found to be less at low (−1) level as compared to central (0) level of factor A (lipid-to-surfactant ratio) along with factor B (polymer) had pronounced effect. This result evident that the efficiency and loading capacity was higher toward at central level of factor A and B lipids but at high (+1) level, it declined because of high lipid concentration made particles like mixed micelle (due to lipid association with surfactant particle), which made them as low-loading drug carrier [ 40 ], whereas factors A and C have direct relationship rather than B and C inversely proportional to EE. The combination of two factors at a time effect on SLNbp EE (R1) has also been shown by two- (contour) and three-dimensional (response surface) plots (Figs 2a , 3a , and 4a ) simultaneously.…”

Section: Resultsmentioning

confidence: 99%

Nano-colloidal carrier via polymeric coating for oral delivery of isradipine

Kumar

Chaudhary²,

Kamboj³

2017

Interventional Medicine and Applied Science

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Our research objective was to develop, characterize, and optimize stable form of nano-colloidal carrier with Eudragit-coated solid lipid nanobioparticles (SLNbp) for oral delivery of isradipine (ISR). To achieve, a three factors, i.e., lipid-to-surfactant ratio (A, % w/w), Eudragit L100 (B, % w/w), and sonication time (C, minutes) at three levels (−1 and +1 levels of quality central level) was applied to develop SLNbp using response surface methodology at constant ratio of ISR and rutin. The second-order polynomial quadratic equations of responses [R1, R2, and R3; entrapment efficiency (EE), particle size, and drug release] were constructed and also plotted response surface (two- and three-dimensional) plots. The derived polynomial equation and 2D and 3D model were showed the relationship between the responses of the selected independent variables (A, B, and C). The model validation and optimization was performed by numerical checkpoint analysis to predict the optimized solid lipid nanobioparticle formulas (ONbp 1–10). The optimized formulations prepared and during evaluation ONbp 3 has better smaller particle size (106 nm), sustainable release (95.61% up to 40 h), higher EE (97.85%), and drug content (99.92% ± 0.08%) during 3-month storage showed good stability. Therefore, its performance can be considered for further development of stable oral drug delivery system of ISR.

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Rapamycin-loaded solid lipid nanoparticles: Morphology and impact of the drug loading on the phase transition between lipid polymorphs

Cited by 25 publications

References 69 publications

Solid Lipid Nanoparticles for Drug Delivery: Pharmacological and Biopharmaceutical Aspects

Solid Lipid Nanoparticles for Drug Delivery: Pharmacological and Biopharmaceutical Aspects

Novel Phenobarbital-Loaded Nanostructured Lipid Carriers for Epilepsy Treatment: From QbD to In Vivo Evaluation

Nano-colloidal carrier via polymeric coating for oral delivery of isradipine

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