Selection and Characterization of Suitable Lipid Excipients for use in the Manufacture of Didanosine-Loaded Solid Lipid Nanoparticles and Nanostructured Lipid Carriers

Kasongo, W.A.; Pardeike, Jana; Müller, Rainer H.; Walker, Roderick B.

doi:10.1002/jps.22711

Cited by 99 publications

(39 citation statements)

References 20 publications

(32 reference statements)

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“…In selecting lipids for NLC development, it is necessary to consider the compatibility between solid and liquid lipids. Kasongo and co-workers [12] used the differential scanning calorimetry (DSC) in order to determine the interaction between solid and liquid lipids in a binary mixture. The stability related to chemical degradation (e.g., oxidation and lipolysis) of the lipid phase should be considered as well.…”

Section: Introductionmentioning

confidence: 99%

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Effect of Ouratea sp. butter in the crystallinity of solid lipids used in nanostructured lipid carriers (NLCs)

Galvão

Trindade

Santos

et al. 2015

J Therm Anal Calorim

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The aim of this work was to evaluate the effect of Ouratea sp. butter (OB) on crystallinity of solid lipids used in nanostructured lipid carriers systems. Firstly, the composition of fatty acids in OB was evaluated by transesterification reaction for gas chromatography fatty acid methyl ester analysis. The solid lipids such as stearic acid (SA), beeswax (BW) and carnauba wax (CW) were submitted to recrystallization process (heating-cooling). Moreover, binary mixtures between solid lipids and OB were prepared in ratio 1:1 (w/w) by heating of the components above the melting point followed by cooling at room temperature. Thus, the samples were characterized by differential scanning calorimetry (DSC), thermogravimetry (TG), X ray diffraction (XRD) and hot-stage polarized optical microscopy (HSPOM). DSC curves showed a shift of the melting point to lower temperatures in the lipid mixtures with OB. TG data suggested a thermal stability reduction in the lipid mixtures containing SA and CW and an increase thermal stability in the mixture containing BW. XRD data confirmed DSC results, showing a reduction in intensity of main diffraction peaks of the lipid mixtures and a presence of the amorphous portion in angle 2h: 22°. Finally, HSPOM demonstrated that the microstructures of solid lipids decreased in size and thickness in the mixtures containing OB at room temperature and slightly before the melting point, confirming previous characterizations. These results suggest that lipid mixtures with OB present a lower crystallinity, and it is expected that amorphous portion facilitates drug incorporation, for example.

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Section: Introductionmentioning

confidence: 99%

“…The stability related to chemical degradation (e.g., oxidation and lipolysis) of the lipid phase should be considered as well. Furthermore, the lipids should be biodegradable, be non-toxic and be capable of producing particles in nanometric range [8,12,13].…”

Section: Introductionmentioning

confidence: 99%

Effect of Ouratea sp. butter in the crystallinity of solid lipids used in nanostructured lipid carriers (NLCs)

Galvão

Trindade

Santos

et al. 2015

J Therm Anal Calorim

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“…The application of NLCs to the treatment and prevention of infectious diseases has been attempted in various studies focused on the development of new antimalarial treatments [86–88] or in the improvement of encapsulation of hydrophilic antiretroviral drugs [89–91]. Although there are few reports about the application of NLCs as RNAi delivery systems, they could be an interesting alternative in codelivery strategies with conventional drugs.…”

Section: Lipid Nanoparticles (Lnp)mentioning

confidence: 99%

Lipid Nanoparticles as Carriers for RNAi against Viral Infections: Current Status and Future Perspectives

Torrecilla

Rodríguez-Gascón

Solinís

et al. 2014

BioMed Research International

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The efforts made to develop RNAi-based therapies have led to productive research in the field of infections in humans, such as hepatitis C virus (HCV), hepatitis B virus (HBV), human immunodeficiency virus (HIV), human cytomegalovirus (HCMV), herpetic keratitis, human papillomavirus, or influenza virus. Naked RNAi molecules are rapidly digested by nucleases in the serum, and due to their negative surface charge, entry into the cell cytoplasm is also hampered, which makes necessary the use of delivery systems to exploit the full potential of RNAi therapeutics. Lipid nanoparticles (LNP) represent one of the most widely used delivery systems for in vivo application of RNAi due to their relative safety and simplicity of production, joint with the enhanced payload and protection of encapsulated RNAs. Moreover, LNP may be functionalized to reach target cells, and they may be used to combine RNAi molecules with conventional drug substances to reduce resistance or improve efficiency. This review features the current application of LNP in RNAi mediated therapy against viral infections and aims to explore possible future lines of action in this field.

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“…Although a systematic and standard procedure of selecting an appropriate solid lipid has not been published yet, some criteria have been defined in the literature, such as qualitative solubility 21,26 and partitioning behavior. 22,27 Among the screened solid lipids, four lipids (palmitic acid, stearic acid, Precirol ATO 5, and Geleol) showed similar ability to dissolve TP (1.0-1.25 mg/g), with a relatively higher solubility that was found in Compritol 888 ATO (1.4 mg/g).…”

Section: Preparation Of Tp-nlcs Screening Of Lipidsmentioning

confidence: 99%

Nanostructured lipid carriers as a novel oral delivery system for triptolide: induced changes in pharmacokinetics profile associated with reduced toxicity in male rats

Zhang¹,

Fan²,

Liu³

et al. 2014

IJN

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After oral administration in rodents, triptolide (TP), a diterpenoid triepoxide compound, active as anti-inflammatory, immunosuppressive, anti-fertility, anti-cystogenesis, and anticancer agent, is rapidly absorbed into the blood circulation (from 5.0 to 19.5 minutes after dosing, depending on the rodent species) followed by a short elimination half-life (from about 20 minutes to less than 1 hour). Such significant and rapid fluctuations of TP in plasma likely contribute to its toxicity, which is characterized by injury to hepatic, renal, digestive, reproductive, and hematological systems. With the aim of prolonging drug release and improving its safety, TP-loaded nanostructured lipid carriers (TP-NLCs), composed of Compritol® 888 ATO (solid lipid) and Capryol™ 90 (liquid lipid), were developed using a microemulsion technique. The formulated TP-NLCs were also characterized and in vitro release was evaluated using the dialysis bag diffusion technique. In addition, the pharmacokinetics and toxicology profiles of TP-NLCs were compared to free TP and TP-loaded solid lipid nanoparticles (TP-SLNs; containing Compritol 888 ATO only). Results demonstrate that TP-NLCs had mean particle size of 231.8 nm, increased drug encapsulation with a 71.6% efficiency, and stable drug incorporation for over 1-month. TP-NLCs manifested a better in vitro sustained-release pattern compared to TP-SLNs. Furthermore, TP-NLCs prolonged mean residence time (MRT) 0–t ( P <0.001, P <0.001), delayed T max ( P <0.01, P <0.05) and decreased C max ( P <0.01, P <0.05) compared to free TP and TP-SLNs, respectively, which was associated with reduced subacute toxicity in male rats. In conclusion, our data suggest that TP-NLCs are superior to TP-SLNs and could be a promising oral delivery system for a safer use of TP.

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Selection and Characterization of Suitable Lipid Excipients for use in the Manufacture of Didanosine-Loaded Solid Lipid Nanoparticles and Nanostructured Lipid Carriers

Cited by 99 publications

References 20 publications

Effect of Ouratea sp. butter in the crystallinity of solid lipids used in nanostructured lipid carriers (NLCs)

Effect of Ouratea sp. butter in the crystallinity of solid lipids used in nanostructured lipid carriers (NLCs)

Lipid Nanoparticles as Carriers for RNAi against Viral Infections: Current Status and Future Perspectives

Nanostructured lipid carriers as a novel oral delivery system for triptolide: induced changes in pharmacokinetics profile associated with reduced toxicity in male rats

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