Evaluation of miscibility and polymorphism of synthetic and natural lipids for nanostructured lipid carrier (NLC) formulations by Raman mapping and multivariate curve resolution (MCR)

Mitsutake, Hery; Ribeiro, Lígia Nunes de Morais; Silva, Gustavo Henrique Rodrigues da; Castro, Simone R.; Paula, Eneida de; Poppi, Ronei J.; Breitkreitz, Márcia Cristina

doi:10.1016/j.ejps.2019.05.002

Cited by 18 publications

(24 citation statements)

References 31 publications

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“…These results also explain the instability of CP-TRANS under storage, as revealed by DLS (Fig. 6 ), and confirm the applicability of Raman mapping for the selection of excipients in pharmaceutical studies 22 , 23 . So, for stability reasons, only the formulations containing DK as the liquid lipid were used in subsequent steps.…”

Section: Resultssupporting

confidence: 80%

A pre-formulation study of tetracaine loaded in optimized nanostructured lipid carriers

Castro

Ribeiro

Breitkreitz

et al. 2021

Sci Rep

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Tetracaine (TTC) is a local anesthetic broadly used for topical and spinal blockade, despite its systemic toxicity. Encapsulation in nanostructured lipid carriers (NLC) may prolong TTC delivery at the site of injection, reducing such toxicity. This work reports the development of NLC loading 4% TTC. Structural properties and encapsulation efficiency (%EE > 63%) guided the selection of three pre-formulations of different lipid composition, through a 23 factorial design of experiments (DOE). DLS and TEM analyses revealed average sizes (193–220 nm), polydispersity (< 0.2), zeta potential |− 21.8 to − 30.1 mV| and spherical shape of the nanoparticles, while FTIR-ATR, NTA, DSC, XRD and SANS provided details on their structure and physicochemical stability over time. Interestingly, one optimized pre-formulation (CP-TRANS/TTC) showed phase-separation after 4 months, as predicted by Raman imaging that detected lack of miscibility between its solid (cetyl palmitate) and liquid (Transcutol) lipids. SANS analyses identified lamellar arrangements inside such nanoparticles, the thickness of the lamellae been decreased by TTC. As a result of this combined approach (DOE and biophysical techniques) two optimized pre-formulations were rationally selected, both with great potential as drug delivery systems, extending the release of the anesthetic (> 48 h) and reducing TTC cytotoxicity against Balb/c 3T3 cells.

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Section: Resultssupporting

confidence: 80%

A pre-formulation study of tetracaine loaded in optimized nanostructured lipid carriers

Castro

Ribeiro

Breitkreitz

et al. 2021

Sci Rep

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“…On liquid excipients, like sesame oil, bands at 800–900 cm −1 are related to -(CH2)n- stretching [ 57 ]. Weak peaks from 1736 to 1748 cm −1 are related to the carbonyl bond (C=O), which can be seen in the spectra of cocoa butter, P80H, sesame oil, and Tween 80 [ 58 , 59 ].…”

Section: Resultsmentioning

confidence: 99%

“…Peaks around 1330 are attributed to CH 2 twisting. The olefinic unsaturation C=C stretch or the conjugated double bond system showed a relatively strong absorption peak above 1650 cm −1 , which may be related to the presence of conjugated double bonds in geraniol, the major chemical compound present in PEO [ 59 , 61 ]. In addition, a peak at 2914 cm −1 is attributed to the symmetric C-H stretch [ 56 ].…”

Section: Resultsmentioning

confidence: 99%

Design of Nanostructured Lipid Carriers Containing Cymbopogon martinii (Palmarosa) Essential Oil against Aspergillus nomius

et al. 2021

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Palmarosa essential oil (PEO) is an alternative to synthetic fungicides to control the contamination by food-deteriorating fungi, such as Aspergillus nomius. Nonetheless, the low long-term stability and volatility hamper its utilization. Thus, this study aimed to develop nanostructured lipid carriers (NLCs) containing PEO to improve its stability and consequently prolong the activity against A. nomius. A mixture design was applied to find the best preparation conditions for antifungal activity. The characterization analyses included size measurements, zeta potential (ζ-potential), entrapment efficiency (EE), and antifungal activity (by inhibition of mycelial growth (IMG) and/or in situ test (pre-contaminated Brazil nuts) tests). The nanocarriers presented particle sizes smaller than 300 nm, homogeneous size distribution, ζ-potential of −25.19 to −41.81 mV, and EE between 73.6 and 100%. The formulations F5 and F10 showed the highest IMG value (98.75%). Based on the regression model, three optimized formulations (OFs) were tested for antifungal activity (IMG and in situ test), which showed 100% of inhibition and prevented the deterioration of Brazil nuts by A. nomius. The preliminary stability test showed the maintenance of antifungal activity and physicochemical characteristics for 90 days. These results suggest a promising system as a biofungicide against A. nomius.

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“…The lipid excipient miscibility and structural modifications (polymorphism) play an important role in formulation stability and are not easily predicted in the early pharmaceutical progress. Even if the excipients are macroscopically miscible, microscopic heterogeneity during storage will result in phase separation, which can only be observed after many months of stability studies [ 124 ]. As extensively detailed in Section 3.2.7 , phytosterols are biosynthetically derived from squalene.…”

Section: Nanoformulations Involving Vegetable Oil-based Nutraceutimentioning

confidence: 99%

Nutraceutical Vegetable Oil Nanoformulations for Prevention and Management of Diseases

Vergallo

2020

Nanomaterials

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The scientific community is becoming increasingly interested in identifying, characterizing, and delivering nutraceuticals, which constitutes a multi-billion-dollar business. These bioactive agents are claimed to exhibit several health benefits, including the prevention and treatment of diseases such as arthritis, cancer, osteoporosis, cataracts, Alzheimer’s, and Huntington’s diseases, heart, brain and metabolic disorders, etc. Nutraceuticals are typically consumed as part of a regular human diet and are usually present within foods, comprising vegetable oil, although at low levels and variable composition. Thus, it is difficult to control the type, amount and frequency of their ingestion by individuals. Nanoformulations about vegetable oil-based bioactive compounds with nutraceutical properties are useful for overcoming these issues, while improving the uptake, absorption, and bioavailability in the body. The purpose of this current study is to review papers on such nanoformulations, particularly those relevant for health benefits and the prevention and management of diseases, as well as bioactives extracted from vegetable oils enhancing the drug effectiveness, retrieved through bibliographic databases by setting a timespan from January 2000 to April 2020 (about 1758 records).

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Evaluation of miscibility and polymorphism of synthetic and natural lipids for nanostructured lipid carrier (NLC) formulations by Raman mapping and multivariate curve resolution (MCR)

Cited by 18 publications

References 31 publications

A pre-formulation study of tetracaine loaded in optimized nanostructured lipid carriers

A pre-formulation study of tetracaine loaded in optimized nanostructured lipid carriers

Design of Nanostructured Lipid Carriers Containing Cymbopogon martinii (Palmarosa) Essential Oil against Aspergillus nomius

Nutraceutical Vegetable Oil Nanoformulations for Prevention and Management of Diseases

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