Influence of stearic acid and beeswax as solid lipid matrix of lipid nanoparticles containing tacrolimus

Dantas, Isabella Lima; Bastos, Kelven Tadeu S.; Machado, Micheline; Galvão, Juliana Gouveia; Lima, Alyne Dantas; Gonsalves, Joyce Kelly M.C.; Almeida, Ellen Denise Prado; Araújo, Adriano A. S.; Meneses, C.T.; Sarmento, Víctor Hugo Vitorino; Nunes, Rogéria de Souza; Lira, Ana Amélia Moreira

doi:10.1007/s10973-018-7072-7

Cited by 39 publications

(15 citation statements)

References 51 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The XRD data for TAC, PCL, PM, non-loaded, and TAC-loaded nanocapsules are shown in Figure 3. Regarding the pure drug, intense peaks of crystallinity between 2θ = 5 and 25 • were achieved as previously reported [39][40][41][42][43], while PCL proved its semicrystalline nature with characteristic peaks at 2θ of 21.45 and 23.73 • [30,44,45]. The PM shows crystallinity peaks coincident with those observed for the drug and the polymer.…”

Section: X-ray Diffraction (Xrd)supporting

confidence: 80%

“…In all formulations, the crystallinity peaks of PCL appeared. [39,41,43] observed that the TAC incorporation into nanosystems leads to a disorder in the crystalline system and thus reduces its structural organization. The absence of drug peaks in the XRD of NCs may be due to the low amount of the drug or the total conversion of the drug into its amorphous form during their preparation.…”

Section: X-ray Diffraction (Xrd)mentioning

confidence: 99%

See 1 more Smart Citation

Characterization and In Vitro and In Vivo Evaluation of Tacrolimus-Loaded Poly(ε-Caprolactone) Nanocapsules for the Management of Atopic Dermatitis

et al. 2021

View full text Add to dashboard Cite

Background: Tacrolimus (TAC) is a drug of natural origin used in conventional topical dosage forms to control atopic dermatitis. However, direct application of the drug often causes adverse side effects in some patients. Hence, drug nanoencapsulation could be used as an improved novel therapy to mitigate the adverse effects and enhance bioavailability of the drug. Methods: Physicochemical properties, in vitro drug release experiments, and in vivo anti-inflammatory activity studies were performed. Results: TAC-loaded nanocapsules were successfully prepared by the interfacial deposition of preformed polymer using poly(ε-caprolactone) (PCL). The nanoparticulate systems presented a spherical shape with a smooth and regular surface, adequate diameter (226 to 250 nm), polydispersity index below 0.3, and suitable electrical stability (−38 to −42 mV). X-ray diffraction confirmed that the encapsulation method provided mainly the drug molecular dispersion in the nanocapsule oily core. Fourier-transform infrared spectra suggested that nanoencapsulation did not result in chemical bonds between drug and polymer. In vitro drug dissolution experiments showed a controlled release with a slight initial burst. The release kinetics showed zero-order kinetics. As per the Korsmeyer–Peppas model, anomalous transport features were observed. TAC-loaded PCL nanocapsules exhibited excellent anti-inflammatory activity when compared to the free drug. Conclusions: TAC-loaded PCL nanocapsules can be suitably used as a novel nano-based dosage form to control atopic dermatitis.

show abstract

Section: X-ray Diffraction (Xrd)supporting

confidence: 80%

Section: X-ray Diffraction (Xrd)mentioning

confidence: 99%

Characterization and In Vitro and In Vivo Evaluation of Tacrolimus-Loaded Poly(ε-Caprolactone) Nanocapsules for the Management of Atopic Dermatitis

et al. 2021

View full text Add to dashboard Cite

show abstract

“…Therefore, the particle size of GDS‐NLC was smaller (Table 1) and its EPA entrapment rate was higher (Table 4). During the processes of storage, transportation and application, NLC with a lower RI value is conducive to preventing the leakage and oxidation of embedded bioactive substances (Truong et al ., 2016; Dantas et al ., 2018). Compared with triglycerides with the same chain length, diglycerides formed more lattice defects during the recrystallisation process to entrap more EPA (Jenning et al ., 2001; Salminen et al ., 2014).…”

Section: Resultsmentioning

confidence: 99%

Influence of different solid lipids on the properties of a novel nanostructured lipid carrier containing Antarctic krill oil

Lin

Yin

et al. 2022

Int J of Food Sci Tech

View full text Add to dashboard Cite

Summary This study aimed to investigate the effect of solid lipids (lauric acid (LAU), myristic acid (MYR), stearic acid (STE), glycerol monostearate (GMS), glycerol 1,3‐distearate (GDS), glycerol tristearate (GTS), glycerol trimyristate (GTM) and glycerol trilaurate (GTL)) on the characteristics of novel nanostructured lipid carrier (NLC) containing Antarctic krill oil through ultrasound. The fatty acids (LAU, MYR, STE and GMS) were unsuitable solid lipid materials, as apparent stratification was quickly observed during the NLC preparation. NLCs were successfully prepared using GTS, GTM, GTL and GDS. The zeta potential of all NLCs exceeded −30 mV indicating good uniformity and stability. These NLCs appeared spherical or oval. Differential calorimetry and X‐ray diffraction analysis revealed these NLCs formed imperfect crystals. As the carbon chain length of triglycerides increased from C12 to C18, the particle size of NLCs increased from 235.8 ± 2.3 nm to 340.5 ± 2.2 nm, the degree of recrystallisation increased from 39.06% to 49.99%, while the EPA encapsulation efficiency decreased from 88.72 ± 0.47% to 72.86 ± 1.06%. NLC prepared with GDS had the smallest particle size (112.4 ± 0.4 nm), the lowest recrystallisation and the highest EPA encapsulation efficiency (>99%). GDS was the most suitable to prepare high encapsulate efficiency krill oil‐loaded NLC.

show abstract

“…This allowed the packing of SA in the SLN core in minimal space. This observation by Dantas et al stated that the presence of the lipophilic drug in beeswax (solid lipid) resulted in a loss of lipid crystallinity [12].…”

Section: Physicochemical Properties Of Sln Nlc and Lementioning

confidence: 96%

Engineered Nanoscale Lipid-Based Formulation as Potential Enhancer of Gefitinib Lymphatic Delivery: Cytotoxicity and Apoptotic Studies Against the A549 Cell Line

et al. 2022

View full text Add to dashboard Cite

The present study aimed to engineer a nanoscale lipid-based lymphatic drug delivery system with D-α-Tocopherol polyethylene glycol 1000 succinate to combat the lymphatic metastasis of lung cancer. The nanoscale lipid-based systems including GEF-SLN, GEF-NLC, and GEF-LE were prepared and pharmaceutically characterized. In addition, the most stable formulation (GEF-NLC) was subjected to an in vitro release study. Afterward, the optimized GEF-NLC was engineered with TPGS (GEF-TPGS-NLC) and subjected to in vitro cytotoxicity, and apoptotic studies using the A549 cells line as a surrogate model for lung cancer. The present results revealed that particle size and polydispersity index of freshly prepared formulations were ranging from 198 to 280 nm and 0.106 to 0.240, respectively, with negative zeta potential ranging from − 14 to − 27.6.mV. An in vitro release study showed that sustained drug release was attained from GEF-NLC containing a high concentration of lipid. In addition, GEF-NLC and GEF-TPGS-NLC showed remarkable entrapment efficiency above 89% and exhibited sustained release profiles. Cytotoxicity showed that IC 50 of pure GEF was 11.15 μg/ml which decreased to 7.05 μg/ml for GEF-TPGS-NLC. The apoptotic study revealed that GEF-TPGS-NLC significantly decreased the number of living cells from 67 to 58% when compared with pure GEF. The present results revealed that the nanoscale and lipid composition of the fabricated SLN, NLC, and LE could mediate the lymphatic uptake of GEF to combat the lymphatic tumor metastasis. Particularly, GEF-TPGS-NLC is a promising LDDS to increase the therapeutic outcomes of GEF during the treatment of metastatic lung cancer.

show abstract

Influence of stearic acid and beeswax as solid lipid matrix of lipid nanoparticles containing tacrolimus

Cited by 39 publications

References 51 publications

Characterization and In Vitro and In Vivo Evaluation of Tacrolimus-Loaded Poly(ε-Caprolactone) Nanocapsules for the Management of Atopic Dermatitis

Characterization and In Vitro and In Vivo Evaluation of Tacrolimus-Loaded Poly(ε-Caprolactone) Nanocapsules for the Management of Atopic Dermatitis

Influence of different solid lipids on the properties of a novel nanostructured lipid carrier containing Antarctic krill oil

Engineered Nanoscale Lipid-Based Formulation as Potential Enhancer of Gefitinib Lymphatic Delivery: Cytotoxicity and Apoptotic Studies Against the A549 Cell Line

Contact Info

Product

Resources

About