Altered chemical and biological activities of all-trans retinoic acid incorporated in solid lipid nanoparticle powders

2004 ◽  
Vol 100 (1) ◽  
pp. 53-61 ◽  
Author(s):  
Soo-Jeong Lim ◽  
Mi-Kyung Lee ◽  
Chong-Kook Kim
Keyword(s):  
Retinoic Acid ◽  
Biological Activities ◽  
Solid Lipid Nanoparticle ◽  
Solid Lipid ◽  
Trans Retinoic Acid ◽  
Lipid Nanoparticle ◽  
All Trans Retinoic Acid

Enhanced Oral Absorption of All-trans Retinoic Acid upon Encapsulation in Solid Lipid Nanoparticles

2020 ◽  
Vol 8 (6) ◽  
pp. 495-510
Author(s):  
Manoj Kumar ◽  
Garima Sharma ◽  
Dinesh Singla ◽  
Sukhjeet Singh ◽  
Vandita Kakkar ◽  
...  
Keyword(s):  
Retinoic Acid ◽  
Side Effects ◽  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Lipid Nanoparticles ◽  
Solid Lipid ◽  
Trans Retinoic Acid ◽  
All Trans Retinoic Acid ◽  
Vitro Release

Background:: All-trans retinoic acid (ATRA) is widely employed in the treatment of various proliferative and inflammatory diseases. However, its therapeutic efficacy is imperiled due to its poor solubility and stability. Latter was surmounted by its incorporation into a solid matrix of lipidic nanoparticles (SLNs). Methods:: ATRA loaded SLNs (ATRA-SLNs) were prepared using a novel microemulsification technique (USPTO 9907758) and an optimal composition and were characterized in terms of morphology, differential scanning calorimetry (DSC), and powder X-ray diffraction studies (PXRD). In vitro release, oral plasma pharmacokinetics (in rats) and stability studies were also done. Results:: Rod-shaped ATRA-SLNs could successfully incorporate 3.7 mg/mL of ATRA, increasing its solubility (from 4.7 μg/mL) by 787 times, having an average particle size of 131.30 ± 5.0 nm and polydispersibility of 0.283. PXRD, DSC, and FTIR studies confirmed the formation of SLNs. Assay/total drug content and entrapment efficiency of ATRA-SLNs was 92.50 ± 2.10% and 84.60 ± 3.20% (n=6), respectively, which was maintained even on storage for one year under refrigerated conditions as an aqueous dispersion. In vitro release in 0.01 M phosphate buffer (pH 7.4) with 3% tween 80 was extended 12 times from 2h for free ATRA to 24 h for ATRA-SLNs depicting Korsmeyer Peppas release. Oral administration in rats showed 35.03 times enhanced bioavailability for ATRA-SLNs. Conclusion:: Present work reports preparation and evaluation of bioenhanced ATRA-SLNs containing a high concentration of ATRA (>15 times than that reported by others). Latter is attributed to the novel preparation process and intelligent selection of components. Lay Summary: All-trans retinoic acid (ATRA) shows an array of pharmacological activities but its efficacy is limited due to poor solubility, stability and side effects. In present study its solubility and efficacy is improved by 787 and 35.5 times, respectively upon incorporation into solid lipid nanoparticles (ATRA-SLNs). Latter extended its release by 12 times and provided stability for at least a year under refrigeration. A controlled and sustained release will reduce dose related side effects. ATRA-SLNs reported presently can thus be used in treatment /prophylaxis of disorders like cancers, tuberculosis, age related macular degeneration and acne and as an immune-booster.

Development of a new solid lipid nanoparticle formulation containing retinoic acid for topical treatment of acne

2007 ◽  
Vol 24 (5) ◽  
pp. 395-407 ◽  
Author(s):  
Gisele A. Castro ◽  
Rodrigo L. Oréfice ◽  
José M. C. Vilela ◽  
Margareth S. Andrade ◽  
Lucas A. M. Ferreira
Keyword(s):  
Retinoic Acid ◽  
Topical Treatment ◽  
Solid Lipid Nanoparticle ◽  
Solid Lipid ◽  
Lipid Nanoparticle ◽  
Nanoparticle Formulation

Temperature-induced release of all-trans-retinoic acid loaded in solid lipid nanoparticles for topical delivery

2008 ◽  
Vol 16 (8) ◽  
pp. 682-685 ◽  
Author(s):  
Chang-Moon Lee ◽  
Hwan-Jeong Jeong ◽  
Ji-Won Park ◽  
Jin Kim ◽  
Ki-Young Lee
Keyword(s):  
Retinoic Acid ◽  
Solid Lipid Nanoparticles ◽  
Topical Delivery ◽  
Lipid Nanoparticles ◽  
Solid Lipid ◽  
Trans Retinoic Acid ◽  
All Trans Retinoic Acid

Improved In Vitro Antileukemic Activity of All-Trans Retinoic Acid Loaded in Cholesteryl Butyrate Solid Lipid Nanoparticles

2016 ◽  
Vol 16 (2) ◽  
pp. 1291-1300 ◽  
Author(s):  
Elton Luiz Silva ◽  
Flávia Alves Lima ◽  
Guilherme Carneiro ◽  
Jonas Pereira Ramos ◽  
Dawidson Assis Gomes ◽  
...  
Keyword(s):  
Retinoic Acid ◽  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Antileukemic Activity ◽  
Solid Lipid ◽  
Trans Retinoic Acid ◽  
All Trans Retinoic Acid
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