Polymeric Nanoparticle Versus Liposome Formulations: Comparative Physicochemical and Metabolomic Studies as l -Carnitine
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Research Article Polymeric Nanoparticle Versus Liposome Formulations: Comparative Physicochemical and Metabolomic Studies as L-Carnitine Delivery Systems Merve Yaşacan,1,2 Açelya Erikçi,3 Cemil Can Eylem,4 Samiye Yabanoğlu Çiftçi,5 Emirhan Nemutlu,4 Kezban Ulubayram,1,6 and İpek Eroğlu1,6,7 Received 14 August 2020; accepted 12 October 2020 Abstract. L-Carnitine has attracted much more attention especially in the treatment of crucial diseases such as diabetes, regional slimming, and obesity because of its metabolic activities. However, because of its short half-life, low bioavailability, and inability to be stored in the body, frequent dosing is required. In this study, L-carnitine-loaded liposome (lipocarnitine) and PLGA nanoparticle (nano-carnitine) formulations were prepared and characterized. For lipo-carnitine and nano-carnitine formulations, particle size values were 97.88 ± 2.96 nm and 250.90 ± 6.15 nm; polydispersity index values were 0.35 ± 0.01 and 0.22 ± 0.03; zeta potential values were 6.36 ± 0.54 mV and − 32.80 ± 2.26 mV; and encapsulation efficiency percentage values were 14.26 ± 3.52% and 21.93 ± 4.17%, respectively. Comparative in vitro release studies of novel formulations and solution of L-carnitine revealed that Lcarnitine released 90% of its content at the end of 1st hour. On the other hand, lipo-carnitine and nano-carnitine formulations maintained a controlled-release profile for 12 h. The in vitro efficacy of the formulations on cardiac fibroblasts (CFs) was evaluated by metabolomic studies and pathway analysis. Besides the prolonged release, lipo-carnitine/nano-carnitine formulations were also found to be effective on amino acid, carbohydrate, and lipid metabolisms. As a result, innovative nano-formulations were successfully developed as an alternative to conventional preparations which are available on the market. KEY WORDS: nanoparticle(s); liposome(s); polyglycolic acid (PLGA); controlled release; drug delivery system(s).
INTRODUCTION L-Carnitine is a naturally occurring compound in the human body and also a critical co-factor in fatty acid metabolism; it facilitates the entrance of long-chain fatty acids into mitochondria, where it is metabolized for energy production. Although it is both endogenously and
Supplementary Information The online version contains supplementary material available at https://doi.org/10.1208/s12249-020-01852-4. 1
Nanotechnology and Nanomedicine Division, Institute for Graduate Studies in Science and Engineering, Hacettepe University, Ankara, Turkey. 2 ASELSAN Inc., Teknopark Istanbul, 34906, Istanbul, Turkey. 3 Department of Biochemistry, Faculty of Pharmacy, Lokman Hekim University, Ankara, Turkey. 4 Department of Analytical Chemistry, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey. 5 Department of Biochemistry, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey. 6 Department of Basic Pharmaceutical Sciences, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey. 7 To whom correspondence should be addressed. (e–mail: [email protected])
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