Abstract
Objectives
Betulin (BT) is an abundant triterpene found predominantly in the bark of Himalayan birch. It is difficult to deliver it in vivo because of its low aqueous solubility. We have therefore developed novel formulations of BT for improving its solubility, bioavailability and therapeutic efficacy.
Results
Poly-d,l-lactide nanovectors (PLA NVs) were synthesized using poly(vinyl alcohol) and Lonicera japonica leaf extract (LE) as a stabiliser and named as PLA-1 NVs and PLA-2 NVs. PLA-1 NVs and PLA-2 NVs were used for the encapsulation of betulin (BT) and named as BT-En-1 and BT-En-2 NVs. The encapsulation efficiency of BT-En-1 and BT-En-2 NVs were 99.3 and 100 % respectively. Prepared nanoformulations were physically stable. An in vitro study revealed 45 % BT was released over 24 h. BT had a prolonged release from BT-En-2 NVs as compared to BT-En-1 NVs. BT-En-2 NVs had better anticancerous activity against SiHa cells than BT-En-1 NVs.
Conclusions
Developed BT-EN-2 NVs had better biocompatibility, excellent stability and enhanced release characteristics than BT-En-1 NVs.
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Acknowledgments
Authors acknowledge Council of Scientific and Industrial Research, India for providing Senior Research Fellowship to RY. Authors are thankful to the Director, CSIR-IHBT, Palampur for continuous support and encouragement. Financial support in the form of research grant BSC-112 from CSIR is duly acknowledged. RY is also thankful to Academy of Scientific and Innovative Research, New Delhi.
Supporting information
Supplementary Fig. 1—FTIR spectra of PLA -1 NPs and PLA-2 NPs.
Supplementary Fig. 2—Chracteriztion of PLA-1 NPs using AFM, TEM and DLS. AFM image of PLA-1 NPs (a) and TEM image of PLA-1 NPs (b). DLS size of PLA-1 NPs (c).
Supplementary Fig. 3—Chracterization of PLA-2 NPs using AFM, TEM and DLS. AFM image of PLA-2 NPs (a) and TEM image of PLA-2 NPs (b). DLS size of PLA-2 NPs (c).
Supplementary Fig. 4—Zeta potential and TEM image of PLA-1 NPs, PLA-2 NPs, BT-En-1 NPs and BT-En-2 NPs. PLA-1 NPs, PLA-2 NPs, BT-En-1 NPs and BT-En-2 NPs were stored at 37 °C for 45 days and TEM and zeta potential measurements were carried out to study their stability.
Supplementary Fig. 5—HPLC overlapped chromatograms of pure BT (a) and calibration curve of pure BT obtained using various concentration 1, 0.5, 0.25, 0.125, 0.0625 mg/ml) (b). The overlapped chromatogram of supernatants obtained after the seperation of various NPs through centrifugation (c).
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Yadav, R., Kumar, D., Kumari, A. et al. PLA nanovectors with encapsulated betulin: plant leaf extract-synthesized nanovectors are more efficacious than PVA-synthesized nanovectors. Biotechnol Lett 38, 259–269 (2016). https://doi.org/10.1007/s10529-015-1981-3
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DOI: https://doi.org/10.1007/s10529-015-1981-3