Development and Optimization of Nano-Hydroxyapatite Encapsulating Tocotrienol-Rich Fraction Formulation Using Response Surface Methodology

<b>Background/Objective</b>: The tocotrienol-rich fraction (TRF) is a lipid-soluble vitamin that has good antioxidant and anti-inflammatory properties. The TRF is widely studied as a potential treatment for various diseases, including bone diseases. However, its application is limited du...

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Main Authors: Anis Syauqina Mohd Zaffarin, Shiow-Fern Ng, Min Hwei Ng, Haniza Hassan, Ekram Alias
Format: Article
Language:English
Published: MDPI AG 2024-12-01
Series:Pharmaceutics
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Online Access:https://www.mdpi.com/1999-4923/17/1/10
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author Anis Syauqina Mohd Zaffarin
Shiow-Fern Ng
Min Hwei Ng
Haniza Hassan
Ekram Alias
author_facet Anis Syauqina Mohd Zaffarin
Shiow-Fern Ng
Min Hwei Ng
Haniza Hassan
Ekram Alias
author_sort Anis Syauqina Mohd Zaffarin
collection DOAJ
description <b>Background/Objective</b>: The tocotrienol-rich fraction (TRF) is a lipid-soluble vitamin that has good antioxidant and anti-inflammatory properties. The TRF is widely studied as a potential treatment for various diseases, including bone diseases. However, its application is limited due to its poor oral bioavailability profile, warranting an innovative approach to overcome its pharmacokinetic limitations. Recently, the nano-hydroxyapatite (nHA) has been investigated as a drug delivery vehicle for various drugs and active compounds owing to its excellent biocompatibility, biodegradability, and osteogenic properties. The nHA is also a well-known biomaterial which has chemical and structural similarities to bone minerals. Hence, we aim to explore the use of the nHA as a potential nanocarrier for the TRF. <b>Methods</b>: In this study, we develop and optimize the formulation of an nHA-encapsulating TRF (nHA/TRF) by employing the response surface methodology (RSM). <b>Results</b>: RSM outcomes reveal that the mass of the nHA, the concentration of the TRF, and the incubation time have a significant effect on the particle size, zeta potential, and encapsulation efficiency of the nHA/TRF. The outcomes for the optimized formulation are not significantly different from the predicted RSM outcomes. The optimized nHA/TRF formulation is freeze-dried and results in an average particle size of ~270 nm, a negative zeta potential value of ~−20 mV, a polydispersity index of <0.4, and an encapsulation efficiency of ~18.1%. Transmission electron microscopy (TEM) shows that the freeze-dried nHA/TRF has a spherical structure. <b>Conclusions</b>: Taken together, the above findings indicate that the nHA may be established as a nanocarrier for efficient delivery of the TRF, as demonstrated by the promising physical properties.
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spelling doaj-art-84c28f637cc440d18ba93771b7ab8ade2025-01-24T13:45:34ZengMDPI AGPharmaceutics1999-49232024-12-011711010.3390/pharmaceutics17010010Development and Optimization of Nano-Hydroxyapatite Encapsulating Tocotrienol-Rich Fraction Formulation Using Response Surface MethodologyAnis Syauqina Mohd Zaffarin0Shiow-Fern Ng1Min Hwei Ng2Haniza Hassan3Ekram Alias4Department of Biochemistry, Faculty of Medicine, Universiti Kebangsaan Malaysia, Jalan Yaacob Latif, Bandar Tun Razak, Kuala Lumpur 56000, MalaysiaFaculty of Pharmacy, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz, Kuala Lumpur 50300, MalaysiaDepartment of Tissue Engineering and Regenerative Medicine, Faculty of Medicine, Universiti Kebangsaan Malaysia, Jalan Yaacob Latif, Bandar Tun Razak, Kuala Lumpur 56000, MalaysiaDepartment of Human Anatomy, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, Serdang 43400, MalaysiaDepartment of Biochemistry, Faculty of Medicine, Universiti Kebangsaan Malaysia, Jalan Yaacob Latif, Bandar Tun Razak, Kuala Lumpur 56000, Malaysia<b>Background/Objective</b>: The tocotrienol-rich fraction (TRF) is a lipid-soluble vitamin that has good antioxidant and anti-inflammatory properties. The TRF is widely studied as a potential treatment for various diseases, including bone diseases. However, its application is limited due to its poor oral bioavailability profile, warranting an innovative approach to overcome its pharmacokinetic limitations. Recently, the nano-hydroxyapatite (nHA) has been investigated as a drug delivery vehicle for various drugs and active compounds owing to its excellent biocompatibility, biodegradability, and osteogenic properties. The nHA is also a well-known biomaterial which has chemical and structural similarities to bone minerals. Hence, we aim to explore the use of the nHA as a potential nanocarrier for the TRF. <b>Methods</b>: In this study, we develop and optimize the formulation of an nHA-encapsulating TRF (nHA/TRF) by employing the response surface methodology (RSM). <b>Results</b>: RSM outcomes reveal that the mass of the nHA, the concentration of the TRF, and the incubation time have a significant effect on the particle size, zeta potential, and encapsulation efficiency of the nHA/TRF. The outcomes for the optimized formulation are not significantly different from the predicted RSM outcomes. The optimized nHA/TRF formulation is freeze-dried and results in an average particle size of ~270 nm, a negative zeta potential value of ~−20 mV, a polydispersity index of <0.4, and an encapsulation efficiency of ~18.1%. Transmission electron microscopy (TEM) shows that the freeze-dried nHA/TRF has a spherical structure. <b>Conclusions</b>: Taken together, the above findings indicate that the nHA may be established as a nanocarrier for efficient delivery of the TRF, as demonstrated by the promising physical properties.https://www.mdpi.com/1999-4923/17/1/10response surface methodologycentral composite designnano-hydroxyapatitetocotrienol-rich fractionnanoformulationnanocarrier
spellingShingle Anis Syauqina Mohd Zaffarin
Shiow-Fern Ng
Min Hwei Ng
Haniza Hassan
Ekram Alias
Development and Optimization of Nano-Hydroxyapatite Encapsulating Tocotrienol-Rich Fraction Formulation Using Response Surface Methodology
Pharmaceutics
response surface methodology
central composite design
nano-hydroxyapatite
tocotrienol-rich fraction
nanoformulation
nanocarrier
title Development and Optimization of Nano-Hydroxyapatite Encapsulating Tocotrienol-Rich Fraction Formulation Using Response Surface Methodology
title_full Development and Optimization of Nano-Hydroxyapatite Encapsulating Tocotrienol-Rich Fraction Formulation Using Response Surface Methodology
title_fullStr Development and Optimization of Nano-Hydroxyapatite Encapsulating Tocotrienol-Rich Fraction Formulation Using Response Surface Methodology
title_full_unstemmed Development and Optimization of Nano-Hydroxyapatite Encapsulating Tocotrienol-Rich Fraction Formulation Using Response Surface Methodology
title_short Development and Optimization of Nano-Hydroxyapatite Encapsulating Tocotrienol-Rich Fraction Formulation Using Response Surface Methodology
title_sort development and optimization of nano hydroxyapatite encapsulating tocotrienol rich fraction formulation using response surface methodology
topic response surface methodology
central composite design
nano-hydroxyapatite
tocotrienol-rich fraction
nanoformulation
nanocarrier
url https://www.mdpi.com/1999-4923/17/1/10
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