Preparation and characterization of Alendronate depot microspheres based on novel poly(-ε-caprolactone)/Vitamin E TPGS copolymers

Koulouktsi, Christina; Nanaki, Stavroula; Barmpalexis, Panagiotis; Kostoglou, Margaritis; Bikiaris, Dimitrios N.

doi:10.1016/j.ijpx.2019.100014

Cited by 15 publications

(14 citation statements)

References 52 publications

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“…PCL spectrum showed characteristic bands that are in accordance with the literature 34–38 . ALD spectrum provided the following characteristic bands: hydroxyl group bending vibration around 916 cm −1 , amino group stretching vibration around 3478 cm −1 and P = O stretching vibration around 1016 and 1042 cm −1 , which is in agreement with the bands reported in the literature 39–42 …”

Section: Resultssupporting

confidence: 89%

Polycaprolactone/alendronate systems intended for production of biomaterials

Silva

Pereira

Patricio

et al. 2021

J of Applied Polymer Sci

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Sodium alendronate (ALD) is a bisphosphonate used to treat osteoporosis. However, its oral administration has been associated with side effects as gastroesophageal reflux. Moreover, there are some particularities for the intake of the medicine, which also hinder the patient's compliance, for example, the instruction that it has to be taken with an empty stomach, 30 to 60 min before breakfast and avoid the decubitus position after using the drug. Therefore, biomaterials for applications in osteoporotic bones are a good alternative. Thus, this work aimed to produce a Polycaprolactone (PCL) and ALD‐based powder as a supply to build biomaterials by selective laser sintering, compression molding (CM), solvent casting (SC), among others. The powder was produced by coating the ALD particles with PCL and films were produced by SC and CM techniques. The samples were characterized by Scanning Electron Microscopy, Energy‐dispersive X‐ray spectroscopy, X‐ray diffraction, Fourier transform infrared spectrometry and thermal analysis. Furthermore, the drug release was evaluated by UV–Vis spectroscopy. Results showed that ALD particles were successfully coated by PCL and applied to the production of biomaterials, highlighting its potential in the treatment of osteoporosis.

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Section: Resultssupporting

confidence: 89%

Polycaprolactone/alendronate systems intended for production of biomaterials

Silva

Pereira

Patricio

et al. 2021

J of Applied Polymer Sci

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“…Moreover, Shin et al also reported similar shifts in the abovementioned bands when the FTIR spectrum of methoxy PEG was compared to the spectra of methoxy PEO 5000 - b -PCL with different molecular weights of PCL (Mn ~ 4000–17,000 Da) [ 38 ]. These observations verify the presence of intermolecular interactions occurring during the polymer synthesis [ 36 , 39 ].…”

Section: Resultssupporting

confidence: 82%

Design and Development of D‒α‒Tocopheryl Polyethylene Glycol Succinate‒block‒Poly(ε-Caprolactone) (TPGS−b−PCL) Nanocarriers for Solubilization and Controlled Release of Paclitaxel

et al. 2021

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The objective of this study was to synthesize and characterize a set of biodegradable block copolymers based on TPGS-block-poly(ε-caprolactone) (TPGS-b-PCL) and to assess their self-assembled structures as a nanodelivery system for paclitaxel (PAX). The conjugation of PCL to TPGS was hypothesized to increase the stability and the drug solubilization characteristics of TPGS micelles. TPGS-b-PCL copolymer with various PCL/TPGS ratios were synthesized via ring opening bulk polymerization of ε-caprolactone using TPGS, with different molecular weights of PEG (1–5 kDa), as initiators and stannous octoate as a catalyst. The synthesized copolymers were characterized using 1H NMR, GPC, FTIR, XRD, and DSC. Assembly of block copolymers was achieved via the cosolvent evaporation method. The self-assembled structures were characterized for their size, polydispersity, and CMC using dynamic light scattering (DLS) technique. The results from the spectroscopic and thermal analyses confirmed the successful synthesis of the copolymers. Only copolymers that consisted of TPGS with PEG molecular weights ≥ 2000 Da were able to self-assemble and form nanocarriers of ≤200 nm in diameter. Moreover, TPGS2000-b-PCL4000, TPGS3500-b-PCL7000, and TPGS5000-b-PCL15000 micelles enhanced the aqueous solubility of PAX from 0.3 µg/mL up to 88.4 ug/mL in TPGS5000-b-PCL15000. Of the abovementioned micellar formulations, TPGS5000-b-PCL15000 showed the slowest in vitro release of PAX. Specifically, the PAX-loaded TPGS5000-b-PCL15000 micellar formulation showed less than 10% drug release within the first 12 h, and around 36% cumulative drug release within 72 h compared to 61% and 100% PAX release, respectively, from the commercially available formulation (Ebetaxel®) at the same time points. Our results point to a great potential for TPGS-b-PCL micelles to efficiently solubilize and control the release of PAX.

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“…As depicted in the thermograms ( Figure 6 ), ATRA showed a slight endothermic peak at about 146 °C and a relevant peak associated to melting at about 183 °C [ 49 ]. TPGS alone gave an endothermic sharp peak of melting at around 43 °C and a broad peak at 32 °C, due to the minor presence of an amorphous solid [ 50 ]. The DSC thermograms of ATRA-loaded micelles showed only the melting peak of TPGS.…”

Section: Resultsmentioning

confidence: 99%

D-α-Tocopherol-Based Micelles for Successful Encapsulation of Retinoic Acid

et al. 2021

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All-trans-retinoic acid (ATRA) represents the first-choice treatment for several skin diseases, including epithelial skin cancer and acne. However, ATRA’s cutaneous side effects, like redness and peeling, and its high instability limit its efficacy. To address these drawbacks and to improve ATRA solubilization, we prepared ATRA-loaded micelles (ATRA-TPGSs), by its encapsulation in D-α-tocopheryl-polyethylene-glycol-succinate (TPGS). First, to explore the feasibility of the project, a solubility study based on the equilibrium method was performed; then, six ATRA-TPGS formulations were prepared by the solvent-casting method using different TPGS amounts. ATRA-TPGSs showed small sizes (11–20 nm), low polydispersity, slightly negative zeta potential, and proved good encapsulation efficiency, confirmed by a chemometric-assisted Fourier transform infrared spectroscopy (FTIR) investigation. ATRA-TPGS stability was also investigated to choose the most stable formulation. Using Carbopol® 980 as gelling agent, ATRA-TPGS-loaded gels were obtained and analyzed for their rheological profiles. Ex vivo release studies from ATRA-TPGSs were performed by Franz cells, demonstrating a permeation after 24 h of 22 ± 4 µ cm−2. ATRA-TPGSs showed enhanced cytotoxic effects on melanoma cells, suggesting that these formulations may represent a valid alternative to improve patient compliance and to achieve more efficacious therapeutic outcomes.

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Preparation and characterization of Alendronate depot microspheres based on novel poly(-ε-caprolactone)/Vitamin E TPGS copolymers

Abstract: Graphical abstract

Cited by 15 publications

References 52 publications

Polycaprolactone/alendronate systems intended for production of biomaterials

Polycaprolactone/alendronate systems intended for production of biomaterials

Design and Development of D‒α‒Tocopheryl Polyethylene Glycol Succinate‒block‒Poly(ε-Caprolactone) (TPGS−b−PCL) Nanocarriers for Solubilization and Controlled Release of Paclitaxel

D-α-Tocopherol-Based Micelles for Successful Encapsulation of Retinoic Acid

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