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Updated: Jun 28, 2026

Fabricating Highly Open Porous Microspheres (HOPMs) via Microfluidic Technology
Published on: May 16, 2022
Design of methylprednisolone biodegradable microspheres intended for intra-articular administration
Francesco Cilurzo1, Francesca Selmin, Paola Minghetti
1Istituto di Chimica Farmaceutica e Tossicologica "P. Pratesi", Università degli Studi di Milano, Via Mangiagalli 14, 20133 Milan, Italy. francesco.cilurzo@unimi.it
Abstract:
This study aimed to design methyprednisolone (MP)-loaded poly(D,L lactide-co-glycolide) (PLGA) microspheres (MS) intended for intra-articular administration. MP was encapsulated in four different types of PLGA by using an S/O/W technique. The effects of beta-irradiation at the dose of 25 kGy were evaluated on the chemical and physicochemical properties of MS and the drug release profiles. The S/O/W technique with hydroxypropylmethylcellulose (HPMC) as surfactant allowed obtaining MS in the tolerability size (7-50 microm) for intra-articular administration. The MP encapsulation efficiency ranged 56-60%. HPMC traces were evidenced in the loaded and placebo MS by attenuated total reflectance Fourier transform infrared spectroscopy. MS made of the capped PLGA DL5050 2M (MS 2M) and uncapped PLGA DL5050 3A (MS 3A) prolonged the release of MP over a 2- to 3-month period with a triphasic (burst release-dormant period-second release pulse) and biphasic release pattern, respectively. The beta-irradiation did not significantly alter the morphology, chemical, and physicochemical properties of MS. The only variation was evidenced in the drug release for MS 2M in term of shorting of the dormant period. The minimal variations in the properties of irradiated PLGA MS, which are in disagreement with literature data, may be attributed to a radioprotecting effect exerted by HPMC.
Insights
This study developed methyprednisolone (MP)-loaded poly(D,L lactide-co-glycolide) (PLGA) microspheres for joint injections. Beta-irradiation minimally affected microsphere properties, with HPMC potentially offering radioprotection.
Area of Science:
- Biomaterials Science
- Drug Delivery Systems
- Polymer Chemistry
Background:
- Intra-articular administration requires specialized drug delivery systems.
- Poly(D,L lactide-co-glycolide) (PLGA) microspheres are suitable for sustained drug release.
- Methyprednisolone (MP) is a corticosteroid used for inflammatory conditions.
Purpose of the Study:
- To design and characterize methyprednisolone (MP)-loaded poly(D,L lactide-co-glycolide) (PLGA) microspheres for intra-articular administration.
- To evaluate the impact of beta-irradiation on the properties and drug release of these microspheres.
Main Methods:
- Microspheres were prepared using the oil-in-water (O/W) emulsion technique with hydroxypropylmethylcellulose (HPMC) as a surfactant.
- Four types of PLGA with varying properties were used for encapsulation.
- Beta-irradiation (25 kGy) was applied to assess its effects on microsphere characteristics and drug release profiles.
- Attenuated total reflectance Fourier transform infrared spectroscopy (ATR-FTIR) was used to confirm HPMC presence.
Main Results:
- The O/W technique with HPMC yielded microspheres of appropriate size (7-50 microm) for intra-articular injection.
- Encapsulation efficiency for MP ranged from 56-60%.
- Microspheres made from capped (MS 2M) and uncapped (MS 3A) PLGA demonstrated prolonged MP release over 2-3 months, exhibiting triphasic and biphasic patterns, respectively.
- Beta-irradiation showed minimal impact on microsphere morphology and physicochemical properties, with a slight reduction in the dormant release period for MS 2M.
Conclusions:
- PLGA microspheres loaded with methyprednisolone are feasible for intra-articular delivery, providing sustained release over several months.
- Beta-irradiation at 25 kGy does not significantly alter the critical properties of these PLGA microspheres.
- The presence of HPMC may confer a radioprotective effect on the PLGA microspheres, explaining the minimal changes observed post-irradiation, which contrasts with existing literature.
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