Salmon Calcitonin-Loaded PLGA Microspheres as a Sustained-Release Vehicle

The present study aimed to develop inhalable poly (lactic-co-glycolic acid) (PLGA)-based microparticles of salmon calcitonin (sCT) for sustained pharmacological action by the fine droplet drying (FDD) process, a novel powderization technique employing printing technologies. PLGA was selected as a biodegradable carrier polymer for sustained-release particles of sCT (sCT/SR), and physicochemical characterizations of sCT/SR were conducted. To estimate the in vivo efficacy of the sCT/SR respirable powder (sCT/SR-RP), plasma calcium levels were measured after intratracheal administration in rats. The particle size of sCT/SR was 3.6 µm, and the SPAN factor, one of the parameters to present the uniformity of particle size distribution, was calculated to be 0.65. In the evaluation of the conformational structure of sCT, no significant changes were observed in sCT/SR even after the FDD process. The drug release from sCT/SR showed a biphasic pattern with an initial burst and slow diffusion in simulated lung fluid. sCT/SR-RP showed fine inhalation performance, as evidenced by a fine particle fraction value of 28% in the cascade impactor analysis. After the insufflation of sCT samples (40 µg-sCT/kg) in rats, sCT/SR-RP could enhance and prolong the hypocalcemic action of sCT possibly due to the sustained release and pulmonary absorption of sCT. From these observations, the strategic application of the FDD process could be efficacious to provide PLGA-based inhalable formulations of sCT, as well as other therapeutic peptides, to enhance their biopharmaceutical potentials.

Download Full-text

Development of a polysaccharide based multi-unit nanofiber mat for colon-targeted sustained release of salmon calcitonin

Journal of Colloid and Interface Science ◽

10.1016/j.jcis.2019.05.037 ◽

2019 ◽

Vol 552 ◽

pp. 186-195 ◽

Cited By ~ 8

Author(s):

Kun Feng ◽

Chen Li ◽

Yun-Shan Wei ◽

Min-Hua Zong ◽

Hong Wu ◽

...

Keyword(s):

Sustained Release ◽

Salmon Calcitonin

Download Full-text

Pulmonary pharmacokinetics of levofloxacin in rats after aerosolization of immediate-release chitosan or sustained-release PLGA microspheres

European Journal of Pharmaceutical Sciences ◽

10.1016/j.ejps.2016.08.024 ◽

2016 ◽

Vol 93 ◽

pp. 184-191 ◽

Cited By ~ 17

Author(s):

Marisa C. Gaspar ◽

Nicolas Grégoire ◽

João J.S. Sousa ◽

Alberto A.C.C. Pais ◽

Isabelle Lamarche ◽

...

Keyword(s):

Sustained Release ◽

Immediate Release ◽

Plga Microspheres

Download Full-text

Development of Risperidone PLGA Microspheres

Journal of Drug Delivery ◽

10.1155/2014/620464 ◽

2014 ◽

Vol 2014 ◽

pp. 1-11 ◽

Cited By ~ 21

Author(s):

Susan D’Souza ◽

Jabar A. Faraj ◽

Stefano Giovagnoli ◽

Patrick P. DeLuca

Keyword(s):

Steady State ◽

Sustained Release ◽

Sustained Delivery ◽

Plga Microspheres ◽

Sprague Dawley ◽

Multiple Dosing ◽

Duration Of Action ◽

Sprague Dawley Rats

The aim of this study was to design and evaluate biodegradable PLGA microspheres for sustained delivery of Risperidone, with an eventual goal of avoiding combination therapy for the treatment of schizophrenia. Two PLGA copolymers (50 : 50 and 75 : 25) were used to prepare four microsphere formulations of Risperidone. The microspheres were characterized by several in vitro techniques. In vivo studies in male Sprague-Dawley rats at 20 and 40 mg/kg doses revealed that all formulations exhibited an initial burst followed by sustained release of the active moiety. Additionally, formulations prepared with 50 : 50 PLGA had a shorter duration of action and lower cumulative AUC levels than the 75 : 25 PLGA microspheres. A simulation of multiple dosing at weekly or 15-day regimen revealed pulsatile behavior for all formulations with steady state being achieved by the second dose. Overall, the clinical use of Formulations A, B, C, or D will eliminate the need for combination oral therapy and reduce time to achieve steady state, with a smaller washout period upon cessation of therapy. Results of this study prove the suitability of using PLGA copolymers of varying composition and molecular weight to develop sustained release formulations that can tailor in vivo behavior and enhance pharmacological effectiveness of the drug.

Download Full-text

In vivo assessment of salmon calcitonin sustained release from biodegradable microspheres

Journal of Controlled Release ◽

10.1016/0168-3659(91)90059-m ◽

1991 ◽

Vol 17 (2) ◽

pp. 199-205 ◽

Cited By ~ 36

Author(s):

K.C. Lee ◽

E.E. Soltis ◽

P.S. Newman ◽

K.W. Burton ◽

R.C. Mehta ◽

...

Keyword(s):

Sustained Release ◽

Salmon Calcitonin ◽

Biodegradable Microspheres ◽

In Vivo Assessment

Download Full-text

Sustained release of OIC-A006 from PLGA microspheres to induce osteogenesis of composite PLGA/β-TCP scaffolds

Science and Engineering of Composite Materials ◽

10.1515/secm-2015-0372 ◽

2017 ◽

Vol 24 (5) ◽

pp. 721-730 ◽

Cited By ~ 1

Author(s):

Liulan Lin ◽

Yangyang Dong ◽

Qi Zhou

Keyword(s):

Drug Delivery ◽

Sustained Release ◽

High Performance ◽

Freeze Drying ◽

Glycolic Acid ◽

Strength Degradation ◽

Plga Microspheres ◽

Bone Induction ◽

Direct Loading ◽

Cell Adhesion And Proliferation

AbstractIn this article, poly(lactic-co-glycolic acid) (PLGA) microspheres containing the drug OIC-A006 were prepared by ice bath extraction and poly(lactic-co-glycolic acid)/ β-tricalcium phosphate (PLGA/β-TCP) scaffolds were prepared by freeze-drying. Three kinds of scaffold were prepared by adding no drug, direct loading the drug, and loading with drug microspheres. The mechanical strength, degradation, and microstructure of the scaffolds were analyzed. The drug delivery properties of the scaffolds were determined using high-performance liquid chromatography (HPLC). It was found that PLGA/β-TCP scaffolds with PLGA microspheres that contained the drug OIC-A006 exhibited a biphasic drug release pattern. Sustained release of the drug OIC-A006 was beneficial to cell adhesion and proliferation. Experiments on rats showed that composite PLGA/β-TCP scaffolds with PLGA microspheres containing the drug OIC-A006 produced good bone formation and bone induction.

Download Full-text