Biocompatibility of poly(d,l-lactide-co-glycolide) nanoparticles conjugated with alendronate

Cenni, E.; Granchi, Donatella; Avnet, Sofia; Fotia, Caterina; Salerno, Manuela; Micieli, Dorotea; Sarpietro, Maria Grazia; Pignatello, Rosario; Castelli, Francesco; Baldini, Nicola

doi:10.1016/j.biomaterials.2007.12.022

Cited by 120 publications

(109 citation statements)

References 42 publications

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“…Disadvantages of BPs and their advances as novel drug delivery systems. DOI: 10.3109/10717544.2013.870259 PLGA-ALD NPs are suitable for the intravenous administration, and the drug-loading could make them a promising tool for delivering the BPs for treating OP (Cenni et al, 2008;Pignatello et al, 2009). Thus the developed nanoparticulate drug delivery did not show any bleeding from esophagus and no hemolysis was recorded.…”

Section: Polymeric Nanoparticlesmentioning

confidence: 99%

Bisphosphonates: therapeutics potential and recent advances in drug delivery

et al. 2014

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Context: Bisphosphonates (BPs) are widely used for prevention and treatment of osteoporosis. BPs are known as gold standard for osteoporosis (OP) treatment due to their positive results in clinical studies. But some serious side effects are associated with BPs like gastrointestinal adverse effect i.e. esophagitis and ulcer of esophagus. Oral bioavailability (BA) of BPs ranges from 0.6 to 1% due to poor absorption through gastrointestinal tract (GIT). Objective: The main objective of this review is to explore the role of novel drug delivery systems (DDSs) for the delivering of BPs and minimizing the drawbacks associated with them. Methods: The current review is focusing on classification, mechanism of action, and limitations of BPs, and is also dwelling on the use of novel DDSs like nanoparticles, liposomes, topical, transdermal systems, implants, bisphosphonate osteotropic DDS (BP-ODDS), microspheres, and calcium phosphate cements (CPCs) for BPs. This review also gives a critically reviewed compilation of the various in vitro and in vivo studies conducted till date. Conclusion: On the basis of the exhaustive literature, it has been found that the novel DDS minimizes the side effects associated with BPs and enhances the BA. The advance drug delivery has a greater impact on reducing the undesirable effects and increasing the BA of BPs.

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Section: Polymeric Nanoparticlesmentioning

confidence: 99%

Bisphosphonates: therapeutics potential and recent advances in drug delivery

et al. 2014

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“…NP were produced by the PLGA-ALE conjugate by a nanoprecipitation method, using an opportunely adapted emulsion/solvent evaporation technique [33]. The conjugate was dissolved in acetone, DMSO or their 1:1 mixture (v:v).…”

Section: Plga-ale Nanoparticlesmentioning

confidence: 99%

PLGA-Alendronate Conjugate as a New Biomaterial to Produce Osteotropic Drug Nanocarriers

Pignatello¹

2011

Biomaterials Applications for Nanomedicine

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“…This approach ensures the release of the drug to the site of the disease [1]. Moreover, it allows delivery of drugs that have low bioavailability when administrated by conventional routes.…”

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confidence: 99%

“…The microparticles obtained following this method remain to be furthermore characterized in order to evaluate the size distribution, entrapment efficiency, morphology and drug release profile. Also, by altering the manufacturing conditions, copolymer ratio and degradation rate, the microparticles drug loading can be adjusted [1].In a second step, the optimized alendronate loaded microparticles are to be used to develop an implant with high affinity for bone tissue. In conclusion, this system could improve the local delivery of alendronate and have a high potential in bone repair applications.…”

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confidence: 99%

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Development of an Alendronate Controlled Delivery System for Bone Repair Applications

Deca¹,

Belu²,

Croitoru³

et al. 2016

Proceedings of the World Congress on Recent Advances in Nanotechnology

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A great interest has been shown towards designing bone targeted medical delivery systems for the treatment of several bone disorders. This approach ensures the release of the drug to the site of the disease [1]. Moreover, it allows delivery of drugs that have low bioavailability when administrated by conventional routes. This leads to enhanced patient adherence and an improved clinical outcome of bone related diseases [2].Given that hydroxyapatite is a major component of the bone matrix, it represents a target for specific delivery systems [3]. Due to their structure which consists in two phosphonates groups linked to a carbon atom, bisphosphonates show a high affinity for hydroxyapatite. Furthermore they increase both osteoblast proliferation and osteoclast apoptosis leading to bone remodeling [4]. Alendronate is a bisphosphonate used in the treatment and prevention of osteoporosis, Paget's disease, primary hyperparathyroidism, bone metastasis, multiple myeloma [5].Microparticle-mediated drug delivery to the bone is a promising approach which ensures a high local alendronate concentration and a controlled release of the drug [4,6]. A recent study conducted by Stadelmann et al. [7] shows an increase in bone density when zoledronate was locally delivered.Poly lactic-co-glycolic acid (PLGA) is a copolymer approved to be safe in pharmaceutical applications by the FDA due to its biocompatibility and biodegradability. A number of PLGA compounds with different copolymer ratio are used to design microparticles with various properties [8].The aim of the study is to develop and optimize a PLGA-alendronate microparticles based delivery device, designed to target the bone tissue. This carrier system has the advantages of a high biocompatibility and a controlled release of the incorporated drug. Furthermore, it has the benefit of being a biodegradable system [8,9].In a first step, the microencapsulation process is to be optimized. There are a number of techniques for PLGA microparticles preparation such as supercritical fluid extraction, extrusion and spray drying [6]. However, the method optimized for this study is the solvent evaporation method. Using this method the microparticles are prepared via a water/oil/water (w/o/w) double emulsion. Initially we prepared two solutions: the alendronate aqueous solution and the PLGA organic solution. The solutions were used to form the primary emulsion which was poured into a polyvinyl alcohol aqueous solution resulting into the w/o/w double emulsion. In order to evaporate the solvent and form the microparticles, the double emulsion was stirred at room temperature for 4 hours. The microparticles obtained following this method remain to be furthermore characterized in order to evaluate the size distribution, entrapment efficiency, morphology and drug release profile. Also, by altering the manufacturing conditions, copolymer ratio and degradation rate, the microparticles drug loading can be adjusted [1].In a second step, the optimized alendronate loaded microparticles are to be used t...

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Biocompatibility of poly(d,l-lactide-co-glycolide) nanoparticles conjugated with alendronate

Cited by 120 publications

References 42 publications

Bisphosphonates: therapeutics potential and recent advances in drug delivery

Bisphosphonates: therapeutics potential and recent advances in drug delivery

PLGA-Alendronate Conjugate as a New Biomaterial to Produce Osteotropic Drug Nanocarriers

Development of an Alendronate Controlled Delivery System for Bone Repair Applications

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