Hydrophilic polymeric nanoparticles prepared from Delonix galactomannan with low cytotoxicity for ocular drug delivery

Ogunjimi, Abayomi Tolulope; Melo, Shaiani Maria Gil de; Vargas-Rechia, Carem Gledes; Emery, Flávio da Silva; Lopez, Renata Fonseca Vianna

doi:10.1016/j.carbpol.2016.10.076

Cited by 42 publications

(15 citation statements)

References 47 publications

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“…In vitro NTX skin flux from Formulations F7, F19, and F27 containing 12-mg/mL NTX applied to MN-treated porcine ear skin were 3.89 ± 0.96, 4.24 ± 1.57, and 3.28 ± 0.98 µg/cm 2 ·h, respectively. There was no significant difference in NTX flux between these three formulations when applied to MN-treated skin, despite that in vitro NTX release from microspheres containing 2-mg/mL NTX showed that increased chitosan MW led to a decreased cumulative NTX release over 24 h. This result may be explained by the properties of the hydrophilic natural polymers such as chitosan, which swell rapidly in aqueous mediums, forming a gel-like structure that can control and slow down drug release [ 14 ]. The higher amount of chitosan (12 mg/mL) in the formulations used in this skin permeation study vs. that of in vitro release studies (2 mg/mL) may have canceled out the effect that chitosan MW had on the NTX flux.…”

Section: Resultsmentioning

confidence: 99%

“…This technique has been used to entrap drugs into polymers, which are used to deliver high drug concentrations, protect the drug from degradation, and provide sustained drug release [ 13 ]. Biodegradable polymers, particularly natural polymers such as chitosan, have attracted more interest due to their affordability, biocompatibility, low irritation, little or no toxicity, and widespread availability [ 14 ]. Chitosan is a natural cationic linear polysaccharide that has been used extensively for drug delivery because of the aforementioned properties and, also, because of its mucoadhesive nature and ability for controlled drug release [ 15 , 16 , 17 ].…”

Section: Introductionmentioning

confidence: 99%

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Design and Characterization of Spray-Dried Chitosan-Naltrexone Microspheres for Microneedle-Assisted Transdermal Delivery

2020

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Naltrexone (NTX) hydrochloride is a potent opioid antagonist with significant first-pass metabolism and notable untoward effects when administered orally or intramuscularly. Microneedle (MN)-assisted transdermal delivery is an attractive alternative that can improve therapeutic delivery to deeper skin layers. In this study, chitosan-NTX microspheres were developed via spray-drying, and their potential for transdermal NTX delivery in association with MN skin treatment was assessed. A quality-by-design approach was used to evaluate the impact of key input variables (chitosan molecular weight, concentration, chitosan-NTX ratio, and feed flow rate) on microsphere physical characteristics, encapsulation efficiency, and drug-loading capacity. Formulated microspheres had high encapsulation efficiencies (70–87%), with drug-loading capacities ranging from 10–43%. NTX flux through MN-treated skin was 11.6 ± 2.2 µg/cm2·h from chitosan-NTX microspheres, which was significantly higher than flux across intact skin. Combining MN-assisted delivery with the chitosan microsphere formulation enabled NTX delivery across the skin barrier, while controlling the dose released to the skin.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Design and Characterization of Spray-Dried Chitosan-Naltrexone Microspheres for Microneedle-Assisted Transdermal Delivery

2020

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“…The determination of cell viability is a significant assay to evaluate the cytotoxicity of biomaterials and nanosystems [ 68 ]. The MTT assay is a rapid quantitative procedure based on the transformation of a yellow tetrazolium salt to insoluble purple formazan crystals in the mitochondria of viable cells [ 69 ]. Figure 4 A,B shows the bar chart breakdown of the biocompatibility assay of StBAclm and VCM-StBAclm-Qt 1 quatsomes on four different cell lines (A-549, HEK-293, Hep-G2, and MCF-7 cells).…”

Section: Resultsmentioning

confidence: 99%

Formulation of pH-Responsive Quatsomes from Quaternary Bicephalic Surfactants and Cholesterol for Enhanced Delivery of Vancomycin against Methicillin Resistant Staphylococcus aureus

et al. 2020

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Globally, human beings continue to be at high risk of infectious diseases caused by methicillin-resistant Staphylococcus aureus (MRSA); and current treatments are being depleted due to antimicrobial resistance. Therefore, the synthesis and formulation of novel materials is essential for combating antimicrobial resistance. The study aimed to synthesize a quaternary bicephalic surfactant (StBAclm) and thereof to formulate pH-responsive vancomycin (VCM)-loaded quatsomes to enhance the activity of the antibiotic against MRSA. The surfactant structure was confirmed using 1H, 13C nuclear magnetic resonance (NMR), Fourier-transform infrared spectroscopy (FT-IR), and high-resolution mass spectrometry (HRMS). The quatsomes were prepared using a sonication/dispersion method and were characterized using various in vitro, in vivo, and in silico techniques. The in vitro cell biocompatibility studies of the surfactant and pH-responsive vancomycin-loaded quatsomes (VCM-StBAclm-Qt1) revealed that they are biosafe. The prepared quatsomes had a mean hydrodynamic diameter (MHD), polydispersity index (PDI), and drug encapsulation efficiency (DEE) of 122.9 ± 3.78 nm, 0.169 ± 0.02 mV, and 52.22 ± 8.4%, respectively, with surface charge switching from negative to positive at pH 7.4 and pH 6.0, respectively. High-resolution transmission electron microscopy (HR-TEM) characterization of the quatsomes showed spherical vesicles with MHD similar to the one obtained from the zeta-sizer. The in vitro drug release of VCM from the quatsomes was faster at pH 6.0 compared to pH 7.4. The minimum inhibitory concentration (MIC) of the drug loaded quatsomes against MRSA was 32-fold and 8-fold lower at pH 6.0 and pH 7.4, respectively, compared to bare VCM, demonstrating the pH-responsiveness of the quatsomes and the enhanced activity of VCM at acidic pH. The drug-loaded quatsomes demonstrated higher electrical conductivity and a decrease in protein and deoxyribonucleic acid (DNA) concentrations as compared to the bare drug. This confirmed greater MRSA membrane damage, compared to treatment with bare VCM. The flow cytometry study showed that the drug-loaded quatsomes had a similar bactericidal killing effect on MRSA despite a lower (8-fold) VCM concentration when compared to the bare VCM. Fluorescence microscopy revealed the ability of the drug-loaded quatsomes to eradicate MRSA biofilms. The in vivo studies in a skin infection mice model showed that groups treated with VCM-loaded quatsomes had a 13-fold decrease in MRSA CFUs when compared to the bare VCM treated groups. This study confirmed the potential of pH-responsive VCM-StBAclm quatsomes as an effective delivery system for targeted delivery and for enhancing the activity of antibiotics.

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“…Other polysaccharides such as pectin, gum cordia, carboxymethyl tamarind kernel polysaccharide, galactomannan polysaccharide, and hyaluronic acid have also been used to make nanoparticles for ocular drug delivery [104–107, 128]. In an ex vivo study, pectin nanoparticles were found to significantly increase the permeability of timolol maleate across the excised goat cornea 200% more than the conventional timolol maleate ophthalmic solution [104].…”

Section: Nanoparticles For Drug Delivery To the Anterior Segmentmentioning

confidence: 99%

Nanoparticles for drug delivery to the anterior segment of the eye

Janagam

Lowe

2017

Advanced Drug Delivery Reviews

252

153

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Commercially available ocular drug delivery systems are effective but less efficacious to manage diseases/disorders of the anterior segment of the eye. Recent advances in nanotechnology and molecular biology offer a great opportunity for efficacious ocular drug delivery for the treatments of anterior segment diseases/disorders. Nanoparticles have been designed for preparing eye drops or injectable solutions to surmount ocular obstacles faced after administration. Better drug pharmacokinetics, pharmacodynamics, non-specific toxicity, immunogenicity, and biorecognition can be achieved to improve drug efficacy when drugs are loaded in the nanoparticles. Despite the fact that a number of review articles have been published at various points in the past regarding nanoparticles for drug delivery, there is not a review yet focusing on the development of nanoparticles for ocular drug delivery to the anterior segment of the eye. This review fills in the gap and summarizes the development of nanoparticles as drug carriers for improving the penetration and bioavailability of drugs to the anterior segment of the eye.

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Hydrophilic polymeric nanoparticles prepared from Delonix galactomannan with low cytotoxicity for ocular drug delivery

Cited by 42 publications

References 47 publications

Design and Characterization of Spray-Dried Chitosan-Naltrexone Microspheres for Microneedle-Assisted Transdermal Delivery

Design and Characterization of Spray-Dried Chitosan-Naltrexone Microspheres for Microneedle-Assisted Transdermal Delivery

Formulation of pH-Responsive Quatsomes from Quaternary Bicephalic Surfactants and Cholesterol for Enhanced Delivery of Vancomycin against Methicillin Resistant Staphylococcus aureus

Nanoparticles for drug delivery to the anterior segment of the eye

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