Application of Implantable Polylactic-Co-Glycolic Acid Microcapsule in Repairing Alveolar Bone Defects

Alveolar bone defects (ABDs) were a perennial problem, especially in the aged. Bisphosphonates, especially etidronate sodium (ET), were frequently used in clinical treatment of ABD. However, the oral administration of ET had poor absorption (<1%). Therefore, optimization of a suitable dosage form substituted with ET to locally repair the ABD was a straightforward approach. Polylactide-co-glycolide (PLGA) is a biodegradable material and had been used in locally implanted medical devices. Therefore, an ET-PLGA microcapsule may help local delivery and prolong the activity of healing ABD. In this paper, a preparation method of ET-PLGA microcapsule was optimized by the single-factor investigation and response surface method. Subsequently, the rat ABD model was used to evaluate the enhancement effect of these microcapsules. Finally, the optimum parameters were determined as follows: 40% dichloromethane, 160 mg/mL PLGA, 10% internal aqua/oil phase, 4% PVA, and emulsifying for 10 min. These microcapsules were spherical in shape and fairly monodisperse in a particle size of 27,51 μm (PDI = 0.3), encapsulation rate 96.6%, and drug loading 4.58%. Compared with the ET groups, the total healing volume of ABD in ET-PLGA groups was significantly increased P < 0.05 . ET-PLGA microcapsules significantly enhanced the effect of ET on ABD. This study provided important technical support for the treatment of ABD with bisphosphonates by local administration. This paper has an exploratory significance for the development of water-soluble bioactive components with low bioavailability for ABD.

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Mesoporous Silica Molecular Sieve based Nanocarriers: Transpiring Drug Dissolution Research

Current Pharmaceutical Design ◽

10.2174/1381612822666161026162005 ◽

2017 ◽

Vol 23 (3) ◽

pp. 467-480 ◽

Cited By ~ 8

Author(s):

Satyanarayan Pattnaik ◽

Kamla Pathak

Keyword(s):

Drug Release ◽

Mesoporous Silica ◽

Molecular Sieves ◽

Release Kinetics ◽

Drug Loading ◽

Scale Up ◽

Water Soluble ◽

Drug Dissolution ◽

Water Soluble Drugs ◽

Loading Methods

Background: Improvement of oral bioavailability through enhancement of dissolution for poorly soluble drugs has been a very promising approach. Recently, mesoporous silica based molecular sieves have demonstrated excellent properties to enhance the dissolution velocity of poorly water-soluble drugs. Description: Current research in this area is focused on investigating the factors influencing the drug release from these carriers, the kinetics of drug release and manufacturing approaches to scale-up production for commercial manufacture. Conclusion: This comprehensive review provides an overview of different methods adopted for synthesis of mesoporous materials, influence of processing factors on properties of these materials and drug loading methods. The drug release kinetics from mesoporous silica systems, the manufacturability and stability of these formulations are reviewed. Finally, the safety and biocompatibility issues related to these silica based materials are discussed.

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Formulation Development of Tamoxifen Loaded Lipid Nanoparticle by Taguchi (L12 (2 11)) Orthogonal Array Design

Current Computer - Aided Drug Design ◽

10.2174/1573409916666200320162948 ◽

2020 ◽

Vol 16 ◽

Author(s):

Poovi Ganesan ◽

N Damodharan

Keyword(s):

Orthogonal Array ◽

Drug Loading ◽

Optimization Technique ◽

Pharmaceutical Products ◽

Water Soluble ◽

Nanostructured Lipid Carrier ◽

Orthogonal Array Design ◽

Formulation Development ◽

Array Design ◽

Lipid Nanoparticle

Background: A better understanding of the biopharmaceutical and physicochemical properties of drugs and the pharmaco-technical factors would be of great help for developing pharmaceutical products. But, it is extremely difficult to study the effect of each variable and interaction among them through the conventional approach Objective: To screen the most influential factors affecting the particle size (PS) of lipid nanoparticle (LNPs) (solid lipid nanoparticle (SLN) and nanostructured lipid carrier (NLC)) for poorly water-soluble BCS class-II drug like tamoxifen (TMX) to improve its oral bioavailability and to reduce its toxicity to tolerable limits using Taguchi (L12 (2 11)) orthogonal array design by applying computer optimization technique. Results: The size of all LNPs formulations prepared as per the experimental design varied between 172 nm and 3880 μm, polydispersity index between 0.033 and 1.00, encapsulation efficiency between 70.8% and 75.7%, and drug loading between 5.84% and 9.68%. The study showed spherical and non-spherical as well as aggregated and non-aggregated LNPs. Besides, it showed no interaction and amorphous form of the drug in LNPs formulation. The Blank NLCs exhibited no cytotoxicity on MCF-7 cells as compared to TMX solution, SLNs (F5) and NLCs (F12) suggests that the cause of cell death is primarily from the effect of TMX present in NLCs. Conclusions: The screening study clearly showed the importance of different individual factors significant effect for the LNPs formulation development and its overall performance in an in-vitro study with minimum experimentation thus saving considerable time, efforts, and resources for further in-depth study.

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The Correlation between Physical Crosslinking and Water-Soluble Drug Release from Chitosan-Based Microparticles

Pharmaceutics ◽

10.3390/pharmaceutics12050455 ◽

2020 ◽

Vol 12 (5) ◽

pp. 455

Author(s):

Emilia Szymańska ◽

Katarzyna Woś-Latosi ◽

Julia Jacyna ◽

Magdalena Dąbrowska ◽

Joanna Potaś ◽

...

Keyword(s):

Drug Release ◽

Polymer Matrix ◽

Drug Loading ◽

Water Soluble ◽

Dissolution Behavior ◽

Complex Nature ◽

Prolonged Release ◽

Scanning Calorimetry ◽

Burst Effect ◽

The Impact

Microparticles containing water-soluble zidovudine were prepared by spray-drying using chitosan glutamate and beta-glycerophosphate as an ion crosslinker (CF). The Box–Behnken design was applied to optimize the microparticles in terms of their drug loading and release behavior. Physicochemical studies were undertaken to support the results from dissolution tests and to evaluate the impact of the crosslinking ratio on the microparticles’ characteristics. The zidovudine dissolution behavior had a complex nature which comprised two phases: an initial burst effect followed with a prolonged release stage. The initial drug release, which can be modulated by the crosslinking degree, was primarily governed by the dissolution of the drug crystals located on the microparticles’ surfaces. In turn, the further dissolution stage was related to the drug diffusion from the swollen polymer matrix and was found to correlate with the drug loading. Differential Scanning Calorimetry (DSC) studies revealed the partial incorporation of a non-crystallized drug within the polymer matrix, which correlated with the amount of CF. Although CF influenced the swelling capacity of chitosan glutamate microparticles, surprisingly a higher amount of CF did not impact the time required for 80% of the drug to be released markedly. The formulation with the lowest polymer:CF ratio, 3:1, was selected as optimal, providing satisfactory drug loading and displaying a moderate burst effect within the first 30 min of the study, followed with a prolonged drug release of up to 210 min.

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Study on the Antibacterial Performance of the Antibacterial Shutter Blades

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.815.333 ◽

2013 ◽

Vol 815 ◽

pp. 333-338

Author(s):

Ming Li Liu ◽

Chun Feng Li ◽

Yun Long Wang ◽

Kai Lu ◽

Jiu Yin Pang ◽

...

Keyword(s):

Antibacterial Agent ◽

Antibacterial Agents ◽

Drug Loading ◽

Antibacterial Properties ◽

Water Soluble ◽

Single Factor ◽

Antibacterial Performance ◽

Loading Amount ◽

Single Factor Experiment ◽

Impregnation Solution

This study used Ag-embedded nanoTiO2, xylan and water-soluble Chitosan as antibacterial agents, respectively prepared shutter blades through the treating solution of the different concentration and the different drug loading amount of the poplar veneer. Through a single factor experiment, this paper analyzes that the different antibacterial agent, concentration of antibacterial agent and the drug loading amount have an effect on the antibacterial properties of the shutter blades. The results show that the order of antibacterial performance of the shutter blades impregnated antibacterial agents is the Ag-embedded nanoTiO2, Chitosan, Xylan. Comprehensiv-ely thought the antibacterial properties and economic index, the optimal concentration of the Ag-embedded nanoTiO2 impregnation solution is 1%.

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Sterically Stabilized RIPL Peptide-Conjugated Nanostructured Lipid Carriers: Characterization, Cellular Uptake, Cytotoxicity, and Biodistribution

Pharmaceutics ◽

10.3390/pharmaceutics10040199 ◽

2018 ◽

Vol 10 (4) ◽

pp. 199 ◽

Cited By ~ 5

Author(s):

Chang Kim ◽

Si Sung ◽

Eun Lee ◽

Tae Kang ◽

Ho Yoon ◽

...

Keyword(s):

Drug Loading ◽

Mononuclear Phagocyte ◽

Nanostructured Lipid Carriers ◽

Water Soluble ◽

Zeta Potentials ◽

Grafting Ratio ◽

Macrophage Phagocytosis ◽

Water Soluble Drugs ◽

High Payload

As a platform for hepsin-specific drug delivery, we previously prepared IPLVVPLRRRRRRRRC peptide (RIPL)-conjugated nanostructured lipid carriers (RIPL-NLCs) composed of Labrafil® M 1944 CS (liquid oil) and Precirol® ATO 5 (solid lipid). In this study, to prevent the recognition by the mononuclear phagocyte system, polyethylene glycol (PEG)-modified RIPL-NLCs (PEG-RIPL-NLCs) were prepared using PEG3000 at different grafting ratios (1, 5, and 10 mole %). All prepared NLCs showed a homogeneous dispersion (130–280 nm), with zeta potentials varying from −18 to 10 mV. Docetaxel (DTX) was successfully encapsulated in NLCs: encapsulation efficiency (93–95%); drug-loading capacity (102–109 µg/mg). PEG-RIPL-NLCs with a grafting ratio of 5% PEG or higher showed significantly reduced protein adsorption and macrophage phagocytosis. The uptake of PEG(5%)-RIPL-NLCs by cancer cell lines was somewhat lower than that of RIPL-NLCs because of the PEG-induced steric hindrance; however, the uptake level of PEG-RIPL-NLCs was still greater than that of plain NLCs. In vivo biodistribution was evaluated after tail vein injection of NLCs to normal mice. Compared to RIPL-NLCs, PEG(5%)-RIPL-NLCs showed lower accumulation in the liver, spleen, and lung. In conclusion, we found that PEG(5%)-RIPL-NLCs could be a promising nanocarrier for selective drug targeting with a high payload of poorly water-soluble drugs.

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Organic Nanoplatforms for Iodinated Contrast Media in CT Imaging

Molecules ◽

10.3390/molecules26237063 ◽

2021 ◽

Vol 26 (23) ◽

pp. 7063

Author(s):

Peng Zhang ◽

Xinyu Ma ◽

Ruiwei Guo ◽

Zhanpeng Ye ◽

Han Fu ◽

...

Keyword(s):

Contrast Media ◽

New Technologies ◽

Drug Loading ◽

Three Dimensional ◽

Disease Diagnosis ◽

Ct Imaging ◽

Water Soluble ◽

Iodinated Contrast Media ◽

Iodinated Contrast ◽

Anatomical Images

X-ray computed tomography (CT) imaging can produce three-dimensional and high-resolution anatomical images without invasion, which is extremely useful for disease diagnosis in the clinic. However, its applications are still severely limited by the intrinsic drawbacks of contrast media (mainly iodinated water-soluble molecules), such as rapid clearance, serious toxicity, inefficient targetability and poor sensitivity. Due to their high biocompatibility, flexibility in preparation and modification and simplicity for drug loading, organic nanoparticles (NPs), including liposomes, nanoemulsions, micelles, polymersomes, dendrimers, polymer conjugates and polymeric particles, have demonstrated tremendous potential for use in the efficient delivery of iodinated contrast media (ICMs). Herein, we comprehensively summarized the strategies and applications of organic NPs, especially polymer-based NPs, for the delivery of ICMs in CT imaging. We mainly focused on the use of polymeric nanoplatforms to prolong circulation time, reduce toxicity and enhance the targetability of ICMs. The emergence of some new technologies, such as theragnostic NPs and multimodal imaging and their clinical translations, are also discussed.

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Current approach to bone augmentation with allogeneic cortical graft: A case report

International Dental Research ◽

10.5577/intdentres.2021.vol11.suppl1.44 ◽

2021 ◽

Vol 11 (Suppl. 1) ◽

pp. 299-302

Author(s):

Utku Nezih Yılmaz ◽

Fatma Eriş Derkuş

Keyword(s):

Case Report ◽

Dental Implant ◽

Soft Tissues ◽

Alveolar Bone ◽

Healing Process ◽

Bone Defects ◽

Current Approach ◽

Autogenous Bone ◽

Bone Augmentation ◽

Alveolar Crest

Aim: Today, dental implant applications have become the most preferred option in the treatment of tooth deficiencies. Long-term successful results in dental implant applications depend largely on the volume and quality of the hard and soft tissues in the relevant region. Insufficient soft tissues and alveolar crest resorption complicate implant applications. Grafts and additional surgical procedures are required to compensate for resorption and to provide bone augmentation. Shell technique, one of the augmentation methods used in the treatment of alveolar bone defects, is an important procedure for guided bone regeneration. The purpose of this case report is to describe the treatment of vertical and horizontal bone loss with the Shell technique using allogeneic cortical grafts. Methodology: A 58-year-old female patient without any systemic disease was admitted to our clinic with the complaint of tooth loss in the right posterior mandibular region. In the intraoral and radiological examinations, it was determined that the bone volume in the relevant region was not sufficient for dental implant. Two-stage surgical treatment was planned for the patient. First, vertical and horizontal bone defects were augmented with allogeneic cortical graft application under local anesthesia. After the healing process, dental implants were placed in the sufficient volume of the alveolar bone and the patient's treatment was completed. Conclusion: Allogeneic grafts in the treatment of alveolar crest defects; it is a good alternative to autogenous bone grafts,there is no need for a second surgical field and the resulting reduction in morbidity. How to cite this article: Eriş Derkuş F, Yılmaz UN. Current approach to bone augmentation with allogeneic cortical graft: A case report. Int Dent Res 2021;11(Suppl.1):299-302. https://doi.org/10.5577/intdentres.2021.vol11.suppl1.44 Linguistic Revision: The English in this manuscript has been checked by at least two professional editors, both native speakers of English.

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Periodontal disease defects and mandibular cortical index in lupus patients

Brazilian Dental Science ◽

10.14295/bds.2019.v22i4.1808 ◽

2019 ◽

Vol 22 (4) ◽

pp. 506-512

Author(s):

Vagner Braga ◽

Lucas Morita ◽

Luciana Munhoz ◽

Silvia Lourenço ◽

Emiko Arita

Keyword(s):

Regression Analysis ◽

Bone Loss ◽

Periodontal Disease ◽

Lupus Erythematosus ◽

Alveolar Bone ◽

Bone Defects ◽

Panoramic Radiographs ◽

Cortical Index ◽

Multiple Organs ◽

Mandibular Cortical Index

Objective:Systemic lupus erythematosus is an autoimmune disease that affects multiple organs. It is well known that lupus patients have higher risk of osteoporosis, but if the disease affects mandibular cortical bone and alveolar bone is not fully established. The objective of this study was to evaluate periodontal disease defects and mandibular osteoporotic alterations in patients with lupus as compared to healthy patients using panoramic radiographs.Material and Methods:The panoramic radiographs of 72 patients with lupus and 360 healthy patients were evaluated for the presence of bone loss secondary to periodontal disease, classified as horizontal and vertical bone loss. We also assessed mandibular osteoporotic alterations by using the mandibular cortical index. Logistic regression analysis was applied to estimate the risk of mandibular osteoporotic alterations as well as horizontal and vertical bone loss in patients with lupus as compared to healthy patients.Results:There were no statistically significant differences between groups in the presence of horizontal bone defects and mandibular cortical indexes. However, patients with lupus demonstrated that patients with lupus were 2.17 more likely to present vertical bone loss than healthy patients.Conclusions:Patients with lupus might have higher risk of vertical bone loss than healthy patients due to pathophysiology of their disease. Further larger prospective studies should be performed to confirm our findings.

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Considerable Improvement of Ursolic Acid Water Solubility by Its Encapsulation in Dendrimer Nanoparticles: Design, Synthesis and Physicochemical Characterization

Nanomaterials ◽

10.3390/nano11092196 ◽

2021 ◽

Vol 11 (9) ◽

pp. 2196 ◽

Cited By ~ 1

Author(s):

Silvana Alfei ◽

Anna Maria Schito ◽

Guendalina Zuccari

Keyword(s):

Ursolic Acid ◽

Water Solubility ◽

Drug Loading ◽

Physicochemical Characterization ◽

Systemic Toxicity ◽

Water Soluble ◽

Design Synthesis ◽

Pentacyclic Triterpenoid

Ursolic acid (UA) is a pentacyclic triterpenoid found in many medicinal plants and aromas endowed with numerous in vitro pharmacological activities, including antibacterial effects. Unfortunately, UA is poorly administered in vivo, due to its water insolubility, low bioavailability, and residual systemic toxicity, thus making urgent the development of water-soluble UA formulations. Dendrimers are nonpareil macromolecules possessing highly controlled size, shape, and architecture. In dendrimers with cationic surface, the contemporary presence of inner cavities and of hydrophilic peripheral functions, allows to encapsulate hydrophobic non-water-soluble drugs as UA, to enhance their water-solubility and stability, and to promote their protracted release, thus decreasing their systemic toxicity. In this paper, aiming at developing a new UA-based antibacterial agent administrable in vivo, we reported the physical entrapment of UA in a biodegradable not cytotoxic cationic dendrimer (G4K). UA-loaded dendrimer nanoparticles (UA-G4K) were obtained, which showed a drug loading (DL%) much higher than those previously reported, a protracted release profile governed by diffusion mechanisms, and no cytotoxicity. Also, UA-G4K was characterized by principal components analysis (PCA)-processed FTIR spectroscopy, by NMR and elemental analyses, and by dynamic light scattering experiments (DLS). The water solubility of UA-G4K was found to be 1868-fold times higher than that of pristine UA, thus making its clinical application feasible.

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