Minocycline-loaded calcium polyphosphate glass microspheres as a potential drug-delivery agent for the treatment of periodontitis

Background: Periodontitis is an inflammatory disease with a bacterial etiology that affects the supporting structures of the teeth and is a major cause of tooth loss. The objective of this study was to investigate the drug loading and in vitro release of minocycline from novel calcium polyphosphate microspheres intended for use in treating periodontitis. Methods: Calcium polyphosphate coacervate, produced by a precipitation reaction of calcium chloride and sodium polyphosphate solutions, was loaded with minocycline and subsequently used to produce microspheres by an emulsion/solvent extraction technique. Microspheres classified by size were subjected to a 7-day elution in a Tris-buffer solution under dynamic conditions. The physicochemical characteristics of the drug-loaded microspheres were investigated using scanning electron microscopy, particle size analysis, Phosphorus-31 Nuclear Magnetic Resonance spectroscopy, and Inductively Coupled Plasma Optical Emission Spectroscopy. Drug loading and release were determined using ultraviolet -visible (UV/VIS) spectrophotometry. Results: Minocycline-loaded calcium polyphosphate microspheres of varying size were successfully produced, with small and large microspheres having volume mean diameters of 22 ± 1 µm and 193 ± 5 µm, respectively. Polyphosphate chain length and calcium to phosphorus mole ratio remained stable throughout microsphere production. Drug loading was 1.64 ± 0.16, 1.35 ± 0.55, and 0.84 ± 0.14 weight% for the coacervate and large and small microspheres, respectively, corresponding to mean encapsulation efficiencies of 81.7 ± 12.2 % and 50.9 ± 3.9 % for the large and small microspheres. Sustained drug release was observed in vitro over a clinically relevant 7-day period, with small and large microspheres exhibiting similar elution profiles. Antibiotic release generally followed microsphere degradation as measured by Ca and P ion release. Conclusions: This study demonstrated successful drug loading of calcium polyphosphate microspheres with minocycline. Furthermore, in vitro sustained release of minocycline over a 7-day period was observed, suggesting potential utility of this approach for treating periodontitis.

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In Vitro and In Vivo Evaluation of Desogestrel-Loaded Poly(D,L-lactic Acid) Nanoparticles

Journal of Nanomaterials ◽

10.1155/2019/8491269 ◽

2019 ◽

Vol 2019 ◽

pp. 1-14 ◽

Cited By ~ 1

Author(s):

Hui Lin ◽

Guoyong Jia ◽

Peng Sun ◽

Liqiao Zhu ◽

Jinna Chen ◽

...

Keyword(s):

Drug Loading ◽

In Vitro Release ◽

Particle Diameter ◽

Phase Ratio ◽

Diffusion Method ◽

Size Analysis ◽

Average Particle ◽

Solvent Diffusion ◽

Emulsion Solvent Diffusion Method

The aim of this study was to explore the synthesis parameters of desogestrel-polylactic acid nanoparticles (DG-PLA-NPs), optimise the preparation technology, and elucidate the in vitro release characteristics. Considering encapsulation efficiency (EE) and drug loading as the main evaluation indexes, DG-PLA-NPs were prepared using the modified emulsion solvent diffusion method and single factor and orthogonal design tests were performed to investigate the influencing factors and optimise the preparation method. Morphology of the nanoparticles was observed using transmission electron microscopy (TEM), average particle diameter and distribution were determined using dynamic laser particle size analysis, and the EE and drug loading were measured using reversed-phase high-performance liquid chromatography. Among the eight factors, the drug-to-material ratio, water-to-organic phase ratio, and polyvinyl alcohol (PVA) concentration significantly affected the NP EE. In the optimised formulation, the PLA/DG ratio, PVA concentration, and oil-to-water phase ratio were 5, 0.5%, and 5, respectively. The DG-PLA-NPs prepared with the optimised formulation were round or spherical with an average diameter of 209 nm, 79.60% EE, and 6.81% drug loading capacity. The polydispersity index was 0.181, and the zeta potential was −27.37 mV. The in vitro releases of both DG and DG-PLA-NPs conformed to the Weibull equation. The DG-PLA-NPs released desogestrel rapidly in the early stages but slowly at later stages, indicating that compared to DG, the DG-PLA-NPs had obvious sustained-release effects. The DG-PLA-NPs prepared by the modified emulsion solvent diffusion method were small, simple to prepare, and had high drug loading with promising application prospects.

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Preparation and in vitro Evaluation of Bioadhesive Microparticulate System

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2008.1.3.9 ◽

1970 ◽

Vol 1 (3) ◽

pp. 257-266

Author(s):

Nagda C. D. ◽

Chotai N. P. ◽

Patel S. B. ◽

Soni T. J ◽

Patel U. L

Keyword(s):

Drug Loading ◽

In Vitro Release ◽

Phenyl Acetic Acid ◽

Solvent Evaporation Method ◽

Elimination Half ◽

Release Studies ◽

Differential Scanning Colorimetry ◽

Polymer Interactions ◽

Vitro Release

Aceclofenac (ACE) is NSAIDs of a phenyl acetic acid class. It is indicated in arthritis and osteoarthritis, rheumatoid arthritis, ankylosing spondylitis. It has short elimination half life of 4 hours. The objective of the study is to design, characterize and evaluate bioadhesive microspheres of ACE employing carbopol (CP) as bioadhesive polymer. Bioadhesive microspheres of ACE were prepared by solvent evaporation method. The prepared microspheres were free flowing and spherical in shape and characterized for drug loading, mucoadhesion test, infrared spectroscopy (IR), differential scanning colorimetry (DSC) and scanning electron microscopy (SEM). The in-vitro release studies were performed using pH 6.8 phosphate buffer. The drug loaded microspheres in a ratio of 1:5 showed 47% of drug entrapment; percentage mucoadhesion was 81% and 89% release in 10 h. The infrared spectra and DSC showed stable character of aceclofenac in the drug loaded microspheres and revealed the absence of drug-polymer interactions. SEM studies showed that the microspheres are spherical and porous in nature. The in vitro release profiles from microspheres of different polymer-drug ratios followed Higuchi model.

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Stereocomplexation Assisted Assembly of Poly(γ-glutamic Acid)-graft-polylactide Nano-micelles and Their Efficacy as Anticancer Drug Carrier

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520617666170911170104 ◽

2018 ◽

Vol 18 (2) ◽

pp. 302-311

Author(s):

Shulin Dai ◽

Yucheng Feng ◽

Shuyi Li ◽

Yuxiao Chen ◽

Meiqing Liu ◽

...

Keyword(s):

Glutamic Acid ◽

Drug Carrier ◽

Drug Loading ◽

Drug Carriers ◽

Cancer Drug ◽

Drug Release Profile ◽

Sustained Drug Release ◽

Anti Cancer ◽

Physical Interactions

Background: Micelles as drug carriers are characterized by their inherent instability due to the weak physical interactions that facilitate the self-assembly of amphiphilic block copolymers. As one of the strong physical interactions, the stereocomplexation between the equal molar of enantiomeric polylactides, i.e., the poly(L-lactide) (PLLA) and poly(D-lactide) (PDLA), may be harnessed to obtain micelles with enhanced stability and drug loading capacity and consequent sustained release. </P><P> Aims/Methods: In this paper, stereocomplexed micelles gama-PGA-g-PLA micelles) were fabricated from the stereocomplexation between poly(gama-glutamic acid)-graft-PLLA gama-PGA-g-PLA) and poly(gamaglutamic acid)-graft-PDLA gama-PGA-g-PLA). These stereocomplexed micelles exhibited a lower CMC than the corresponding enantiomeric micelles. Result: Furthermore, they showed higher drug loading content and drug loading efficiency in addition to more sustained drug release profile in vitro. In vivo imaging confirmed that the DiR-encapsulated stereocomplexed gama-PGA-g-PLA micelles can deliver anti-cancer drug to tumors with enhanced tissue penetration. Overall, gama-PGA-g-PLA micelles exhibited greater anti-cancer effects as compared with the free drug and the stereocomplexation may be a promising strategy for fabrication of anti-cancer drug carriers with significantly enhanced efficacy.

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Preparation, evaluation, and in vitro release of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules

Technology and Health Care ◽

10.3233/thc-202529 ◽

2020 ◽

pp. 1-9

Author(s):

Yunhong Wang ◽

Rong Hu ◽

Yanlei Guo ◽

Weihan Qin ◽

Xiaomei Zhang ◽

...

Keyword(s):

Drug Release ◽

Sustained Release ◽

Release Rate ◽

Orthogonal Design ◽

Drug Loading ◽

In Vitro Release ◽

Core Material ◽

Evaluation Indexes ◽

Vitro Release

OBJECTIVE: In this study we explore the method to prepare tanshinone self-microemulsifying sustained-release microcapsules using tanshinone self-microemulsion as the core material, and chitosan and alginate as capsule materials. METHODS: The optimal preparation technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules was determined by using the orthogonal design experiment and single-factor analysis. The drug loading and entrapment rate were used as evaluation indexes to assess the quality of the drug, and the in vitro release rate was used to evaluate the drug release performance. RESULTS: The best technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules is as follows: the concentration of alginate is 1.5%, the ratio of tanshinone self-microemulsion volume to alginate volume to chitosan mass is 1:1:0.5 (ml: ml: g), and the best concentration of calcium chloride is 2.0%. To prepare the microcapsules using this technology, the drug loading will be 0.046%, the entrapment rate will be 80.23%, and the 24-hour in vitro cumulative release rate will be 97.4%. CONCLUSION: The release of the microcapsules conforms to the Higuchi equation and the first-order drug release model and has a good sustained-release performance.

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Development of Spanish Broom and Flax Dressings with Glycyrrhetinic Acid-Loaded Films for Wound Healing: Characterization and Evaluation of Biological Properties

Pharmaceutics ◽

10.3390/pharmaceutics13081192 ◽

2021 ◽

Vol 13 (8) ◽

pp. 1192

Author(s):

Angela Abruzzo ◽

Concettina Cappadone ◽

Valentina Sallustio ◽

Giovanna Picone ◽

Martina Rossi ◽

...

Keyword(s):

Wound Healing ◽

Drug Loading ◽

Healing Process ◽

In Vitro Release ◽

Sodium Hyaluronate ◽

Biological Properties ◽

Glycyrrhetinic Acid ◽

Wound Dressings ◽

Biological Studies

The selection of an appropriate dressing for each type of wound is a very important procedure for a faster and more accurate healing process. So, the aim of this study was to develop innovative Spanish Broom and flax wound dressings, as alternatives to cotton used as control, with polymeric films containing glycyrrhetinic acid (GA) to promote wound-exudate absorption and the healing process. The different wound dressings were prepared by a solvent casting method, and characterized in terms of drug loading, water uptake, and in vitro release. Moreover, biological studies were performed to evaluate their biocompatibility and wound-healing efficacy. Comparing the developed wound dressings, Spanish Broom dressings with GA-loaded sodium hyaluronate film had the best functional properties, in terms of hydration ability and GA release. Moreover, they showed a good biocompatibility, determining a moderate induction of cell proliferation and no cytotoxicity. In addition, the wound-healing test revealed that the Spanish Broom dressings promoted cell migration, further facilitating the closure of the wound.

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Comparative Analysis of Morphological and Release Profiles in Ocular Implants of Acetazolamide Prepared by Electrospinning

Pharmaceutics ◽

10.3390/pharmaceutics13020260 ◽

2021 ◽

Vol 13 (2) ◽

pp. 260

Author(s):

Mariana Morais ◽

Patrícia Coimbra ◽

Maria Eugénia Pina

Keyword(s):

Drug Release ◽

In Vitro Release ◽

Morbidity Rate ◽

Coating Film ◽

Sustained Drug Release ◽

Coated Implant ◽

Poly Ethylene ◽

Coaxial Fibers ◽

Release Profiles

The visual impairment that often leads to blindness causes a higher morbidity rate. The goal of this work is to create a novel biodegradable polymeric implant obtained from coaxial fibers containing the dispersed drug—acetazolamide—in order to achieve sustained drug release and increase patient compliance, which is of the highest importance. Firstly, during this work, uncoated implants were produced by electrospinning, and rolled in the shape of small cylinders that were composed of uniaxial and coaxial fibers with immobilized drug inside. The fibers were composed by PCL (poly ε-caprolactone) and Lutrol F127 (poly (oxyethylene-b-oxypropylene-b-oxyethylene)). The prepared implants exhibited a fast rate of drug release, which led to the preparation of new implants incorporating the same formulation but with an additional coating film prepared by solvent casting and comprising PCL and Lutrol F127 or PCL and Luwax EVA 3 ((poly (ethylene-co-vinyl acetate)). Implants were characterized and in vitro release profiles of acetazolamide were obtained in phosphate buffered saline (PBS) at 37 °C. The release profile of the acetazolamide from coated implant containing Luwax EVA 3 is considerably slower than what was observed in case of coated implants containing Lutrol F127, allowing a sustained release and an innovation relatively to other ocular drug delivery systems.

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Eudragit S-100 coated sodium alginate microspheres of naproxen sodium: Formulation, optimization and in vitro evaluation / Alginatne mikrosfere naproksen natrija obložene Eudragitom S-100: Priprava, optimizacija i in vitro vrednovanje

Acta Pharmaceutica ◽

10.2478/v10007-012-0034-x ◽

2012 ◽

Vol 62 (4) ◽

pp. 529-545 ◽

Cited By ~ 23

Author(s):

Anuj Chawla ◽

Pooja Sharma ◽

Pravin Pawar

Keyword(s):

Drug Release ◽

Sodium Alginate ◽

Naproxen Sodium ◽

Drug Loading ◽

Size Analysis ◽

Scanning Calorimetry ◽

Sem Images ◽

S 100 ◽

Eudragit S 100

The aim of the study was to prepare site specific drug delivery of naproxen sodium using sodium alginate and Eudragit S-100 as a mucoadhesive and pH-sensitive polymer, respectively. Core microspheres of alginate were prepared by a modified emulsification method followed by cross-linking with CaCl2, which was further coated with the pH dependent polymer Eudragit S-100 (2.5 or 5 %) to prevent drug release in the upper gastrointestinal environment. Microspheres were characterized by FT-IR spectroscopy, X-ray diffraction, differential scanning calorimetry and evaluated by scanning electron microscopy, particle size analysis, drug loading efficiency, in vitro mucoadhesive time study and in vitro drug release study in different simulated gastric fluids. Stability studies of the optimized formulation were carried out for 6 months. SEM images revealed that the surface morphology was rough and smooth for core and coated microspheres, respectively. Core microspheres showed better mucoadhesion compared to coated microspheres when applied to the mucosal surface of freshly excised goat colon. The optimized batch of core microspheres and coated microspheres exhibited 98.42 ± 0.96 and 95.58 ± 0.74 % drug release, respectively. Drug release from all sodium alginate microsphere formulations followed Higuchi kinetics. Moreover, drug release from Eudragit S-100 coated microspheres followed the Korsmeyer-Peppas equation with a Fickian kinetics mechanism. Stability study suggested that the degradation rate constant of microspheres was minimal, indicating 2 years shelf life of the formulation.

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Minocycline hydrochloride loaded mPEG-PCLA membranes: Preparation and in vitro evaluation for periodontitis therapy

Journal of Bioactive and Compatible Polymers ◽

10.1177/0883911521992795 ◽

2021 ◽

pp. 088391152199279

Author(s):

Ningtao Wang ◽

Zhengmei Huang ◽

Shenchun Wang ◽

Meidong Lang ◽

Xiuyin Zhang

Keyword(s):

Drug Delivery ◽

Drug Loading ◽

Membrane Surface ◽

Local Treatment ◽

In Vitro Release ◽

Periodontal Pathogen ◽

Antibacterial Drug ◽

Periodontal Ligament Fibroblasts ◽

Minocycline Hydrochloride

This study was aimed at alleviating shortcomings in the treatment of periodontitis by preparation of a biopolymer membrane loaded with minocycline hydrochloride (MH) inserted into periodontal pockets to treat infections. Monomethoxy-poly (ethylene glycol)-poly (ε-caprolactone-co-L-lactide) (mPEG-PCLA) is a biocompatible and biodegradable amphiphilic block copolymer. It, therefore, has attracted considerable attention in drug delivery systems and periodontal treatment. We chose it as a membrane material for MH-drug loading. The MH-loaded membranes were prepared by the solvent casting technique with the content of 5, 8 and 10 wt.%, respectively. Fourier transform infrared spectra (FTIR) revealed no interaction between MH and polymer. The drug-loaded membrane surface morphology was investigated by scanning electron microscopy (SEM). In vitro release studies showed that the initial drug release exceeded 40% within 24 h, followed by a sustained release for up to 2 weeks, which would enable the therapeutic level to maintain over a longer time. The antibacterial activity studies in vitro demonstrated a positive effect on the periodontal pathogen. MH drug-loaded membranes have no adverse effect on the growth of periodontal ligament fibroblasts in the MTT test. The study suggests that mPEG-PCLA membranes containing MH are a potential antibacterial drug delivery system for local treatment of periodontitis.

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Development and characterization of phytosterol nanoemulsions and self-microemulsifying drug delivery systems

10.1101/585166 ◽

2019 ◽

Author(s):

Yuan Chuanxun ◽

Zhang Xueru ◽

Jin Risheng

Keyword(s):

Drug Delivery ◽

Delivery System ◽

Drug Loading ◽

In Vitro Release ◽

Pharmacokinetic Analysis ◽

Polyethylene Glycol 400 ◽

Hydrogenated Castor Oil ◽

Release Curve ◽

Tween 60

AbstractThe aim of this study is to develop a self microemulsion drug delivery system for phytosterols to improve the solubility and bioavailability. The results showed that the formulation of phytosterol self-microemulsion is: lemon essential oil in oil phase, polyoxyethylene hydrogenated castor oil 40 and Tween 60 in emulsifier, polyethylene glycol 400 in co-emulsifier, Km = 7:3, Kp = 3:1, Ke = 50%. The drug loading of phytosterol self-microemulsion prepared by this method was 87.22 mg/g, encapsulation efficiency was 89.65%, particle size was 48.85nm, potential was −12.863mV. In vitro release experiment showed that the release of phytosterols in microemulsion was more than 90%, and the release curve was in accordance with the first-order kinetics equation. The pharmacokinetic analysis of PSSM synthesized by this method shows that PSSM can increase the bioavailability of PS more than three times, so it is necessary to do more in-depth research on the self-microemulsion delivery system of phytosterols.

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Cellulose/guar gum hydrogel microspheres as a magnetic anticancer drug carrier

BioResources ◽

10.15376/biores.14.2.3615-3629 ◽

2019 ◽

Vol 14 (2) ◽

pp. 3615-3629 ◽

Cited By ~ 1

Author(s):

Yanli Li ◽

Yucheng Feng ◽

Jun Jing ◽

Fei Yang

Keyword(s):

Anticancer Drug ◽

Guar Gum ◽

Drug Carrier ◽

Drug Loading ◽

In Vitro Release ◽

Adsorption Effect ◽

Magnetic Hydrogel ◽

Vitro Release ◽

Hydrogel Microspheres

A novel magnetic anticancer drug carrier based on cellulose, guar gum, and Fe3O4 hydrogel microspheres was synthesized by chemical crosslinking. These microspheres were crosslinked with epoxy chloropropane and loaded with 5-fluorouracil (5-fu). The effect of the ratio of cellulose to guar gum on bead size, drug loading, and in vitro release behaviors were investigated. The influence of the magnetic content on drug loading and in vitro release behaviors were also evaluated. The magnetic hydrogel microspheres were characterized via an optical microscope, Fourier transform infrared spectroscopy, swelling behavior analysis, vibrating sample magnetometer, and ultraviolet absorption spectroscopy. The results showed that as the ratio of cellulose to guar gum increased from 3:1 to 5:1, the particle size increased from 395 to 459 um. Moreover, the drug loading capacity, encapsulation efficiency, and in vitro release behavior were influenced by the ratio of cellulose/guar gum and Fe3O4 content. Finally, the Fe3O4 particle had an adsorption effect on the drug, thereby reducing the maximum cumulative release.

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