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

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.

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

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.

Calcium phosphate porous pellets as drug delivery systems: Effect of drug carrier composition on drug loading and in vitro release

2012 ◽  
Vol 32 (11) ◽  
pp. 2679-2690 ◽  
Author(s):  
Hiva Baradari ◽  
Chantal Damia ◽  
Maggy Dutreih-Colas ◽  
Etienne Laborde ◽  
Nathalie Pécout ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Calcium Phosphate ◽  
Drug Delivery Systems ◽  
Drug Carrier ◽  
Drug Loading ◽  
In Vitro Release ◽  
Delivery Systems ◽  
Vitro Release

scholarly journals SYNTHESIS AND CHARACTERIZATION OF THIOLATED JACKFRUIT SEED STARCH AS A COLONIC DRUG DELIVERY CARRIER

2019 ◽  
pp. 53-62 ◽  
Author(s):  
Sanjoy Das ◽  
Malay K. Das
Keyword(s):  
Drug Delivery ◽  
Release Kinetics ◽  
Drug Loading ◽  
Local Treatment ◽  
Entrapment Efficiency ◽  
Esterification Reaction ◽  
Compatibility Study ◽  
Mice Model ◽  
Drug Delivery Carrier

Objective: Site-specific drug delivery into the colonic region is extremely fascinating for local treatment of various colonic diseases like ulcerative colitis, colon cancer but it should be capable of saving the drug from hydrolysis and degradation. The present study reports the application of jackfruit seed starch and its thiol derivative as a drug delivery carrier for the colon. Methods: The starch was extracted from the jackfruit seeds by water extraction method and modified by the esterification reaction with thioglycolic acid. The thiolated starch was characterized for morphology, functional and flow properties. The safety profile of the thiolated starch was confirmed by acute toxicity study in a mice model as per OECD guidelines 423. The microspheres based on thiolated starch were prepared by ionic gelation method incorporating Ibuprofen as a model drug. The prepared microspheres were characterized for particle size, drug entrapment efficiency, drug loading, compatibility study, surface morphology, in vitro drug release and release kinetics. Results: The result attributed that starch was successfully modified by the thiolation with a degree of substitution of 3.30. The size of prepared microspheres ranges from 825.5±4.58 to 857±6.24 µm, the entrapment efficiencies ranges from 69.23±1.19 to 76.15±0.83 % and the drug loading capacity ranges from 17.75±0.30 to 46.05±0.49 %. The FT-IR, DSC and XRD studies confirmed that there is no interaction within drug and excipients. The thiolated starch microspheres show the maximum release of drug at pH 7.4 in the presence of rat caecal content as compared to pH 1.2 and pH 6.8 for up to 24 h and are following first order release kinetics. Conclusion: These results suggest the application of thiolated jackfruit seed starch could be promising as a long-term drug delivery carrier for the colon.

scholarly journals Influence of sterilization on the drug release behaviour of drug coated silicone

2021 ◽  
Vol 7 (2) ◽  
pp. 672-675
Author(s):  
Katharina Wulf ◽  
Stefan Raggl ◽  
Thomas Eickner ◽  
Gerrit Paasche ◽  
Niels Grabow
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Polymer Coating ◽  
Drug Loading ◽  
In Vitro Release ◽  
Physical Chemical ◽  
Release Studies ◽  
Vitro Release ◽  
Dual Drug

Abstract Sterilization processes ensure sterility of drug delivery systems, but may negatively affect the properties of biomaterials and incorporated drugs by changing their physical, chemical, mechanical properties and drug release behaviour. Therefore, it is important to investigate their influence. In this study, the influence of ethylene oxide (EtO) sterilization on the drug loading and release behaviour of incorporated Diclofenac (DCF) in a Poly-L-lactide (PLLA) coating and Dexamethasone (DMS) in the silicone carrier is presented. Silicone samples containing DMS were coated with PLLA containing DCF varying in layer thickness (5, 10, and 20 μm). Half of the samples underwent EtO sterilization, the other half was not sterilized. All un-/sterilized sample surfaces were in view of the morphology and hydrophilicity examined. Furthermore, in vitro release studies of DMS and DCF were conducted. The sterilized sample surfaces showed no morphological and hydrophilicity changes. The DCF and DMS loadings were similar for the sterile and untreated samples. This also applied to the in vitro DMS release profiles apart from the end of the studies where slight differences were evident. The results indicate that both drugs loaded in the polymer coating and the silicone were not impaired by the sterilization process. Thus, EtO sterilization appears suitable for DMS containing silicone and DCF incorporated PLLA coatings as a dual drug delivery system.

scholarly journals Bleomycin Loaded Magnetite Nanoparticles Functionalized by Polyacrylic Acid as a New Antitumoral Drug Delivery System

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
Yue Xu ◽  
Yi Lin ◽  
Lin Zhuang ◽  
Jiong Lin ◽  
Jiahong Lv ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Saturation Magnetization ◽  
Drug Delivery System ◽  
Delivery System ◽  
Magnetite Nanoparticles ◽  
Polyacrylic Acid ◽  
Drug Loading ◽  
In Vitro Release ◽  
Potential Candidate

Objective. To prepare, characterize, and analyze the release behavior of bleomycin-loaded magnetite nanoparticles (BLM-MNPs) coated with polyacrylic acid (PAA) as a new drug delivery system that can be specifically distributed in the tumor site.Methods. BLM-MNPs coated with PAA were prepared using a solvothermal approach. The particles were characterized using scanning electron microscope (SEM), vibrating sample magnetometer (VSM), and Fourier transform infrared spectroscopy (FTIR). The loading and release behaviors of BLM-MNPs were examined by a mathematical formula and in vitro release profile at pH 7.5.Results. The sphere Fe3O4nanoparticles with the size of approximately 30 nm exhibit a saturation magnetization of 87 emu/g. The noncoordinated carboxylate groups of PAA confer on the good dispersibility in the aqueous solution and lead to a good loading efficiency of BLM reaching 50% or higher. Approximately 98% of immobilized BLM could be released within 24 h, of which 22.4% was released in the first hour and then the remaining was released slowly and quantitatively in the next 23 hours.Conclusion. BLM-MNPs were prepared and characterized successfully. The particles show high saturation magnetization, high drug loading capacity, and favorable release property, which could contribute to the specific delivery and controllable release of BLM, and the BLM-MNPs could be a potential candidate for the development of treating solid tumors.

Controlled Release of Doxycycline by Magnetized Microporous MIL53(Fe); Focus on Magnetization and Drug Loading

2018 ◽  
Vol 16 (1) ◽  
pp. 42-50 ◽  
Author(s):  
Shakiba Naeimi ◽  
Hossein Faghihian
Keyword(s):  
Drug Delivery ◽  
Controlled Release ◽  
Drug Loading ◽  
In Vitro Release ◽  
Time Intervals ◽  
Drug Content ◽  
Releasing Process ◽  
Phosphate Buffered Saline ◽  
Vitro Release

Background: In this research, MIL-53(Fe) was magnetized and the performance of the magnetized material as a drug delivery system for doxycycline was studied. Objectives: The experiments were designed to load the magnetic delivery compounds with different amount of the drug. Methods: The in vitro release rate of doxycycline from magnetic MIL-53(Fe) with different drug content into saline buffered fluid (SBF, pH=7.4) and phosphate buffered saline (PBS, pH=3) was then studied. Results: The results showed that the releasing process of the drug in PBS media achieved the equilibration within 48h with 98% of releasing efficiency, while the releasing process in SBF media (pH=7.4) was slower and the equilibrium was established within 264 h with the releasing efficiency of 95%. The amount of the released doxycycline from the samples with different drug content was measured at various time intervals. Conclusion: It was concluded that in PBS media after 75 h, 85, 95 and 98% of loaded doxycycline released, respectively, from the sample containing 22, 32 and 35% of the drug. In SBF media, the release was slower and after 350 h, 82, 91 and 95% of loaded doxycycline released from the samples, respectively, containing 22, 32 and 35 % of the drug. The results of this study indicated that by use of drugreleasing profile and selecting appropriate carrier dose, the released amount of the drug into the patient body can be controlled.

scholarly journals Modified Carboxyl-Terminated PAMAM Dendrimers as Great Cytocompatible Nano-Based Drug Delivery System

2019 ◽  
Vol 20 (8) ◽  
pp. 2016 ◽  
Author(s):  
Minh Thanh Vu ◽  
Long Giang Bach ◽  
Duy Chinh Nguyen ◽  
Minh Nhat Ho ◽  
Ngoc Hoi Nguyen ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Loading ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Malignant Cell ◽  
Pamam Dendrimers ◽  
Optimal Size

Polyamidoamine (PAMAM) dendrimers are extensively researched as potential drug delivery system thanks to their desirable features such as controlled and stable structures, and ease of functionalization onto their surface active groups. However, there have been concerns about the toxicity of full generation dendrimers and risks of premature clearance from circulation, along with other physical drawbacks presented in previous formulations, including large particle sizes and low drug loading efficiency. In our study, carboxyl-terminated PAMAM dendrimer G3.5 was grafted with poly (ethylene glycol) methyl ether (mPEG) to be employed as a nano-based drug delivery system with great cytocompatibility for the delivery of carboplatin (CPT), a widely prescribed anticancer drug with strong side effects so that the drug will be effectively entrapped and not exhibit uncontrolled outflow from the open structure of unmodified PAMAM G3.5. The particles formed were spherical in shape and had the optimal size range (around 36 nm) that accommodates high drug entrapment efficiency. Surface charge was also determined to be almost neutral and the system was cytocompatible. In vitro release patterns over 24 h showed a prolonged CPT release compared to free drug, which correlated to the cytotoxicity assay on malignant cell lines showing the lack of anticancer effect of CPT/mPEG-G3.5 compared with CPT.

scholarly journals The Evaluation of Proanthocyanidins/Chitosan/Lecithin Microspheres as Sustained Drug Delivery System

2018 ◽  
Vol 2018 ◽  
pp. 1-11 ◽  
Author(s):  
Hong-Li Yu ◽  
Zhan-Qin Feng ◽  
Jing-Jing Zhang ◽  
Yong-Hong Wang ◽  
De-Jun Ding ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Loading ◽  
In Vitro Release ◽  
Sustained Drug Delivery ◽  
Swelling Rate ◽  
Drying Technology ◽  
The Stability

Proanthocyanidin (PC) has attracted wide attention on cosmetics and pharmaceutical due to its antioxidant, anticancer, antimicrobial, antiangiogenic, and anti-inflammatory activities. However, PC applications are limited because of its sensitivity to thermal treatment, light, and oxidation and the poor absorption in the gastrointestinal tract. Thus, a novel dosage form of PC needs to be designed to improve its stability and bioavailability for drug delivery. The objective of this study is to fabricate proanthocyanidins/chitosan/lecithin (PC/CTS/LEC) microspheres and investigate various characteristics. In the current study, PC/CTS/LEC microspheres were prepared by spray-drying technology. The yield (61.68%), encapsulation efficiency (68.19%), and drug loading capacity (17.05%) were found in the results. The scanning electron microscope demonstrated that the microspheres were spherical in shape with wrinkled surfaces. DSC study displayed that the microspheres stability was greatly improved when comparing with bare PC. The in vitro release study showed that the 76.92% of PC was released from microspheres within 48 h. The moisture contents of microspheres ranged from 8% to 13%. The swelling rate and tapped density of microspheres were elevated with increasing the concentration of chitosan in the formulations. The moisture uptake of microspheres was saturated at 40°C/RH75% within 12 h. Our results indicated that the stability of PC/CTS/LEC microspheres was enhanced, and it is a promising carrier for sustained drug delivery system.

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