release curve
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2022 ◽  
Vol 12 (4) ◽  
pp. 756-762
Author(s):  
Changying Liu ◽  
Xuezhu Wei ◽  
Jun Li ◽  
Chao Liang ◽  
Wei Geng ◽  
...  

The patients with type 2 diabetes mellitus (T2DM) have high dental implant failure frequency. This study explores the function of glimepiride local delivery on dental implant osseointegration in diabetes animal. Glimepiride loaded PLGA microspheres were loaded on the surface of the dental implant, and transplanted into ten Goto-Kakizaki (GK) rats. Blood sugar level and Implant Stability Quotient (ISQ) were measured every week after surgery. Histological, osseointegration rate and bone-implant contact (BIC) rate analysis were performed to evaluate dental osseointegration. The results showed that Glimepiride loaded Poly-lactide-co-glycolide (PLGA) microspheres have sustained-release curve. The glimepiride group exhibited greater ISQ than the control group. The BIC rate of the control and glimepiride group was 44.60%±1.95% and 59.80%±1.79%, respectively. This study demonstrated that the glimepiride group has a significantly greater osseointegration rate than that of the control group. Thus, Glimepiride could provide an alternative drug release microspheres for enhance the dental implant osseointegration in diabetes patients.


Author(s):  
Irene Isabel López-Torres ◽  
Javier Vaquero-Martín ◽  
Ana-Isabel Torres-Suárez ◽  
Federico Navarro-García ◽  
Ana-Isabel Fraguas-Sánchez ◽  
...  

Abstract Purpose Microencapsulation techniques have allowed the addition of rifampicin to bone cement, but its in vivo efficacy has not been proven. The aim of our study is to determine the superiority of cement containing gentamicin and rifampicin microcapsules in the treatment of PJI versus cement exclusively containing gentamicin. Methods An S. aureus PJI was induced in 15 NZW rabbits. A week after inoculation, the first stage of replacement was carried out, and the animals were divided into two groups: group R received a spacer containing gentamicin and rifampicin microcapsules, and group C received a spacer containing gentamicin. Intra-articular release curve of rifampicin and infection and toxicity markers were monitored for four weeks post-operatively, when microbiological analysis was performed. Results The microbiological cultures showed a significantly lower growth of S. aureus in soft tissue (2.3·104 vs 0; p = 0.01) and bone (5.7·102 vs 0; p = 0.03) in the group with rifampicin microcapsules. No differences were found in systemic toxicity markers. Rifampicin release from the cement spacer showed higher concentrations than the staphylococcal MIC throughout the analysis. Conclusion The in vivo analyses demonstrated the superiority of cement containing gentamicin and rifampicin microcapsules versus the isolated use of gentamicin in the treatment of PJI in the rabbit model without serious side effects due to the systemic absorption of rifampicin. Given the increasing incidence of staphylococci-related PJI, the development of new strategies for intra-articular administration of rifampicin for its treatment has a high clinical impact.


Author(s):  
Christian A. Boada ◽  
Assaf Zinger ◽  
Scott Rohen ◽  
Jonathan O. Martinez ◽  
Michael Evangelopoulos ◽  
...  

Apolipoprotein-based drug delivery is a promising approach to develop safe nanoparticles capable of targeted drug delivery for various diseases. In this work, we have synthesized a lipid-based nanoparticle (NPs) that we have called “Aposomes” presenting native apolipoprotein B-100 (apoB-100), the primary protein present in Low-Density Lipoproteins (LDL) on its surface. The aposomes were synthesized from LDL isolated from blood plasma using a microfluidic approach. The synthesized aposomes had a diameter of 91 ± 4 nm and a neutral surface charge of 0.7 mV ± mV. Protein analysis using western blot and flow cytometry confirmed the presence of apoB-100 on the nanoparticle’s surface. Furthermore, Aposomes retained liposomes’ drug loading capabilities, demonstrating a prolonged release curve with ∼80% cargo release at 4 hours. Considering the natural tropism of LDL towards the atherosclerotic plaques, we evaluated the biological properties of aposomes in a mouse model of advanced atherosclerosis. We observed a ∼20-fold increase in targeting of plaques when comparing aposomes to control liposomes. Additionally, aposomes presented a favorable biocompatibility profile that showed no deviation from typical values in liver toxicity markers (i.e., LDH, ALT, AST, Cholesterol). The results of this study demonstrate the possibilities of using apolipoprotein-based approaches to create nanoparticles with active targeting capabilities and could be the basis for future cardiovascular therapies.


Biomedicines ◽  
2021 ◽  
Vol 9 (10) ◽  
pp. 1298
Author(s):  
Chenjia Zhao ◽  
Jingyuan Ji ◽  
Tianjun Yin ◽  
Jing Yang ◽  
Yuan Pang ◽  
...  

Hydrogels have recently received attention as delivery carriers owing to their good biocompatibility and structural similarity to natural extracellular matrices. However, the utilization of traditional single-network (SN) hydrogels is limited by poor mechanical properties and burst drug release. Therefore, we developed a novel double-network (DN) hydrogel, which employs an alginate (ALG)/polyethylene glycol diacrylate (PEGDA) network to adjust the mechanical strength and a positively charged monomer AETAC (2-(acryloyloxy)ethyl]trimethyl-ammonium chloride) to regulate the release curve of the electronegative anti-human papillomavirus (HPV) protein (bovine β-lactoglobulin modified with 3-hydroxyphthalic anhydride) based on an affinity-controlled delivery mechanism. The results show that the double-network hydrogel strongly inhibits the burst release, and the burst release amount is about one-third of that of the single-network hydrogel. By changing the concentration of the photoinitiator, the mechanical strength of the DN hydrogels can be adjusted to meet the stiffness requirements for various tissues within the range of 0.71 kPa to 10.30 kPa. Compared with the SN hydrogels, the DN hydrogels exhibit almost twice the mechanical strength and have smaller micropores. Cytotoxicity tests indicated that these SN and DN hydrogels were not cytotoxic with the result of over 100% relative proliferation rate of the HUVECs. Furthermore, DN hydrogels can significantly alleviate the burst release of antiviral proteins and prolong the release time to more than 14 days. Finally, we utilized digital light processing (DLP) technology to verify the printability of the DN hydrogel. Our study indicates that ALG/PEGDA-AETAC DN hydrogels could serve as platforms for delivering proteins and show promise for diverse tissue engineering applications.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1228
Author(s):  
Peipei Huo ◽  
Xinxu Han ◽  
Wenyu Zhang ◽  
Jing Zhang ◽  
Parveen Kumar ◽  
...  

The application of artemisinin (ART) in the treatment of malaria has been restricted to a certain degree due to its inherent limitations, such as short half-life, poor solubility, limited bioavailability, and re-crystallization. Electrospun nanofibers loaded with ART provide an excellent solution to these limitations and yield sustained drug release as well as inhibition of drug re-crystallization. In this study, ART-loaded polycaprolactone (PCL)/collagen (Col) nanofibers with different proportions of polymers were prepared. ART-loaded PCL/Col nanofibers were characterized, and further ART anti-crystallization and release behaviors were studied. SEM was used to observe the morphology of PCL/Col nanofibers. X-ray diffraction (XRD) was used to characterize the physical state of ART in ART-loaded PCL/Col nanofibers. Fourier transform infrared spectroscopy (FTIR), water contact angle measurement, weight loss, degree of swelling, and drug release experiments can verify the differences in performance of ART-loaded PCL/Col nanofibers due to different polymer ratios. The release curve was analyzed by kinetics, showing sustained release for up to 48 h, and followed the Fickian release mechanism, which was shown by the diffusion index value obtained from the Korsmeyer-Peppas equation.


Nanomaterials ◽  
2021 ◽  
Vol 11 (7) ◽  
pp. 1758
Author(s):  
Shuaikai Ren ◽  
Chunxin Wang ◽  
Liang Guo ◽  
Congcong Xu ◽  
Yan Wang ◽  
...  

Microcapsules have been widely studied owing to their biocompatibility and potential for application in various areas, particularly drug delivery. However, the size of microcapsules is difficult to control, and the size distribution is very broad via various encapsulation techniques. Therefore, it is necessary to obtain microcapsules with uniform and tailored size for the construction of controlled-release drug carriers. In this study, emulsification and solvent evaporation methods were used to prepare a variety of ovalbumin-loaded poly (lactic-co-glycolic acid) (PLGA) microcapsules to determine the optimal preparation conditions. The particle size of the PLGA microcapsules prepared using the optimum conditions was approximately 200 nm, which showed good dispersibility with an ovalbumin encapsulation rate of more than 60%. In addition, porous microcapsules with different pore sizes were prepared by adding a varying amount of porogen bovine serum albumin (BSA) to the internal water phase. The release curve showed that the rate of protein release from the microcapsules could be controlled by adjusting the pore size. These findings demonstrated that we could tailor the morphology and structure of microcapsules by regulating the preparation conditions, thus controlling the encapsulation efficiency and the release performance of the microcapsule carrier system. We envision that this controlled-release novel microcapsule carrier system shows great potential for biomedical applications.


Author(s):  
Larissa L Becker ◽  
Madie R Wensley ◽  
Joel M DeRouchey ◽  
Jason C Woodworth ◽  
Mike D Tokach ◽  
...  

Abstract The objective of this study was to determine the available P (aP) release curve for a new phytase source, GraINzyme Phytase (Agrivida Inc., Woburn, MA), which is expressed in corn containing an engineered Escherichia coli phytase called Phy02. Plant-expressed phytases are created by inserting phytase-encoding genes into plants resulting in their ability to produce seeds with increased concentrations of phytase. A total of 360 pigs (Line 200 × 400, DNA, Columbus, NE, initially 9.9 ± 0.19 kg) were used in a 21-d growth study. Pigs were weaned at approximately 21-d of age, randomly allotted to pens based on initial body weight (BW) and fed common starter diets. From d 18 to 21 post-weaning, all pigs were fed a diet containing 0.11% aP. On d 21 post-weaning, considered d 0 of the study, pens were blocked by BW and randomly allotted to 1 of 8 dietary treatments with 5 pigs per pen and 9 pens per treatment. Dietary treatments were formulated to include increasing aP derived from either an inorganic P source (0.11, 0.19, or 0.27% from monocalcium P) or increasing phytase (150, 250, 500, 1,000, or 1,500 FTU/kg). Diets were corn-soybean meal-based and contained 1.24% standardized ileal digestible (SID) Lys. On d 21 of the trial, 1 pig per pen (weighing closest to the mean pen BW) was euthanized and the right fibula was collected to determine bone ash using the non-defatted processing method. Overall (d 0 to 21), pigs fed increasing aP from inorganic P or phytase had increased (linear, P < 0.002) ADG, ADFI, and G:F (quadratic, P < 0.05). Bone ash weight (g) and percentage bone ash increased (linear, P < 0.001) with increasing inorganic P or added phytase. Based on the composition of the diets used in this study, the release equations developed for GraINzyme for ADG, G:F, bone ash weight, and percentage bone ash are: aP = (0.255 × FTU) ÷ (1299.969 + FTU), aP = (0.233 × FTU) ÷ (1236.428 + FTU), aP = (45999.949 × FTU) ÷ (462529200 + FTU), and aP = (0.272 × FTU) ÷ (2576.581 + FTU), respectively.


2021 ◽  
Vol 11 (2-S) ◽  
pp. 103-108
Author(s):  
M. Chandana ◽  
M. Venkata Ramana ◽  
N. Rama Rao

Valsartan is a potent and specific competitive angiotensin II antagonist which is used in the management of hypertension. It is well absorbed following oral administration, with rather poor bioavailability of about 25 %. Peak plasma concentration of valsartan occurs 2-4 hours after ingestion. Optimized VAL_SLNS are prepared by hot homogenization method and spray dried to improve handling processing and stability. Solid state studies such as FTIR indicated absence of any chemical interaction between valsartan and the lipid. The mean particles size, Polydispersity index (PDI) and entrapment efficiency of optimized formulation (F-05) was found to be 136.5 nm, 0.424, 80.98% respectively. The drug release study from the nano formulation was studied in Phosphate buffer 6.8 for all the formulations F1 F2 F3 F4 and F5. The results demonstrated that V-SLN formulation (F-5) showed biphasic behaviour with an initial burst release followed by a sustained release maximum up to 72-79% till 12 hours. The release curve was found to follow Korsmeyer Peppas model (R2=0.98). Keywords: hot homogenization, hydrogenated soya phosphatidyl choline, sustained release


2020 ◽  
Vol 98 (Supplement_3) ◽  
pp. 39-39
Author(s):  
Madie R Wensley ◽  
Jason C Woodworth ◽  
Joel M DeRouchey ◽  
Mike D Tokach ◽  
Robert D Goodband ◽  
...  

Abstract Two nursery trials (DNA 241×600) with 320 or 280 pigs, respectively (initially 10 kg) were used to determine the available P (aP) release curve for Smizyme TS G5 2,500 (Origination, Inc., Saint Paul, MN). Pigs were weaned at approximately 21-d of age, randomly allotted to pens based on initial body weight (BW) and fed a common diet. On d 21 post-weaning, pens were blocked by BW and randomly allotted to 1 of 8 (Exp. 1) or 7 (Exp. 2) dietary treatments with 5 pigs/pen and 8 pens/treatment. Treatments were formulated to include increasing aP from either inorganic P (0.12%, 0.18%, or 0.24% in Exp. 1 and 0.11%, 0.19%, or 0.27% in Exp. 2 from monocalcium P) or increasing phytase (150, 250, 500, 750, or 1,000 FTU/kg in Exp. 1 and 250, 500, 1000, or 1,500 FTU/kg in Exp. 2). Prior to beginning the 21-d studies, all pigs were fed the lowest inorganic P diet for a 3-d period. At the conclusion of the experiments, the pig closest to the pen mean BW was euthanized and the right fibula was collected to determine bone ash. In both experiments, pigs fed increasing aP from inorganic P had increased (linear, P< 0.01) ADG, G:F, and final BW. Additionally, pigs fed diets with increasing phytase had increased (Exp. 1 linear, P< 0.01, Exp. 2 linear and quadratic, P< 0.05) ADG, ADFI, and G:F. The aP release increased for ADG (Exp. 1 linear, P< 0.01; Exp. 2 linear and quadratic, P< 0.01), G:F (linear, P< 0.01), and bone ash percent (Exp. 1 linear and quadratic, P< 0.05; Exp. 2 linear, P< 0.01) up to the highest phytase inclusion. When combining the release values from Exp. 1 and 2, the release equations for Smizyme TS G5 2,500 are aP=(0.197×FTU)÷(584.956+FTU), aP=(0.175×FTU)÷(248.348+FTU), and aP=(0.165×FTU)÷(178.146+FTU) for ADG, G:F, and bone ash percent, respectively.


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