Minocycline hydrochloride plus metronidazole versus metronidazole alone for peri-implantitis: a comparative study.

OBJECTIVE: To evaluate the efficacy of minocycline hydrochloride combined with metronidazole versus metronidazole alone in treating peri-implantitis and their impact on specific inflammatory markers. METHODS: A retrospective review was undertaken of 107 patients with peri-implantitis from January 2018 to January 2021. Patients were treated either with metronidazole alone (Con group, n = 57) or with additional minocycline hydrochloride (Exp group, n = 50). Inflammatory markers, including interleukin-6 (IL-6), interleukin-1 beta (IL-1ß), tumor necrosis factor alpha (TNF-α), and matrix metalloproteinase-8 (MMP-8) were determined before and after treatment. Clinical outcomes were determined using the plaque index (PLI), gingival sulcus bleeding index (SBI), and periodontal probing depth (PD). Furthermore, receiver operator characteristic (ROC) curves analyzed the clinical relevance of the markers. Logistic regression was conducted to analyze the risk factors affecting efficacy in patients. RESULTS: The Exp group exhibited more favorable clinical outcomes and showed lower levels of IL-6, IL-1ß, TNF-α, and MMP-8 than the Con group. IL-1ß, TNF-α, and MMP-8 levels were significantly correlated with treatment success (P < 0.05), but IL-6 was not (P > 0.05). The ROC curves for IL-1ß and TNF-α significantly outperformed those for IL-6 and MMP-8 (P < 0.05). Logistic regression analysis showed that only IL-1ß and TNF-α were independent risk factors affecting efficacy in patients. CONCLUSION: Combining minocycline hydrochloride with metronidazole yields better outcomes for peri-implantitis compared to metronidazole alone. Of the factors analyzed, only IL-1ß and TNF-α emerged as dependable independent efficacy indicators.

Minocycline hydrochloride ointment combined with Vitapex paste is effective for middle-aged and elderly patients with combined periodontal-endodontic lesions.

OBJECTIVE: This study was designed to determine the efficacy of minocycline hydrochloride ointment (MHO) combined with Vitapex paste on middle-aged and elderly patients with combined periodontal-endodontic lesions (CPELs) and its effect on the inflammatory factors. METHODS: The data of 88 elderly patients with CPELs treated in the First Affiliated Hospital of Gannan Medical University from March 2020 to March 2022 were analyzed retrospectively. Among them, the patients treated with MHO and iodoform zinc oxide clove oil paste were assigned into the control group (n = 42) and the rest of the patients treated by MHO and Vitapex paste were assigned to the study group (n = 46). The inflammatory factors, periodontal indexes and efficacy were determined and compared between the two groups. The MOS 36-Item Short-Form Health Survey (SF-36) was adopted to evaluate the quality of life (QoL) of patients before and after treatment. Additionally, the adverse reactions of the two groups during treatment were analyzed and compared. The prognosis of the two groups of patients was analysed, and factors impacting their prognosis was analysed through the Logistic regression analysis. RESULTS: Before treatment, the levels of interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α) and interleukin-1ß (IL-1ß) were not significantly different between the two groups (all P > 0.05), while after treatment, these levels in both groups decreased significantly, with notably lower levels in the study group than those in the control group (all P < 0.05). Before treatment, the gingival index (GI), plaque index (PLI), probing depth (PD) and bleeding index (BD) of the two groups were similar (all P > 0.05); however, after treatment, the levels of GI, PD, PLI and BI of both groups decreased significantly (all P < 0.05), with more notable decreases in the study group than those in the control group (all P < 0.05). The study group showed a significantly higher overall response rate than the control group (P < 0.05). Before treatment, the SF-36 scores of the two groups were not significantly different (P > 0.05), while after treatment, both groups had significantly increased SF-36 scores, and the score in study group was significantly higher than the control group (P < 0.05). In addition, the incidence of adverse reactions was not notably different between the two groups (P > 0.05). According to univariate analysis, age, dental lesion grade, course of disease, and persistent dull pain were the risk factors affecting the prognosis of patients. According to multivariate analysis, dental lesion grade was the independent risk factor affecting the prognosis. CONCLUSION: MHO combined with Vitapex paste is effective for middle-aged and elderly patients with CPELs, which can effectively inhibit the patients' inflammatory reaction and improve their periodontal condition and QoL, with a low adverse reaction rate, so it is worthy of clinical promotion.

C4BP(ß-)-mediated immunomodulation attenuates inflammation in DSS-induced murine colitis and in myeloid cells from IBD patients.

The most recent and promising therapeutic strategies for inflammatory bowel disease (IBD) have engaged biologics targeting single effector components involved in major steps of the immune-inflammatory processes, such as tumor necrosis factor, interleukins or integrins. Nevertheless, these molecules have not yet met expectations regarding efficacy and safety, resulting in a significant percentage of refractory or relapsing patients. Thus, novel treatment options are urgently needed. The minor isoform of the complement inhibitor C4b-binding protein, C4BP(ß-), has been shown to confer a robust anti-inflammatory and immunomodulatory phenotype over inflammatory myeloid cells. Here we show that C4BP(ß-)-mediated immunomodulation can significantly attenuate the histopathological traits and preserve the intestinal epithelial integrity in dextran sulfate sodium (DSS)-induced murine colitis. C4BP(ß-) downregulated inflammatory transcripts, notably those related to neutrophil activity, mitigated circulating inflammatory effector cytokines and chemokines such as CXCL13, key in generating ectopic lymphoid structures, and, overall, prevented inflammatory immune cell infiltration in the colon of colitic mice. PRP6-HO7, a recombinant curtailed analogue with only immunomodulatory activity, achieved a similar outcome as C4BP(ß-), indicating that the therapeutic effect is not due to the complement inhibitory activity. Furthermore, both C4BP(ß-) and PRP6-HO7 significantly reduced, with comparable efficacy, the intrinsic and TLR-induced inflammatory markers in myeloid cells from both ulcerative colitis and Crohn's disease patients, regardless of their medication. Thus, the pleiotropic anti-inflammatory and immunomodulatory activity of PRP6-HO7, able to "reprogram" myeloid cells from the complex inflammatory bowel environment and to restore immune homeostasis, might constitute a promising therapeutic option for IBD.

Characterization of the Interactions between Minocycline Hydrochloride and Trypsin with Spectroscopic and Molecular Docking Technology.

In the current study, the interaction of minocycline hydrochloride (MC) and trypsin (TRP) was studied using fluorescence spectroscopy, synchronous fluorescence spectroscopy, three-dimensional fluorescence spectroscopy, UV-Vis spectroscopy, and molecular docking simulation techniques. The results show that the fluorescence quenching of trypsin at different degrees can be caused by minocycline hydrochloride at different temperatures. According to the Stern-Volmer equation, the fluorescence quenching type was static quenching. By calculating critical distance, we concluded that there is a possibility of non-radiative energy transfer between minocycline hydrochloride and trypsin. The effect of minocycline hydrochloride on the secondary structure of trypsin was demonstrated using ultraviolet spectroscopy. Synchronous fluorescence spectroscopy showed that minocycline hydrochloride could bind to tryptophan residues in trypsin, resulting in corresponding changes in the secondary structure of trypsin. Three-dimensional fluorescence spectroscopy showed that minocycline hydrochloride had a particular effect on the microenvironment of trypsin that led to changes in the secondary structure of trypsin. The molecular docking technique demonstrated that the binding of minocycline hydrochloride and trypsin was stable. Circular dichroism showed that the secondary structure of trypsin could be changed by minocycline hydrochloride.

A multiple controlled-release hydrophilicity minocycline hydrochloride delivery system for the efficient treatment of periodontitis.

The complexity of periodontitis, including the complex formation mechanisms and the complex periodontium physiological environment, as well as the complex association with multiple complications, often results in poor therapy effects. Herein, we aimed to design a nanosystem with a controlled release of minocycline hydrochloride (MH) and good retention to effectively treat periodontitis by inhibiting inflammation and repairing the alveolar bone. Firstly, insoluble ion-pairing (IIP) complexes were constructed to improve the encapsulation efficiency of hydrophilic MH in PLGA nanoparticles. Then, a nanogenerator was constructed and combined with a double emulsion method to encapsulate the complexes into PLGA nanoparticles (MH-NPs). The average particle size of MH-NPs was about 100 nm as observed by AFM and TEM, and the drug loading and encapsulation efficiency were 9.59% and 95.58%, respectively. Finally, a multifunctional system (MH-NPs-in-gels) was prepared by dispersing MH-NPs into thermosensitive gels, which could continue to release drug for 21 days in vitro. And the release mechanism showed that this controlled release behavior for MH was influenced by the insoluble ion-pairing complex, PLGA nanoparticles, and gels. In addition, the periodontitis rat model was established to investigate the pharmacodynamic effects. After 4 weeks of treatment, changes in the alveolar bone were assessed by Micro-CT (BV/TV: 70.88%; BMD: 0.97 g/cm3; TB.Th: 0.14 mm; Tb.N: 6.39 mm-1; Tb.Sp: 0.07 mm). The mechanism of MH-NPs-in-gels in vivo was clarified by the analysis of pharmacodynamic results, which showed that insoluble ion-pairing complexes with the aid of PLGA nanoparticles and gels achieved significant anti-inflammatory effects and bone repair capabilities. In conclusion, the multiple controlled-release hydrophilicity MH delivery system would have good prospects for the effective treatment of periodontitis.

Clinical Efficacy of Minocycline Hydrochloride for the Treatment of Peri-Implant Disease: A Systematic Review With Meta-Analysis of Randomized Controlled Trials.

This systematic review aimed to assess the clinical efficacy of the local application of minocycline hydrochloride for treating peri-implantitis. Four databases-PubMed, EMBASE, Cochrane Library, and China National Knowledge Infrastructure-were searched from their inception through December 2020. English and Chinese randomized controlled trials (RCTs) that compared minocycline hydrochloride with control regimes, including negative control, iodine solution or glycerin, and chlorhexidine, for patients with peri-implant diseases were retrieved. Three outcomes-plaque index (PLI), probing depth (PD), and sulcus bleeding index (SBI)-were assessed using meta-analysis based on the random-effects model. Fifteen RCTs were included in the present meta-analysis, and results suggested that minocycline hydrochloride significantly affected PLI, PD, or SBI reduction regardless of the type of comparator regime. However, subgroup analyses suggested that minocycline hydrochloride was not superior to chlorhexidine in terms of reduction of PLI (1 week: MD = -0.18, 95% CI = -0.55 to 0.20, P = .36; 4 weeks: MD = -0.08, 95% CI = -0.23 to 0.07, P = .28; 8 weeks: MD = -0.01, 95% CI = -0.18 to 0.16, P = .91) and PD (1 week: MD = 0.07, 95% CI = -0.27 to 0.41, P = .68; 4 weeks: MD = -0.10, 95% CI = -0.43 to 0.24, P = .58; 8 weeks: MD = -0.30, 95% CI = -0.68 to 0.08, P = .12), and minocycline hydrochloride was also not better than chlorhexidine regarding reduction of SBI at 1 week after treatment (MD = -0.10; 95% CI = -0.21 to 0.01; P = .08). This study concludes that minocycline hydrochloride as adjuvant therapy of nonsurgical treatment enhances the clinical results when compared to control regimes. However, the difference between minocycline hydrochloride and chlorhexidine should be further investigated by designing additional high-quality studies with large sample sizes.

Efficacy of minocycline hydrochloride aspiration sclerotherapy with additional monoethanolamine oleate aspiration sclerotherapy for symptomatic hepatic cysts.

AIM: Minocycline hydrochloride (MINO) aspiration sclerotherapy (AS) has been widely used for treating hepatic cysts (HC). However, cyst recurrence remains problematic. Information on monoethanolamine oleate (EO) AS, another effective HC treatment, is currently limited. We investigated the efficacy of EO on ineffective MINO treatments, and the relationship between MINO AS and cyst fluid pH. METHODS: A total of 22 cases with symptomatic HC underwent AS with 500 mg of MINO from January 2016 to June 2021. Cyst fluid pH was measured before and after MINO injection. Cyst volume ratio (CVR, %) after 2 weeks was calculated as follows:cyst volume 2 weeks after MINO injection / pre-treatment cyst volume × 100. Treatment was completed if CVR after 2 weeks was ≤35% (MINO-group). For patients with CVR >35%, 2 g of EO was added (MINO/EO-group). Cyst volume ratio was measured every 12 months thereafter. RESULTS: There were no recurrence symptoms in any of the patients during follow-up. Of the 22 cases, 21 had CVR ≤20% after 12 months. The MINO/EO-group (n = 8) tended to have smaller CVRs after 12 months than the MINO-group (n = 14). Cyst volume ratio after 2 weeks was correlated to pH change (p = 0.012) and was larger in patients whose pH decreased by <1.5 (p = 0.015). All adverse events were mild, including in elderly patients. CONCLUSION: Adding EO is an effective and safe treatment for symptomatic HC when MINO AS alone is insufficient. Patients with pH decreases of <1.5 should be considered for additional EO treatment.

A short-term efficacy evaluation of biological antibacterial peptides in the adjuvant therapy of stageⅢ periodontitis / 口腔医学

Objective@#To investigate the efficacy of antibacterial peptides in the adjuvant therapy of stage Ⅲ periodontitis.@*Methods@#Fifty-one patients were randomly divided into simple mechanical curettage group, minocycline hydrochloride group and antibacterial peptide group according to the treatment mode. Three groups received periodontal sequential treatment, and after the ultrasonic supragingival scaling, they were performed with curettage, root surface planing, polishing and flushing. After treatment in the minocycline hydrochloride group and the biological antibacterial peptide group, minocycline hydrochloride ointment and biological antibacterial peptide periodontal gel were injected into the periodontal pocket respectively. The mechanical curettage group did not take medicine. Periodontal checklists at baseline and 90 d after treatment were recorded to compare differences of the three groups in periodontal probing depth (PD), bleeding index (BI) and attachment level (AL). Enzyme-linked immunosorbent assay (ELSIA) was used to detect the change of tumour necrosis factor-α (TNF-α), interleukin (IL)-1β by collecting the gingival crevicular fluid of the three sets at baseline, 7 d after treatment and 90 d after treatment. @*Results@#There was no statistically significant difference in periodontal clinical examination indexes(PD,BI,AL) and contents of TNF-α and IL-1β in the gingival crevicular fluid between the three groups at baseline (P>0.05). At 7 and 90 d after treatment, all indexes in the three groups were improved compared with those before treatment. The comparison between groups showed that in periodontal pockets with PD≤5 mm, there was no statistically significant difference in the indicators between the three groups. In periodontal pockets with PD≥6 mm, the minocycline hydrochloride group and the bio-antibacterial peptide group had no statistically significant difference in various indicators, but they were all better than the mechanical scaling group.@*Conclusion@#Basic periodontal therapy is an important treatment for stage Ⅲ periodontitis. Minocycline hydrochloride and biological antibacterial peptides are both effective adjuvant drugs for deep periodontal pockets with PD≥6 mm.

Characterization and in vitro release of minocycline hydrochloride microspheres prepared via coacervation.

Coacervation is a commonly used method for protein and peptide drug microencapsulation using biodegradable or bioresorbable polymers. However, there is a lack of literature focused on microencapsulation of small molecule drugs using coacervation techniques. In addition, the apparatus used for this microencapsulation method has not been well-described. The objectives of the present work were to: (1) establish a reliable apparatus for coacervation microencapsulation; (2) investigate the impact of the viscosity of the silicone oil used in processing on microsphere performance; and (3) develop a reproducible in vitro release testing method for minocycline hydrochloride microspheres. Minocycline hydrochloride was chosen as the model drug and two compositionally equivalent microsphere formulations were prepared via coacervation using an in-house designed glass vessel assembly with a novel in-house customized paddle to achieve a relatively homogeneous particle size distribution. The critical physicochemical properties including drug loading, particle size, and morphology of the prepared microspheres and the commercial microspheres product (Arestin) were determined. In vitro release testing of the prepared microspheres as well as of Arestin was performed using a sample-and-separate method. The method showed good reproducibility and discriminatory ability. The physicochemical properties (such as particle size) as well as the in vitro release characteristics of the prepared microspheres were determined to be sensitive to the viscosity of the silicone oil used in coacervation processing. The silicone oil with higher viscosity (1000 cSt) used during the coacervation process resulted in smaller particle sized microspheres and consequently caused a higher initial burst release. Whereas, the silicone oil with lower viscosity resulted in larger sized microspheres with low burst release and a slower drug release rate.

A Drug Screening Reveals Minocycline Hydrochloride as a Therapeutic Option to Prevent Breast Cancer Cells Extravasation across the Blood-Brain Barrier.

Among breast cancer (BC) patients, 15-25% develop BC brain metastases (BCBM), a severe condition due to the limited therapeutic options, which points to the need for preventive strategies. We aimed to find a drug able to boost blood-brain barrier (BBB) properties and prevent BC cells (BCCs) extravasation, among PI3K, HSP90, and EGFR inhibitors and approved drugs. We used BCCs (4T1) and BBB endothelial cells (b.End5) to identify molecules with toxicity to 4T1 cells and safe for b.End5 cells. Moreover, we used those cells in mixed cultures to perform a high-throughput microscopy screening of drugs' ability to ameliorate BBB properties and prevent BCCs adhesion and migration across the endothelium, as well as to analyse miRNAs expression and release profiles. KW-2478, buparlisib, and minocycline hydrochloride (MH) promoted maximal expression of the junctional protein ß-catenin and induced 4T1 cells nucleus changes. Buparlisib and MH further decreased 4T1 adhesion. MH was the most promising in preventing 4T1 migration and BBB disruption, tumour and endothelial cytoskeleton-associated proteins modifications, and miRNA deregulation. Our data revealed MH's ability to improve BBB properties, while compromising BCCs viability and interaction with BBB endothelial cells, besides restoring miRNAs' homeostasis, paving the way for MH repurposing for BCBM prevention.

A Study on the Use of Phase Transition Lysozyme-Loaded Minocycline Hydrochloride in the Local Treatment of Chronic Periodontitis.

Periodontitis is the most important oral disease causing human tooth loss. Although supragingival and subgingival scaling is the main strategy of periodontitis clinical treatments, drug treatment has an indispensable auxiliary role to some degree. Periodontitis medical treatment is divided into systemically administered treatments and local periodontally administered treatments. Compared with systemic administration, local administration can increase local drug concentrations, reduce dosages, and prolong action times while also improving patient compliance and avoiding possible adverse effects due to systemic administration responses. However, some studies show that minocycline ointment, a clinical local drug commonly used in periodontal pockets, has an unstable release rate; 80% of the drug is usually released within 2-3 days after pocket placement. This release is not conducive to controlling periodontal infection and may hinder the periodontal tissue repair and regeneration. Therefore, choosing a suitable carrier for minocycline hydrochloride is necessary to control its local release in periodontal tissue. Phase transition lysozyme (PTL) has been widely used in many studies and the development of macromolecular carrier material, and we selected PTL as the carrier for minocycline hydrochloride drugs because of its good biocompatibility, good drug-carrying capacity, and stable release. Due to its release characteristics and simple preparation, PTL is a promising carrier material.

Effect of diode laser combined with minocycline hydrochloride in nonsurgical periodontal therapy: a randomized clinical trial.

BACKGROUND: This study aimed to assess the effect of diode laser combined with minocycline hydrochloride in conventional nonsurgical periodontal therapy. METHODS: Ninety-two patients and 1206 teeth were included in this study. The patients were diagnosed moderate or severe periodontal diseases with the presence of teeth in at least 3 quadrants in the oral cavity. Each patient's quadrants were randomly divided into three treatment groups as following, Control group: scaling and root planning (SRP); Experimental group 1 (Exp 1): SRP + minocycline hydrochloride; Experimental group 2 (Exp 2): SRP + 809 nm diode laser + minocycline hydrochloride. The minocycline in Exp 1 and Exp 2 was applied once per week, for 4 weeks. Clinical examinations including periodontal probing depth (PD), clinical attachment level (CAL) and bleeding index (BI), and the secretion of inflammatory factor (tumor necrosis factor, TNF-α) was detected by ELISA before and 3, 6 months after the treatments. The differences among these groups were assessed by One-Way ANOVA and Kruskal-Wallis test. P-value < 0.05 was considered significant. RESULTS: All the periodontal indexes (PD, CAL and BI) were improved after each treatment and the secretion of TNF-α was reduced for all three groups. In patients with deep periodontal pockets, Exp 2 showed significant improvements in all indexes comparison with Con group and Exp group 1. CONCLUSIONS: The synergistic effect of SRP and 809 nm diode laser combined with minocycline hydrochloride could play an efficient and reliable effect in the nonsurgical periodontal treatment approach. Trial registration The clinical trial was retrospectively registered in chictr.org.cn with registration ChiCTR2100051708 (01/10/2021).

Protective Effect of Minocycline Hydrochloride on the Mouse Embryonic Development Against Suboptimal Environment.

Numerous studies have reported how inner cell mass (ICM) and trophectoderm (TE) was determined during the process of early mouse embryonic development from zygotes into organized blastocysts, however, multiple mysteries still remain. It is noteworthy that pluripotent stem cells (PSCs), which are derived from embryos at different developmental stages, have identical developmental potential and molecular characteristics to their counterpart embryos. Advances of PSCs research may provide us a distinctive perspective of deciphering embryonic development mechanism. Minocycline hydrochloride (MiH), a critical component for maintaining medium of novel type of extended pluripotent stem cells, which possesses developmental potential similar to both ICM and TE, can be substituted with genetic disruption of Parp1 in our previous study. Though Parp1-deficient mouse ESCs are more susceptible to differentiate into trophoblast derivatives, what role of MiH plays in mouse preimplantation embryonic development is still a subject of concern. Here, by incubating mouse zygotes in a medium containing MiH till 100 h after fertilization, we found that MiH could slow down embryonic developmental kinetics during cleavage stage without impairing blastocyst formation potential. Olaparib and Talazoparib, two FDA approved PARP1 inhibitors, exhibited similar effects on mouse embryos, indicating the aforementioned effects of MiH were through inhibiting of PARP1. Besides, we showed an embryonic protective role of MiH against suboptimal environment including long term exposure to external environment and H2O2 treatment, which could mimic inevitable manipulation during embryo culture procedures in clinical IVF laboratory. To our knowledge, it is not only for the first time to study MiH in the field of embryo development, but also for the first time to propose MiH as a protective supplement for embryo culture, giving the way to more studies on exploring the multiple molecular mechanisms on embryonic development that might be useful in assisted reproductive technology.

Effect of minocycline hydrochloride combined with photodynamic therapy on skin barrier function of patients with acne.

OBJECTIVE: The aim of this study is to evaluate the effects of minocycline hydrochloride combined with photodynamic therapy on skin barrier function of patients with acne. METHODS: Eighty-eight acne patients admitted to our hospital were randomized into research group (n=44, photodynamic therapy on the basis of minocycline hydrochloride) and control group (n=44, minocycline hydrochloride). The clinical efficacy, skin barrier function indexes (transdermal water loss (TEWL), stratum corneum water content, pH value), scores of GAGS and Acne-QOL, cosmetic satisfaction and adverse reaction rates of the two groups were compared. RESULTS: The total effective rate of research group was higher than that of control group (P<0.05). After treatment, TEWL, cuticle water content and pH value were improved compared with those before treatment, and the research group was superior to the control group (all P<0.05). After treatment, the GAGS scores of both groups were lower than those before treatment, and the research group was lower than that of the control group (all P<0.05). The cosmetic satisfaction in the research group was higher than that in the control group (P<0.05). There was no marked difference in the incidence of adverse reactions between the two groups (P>0.05). After treatment, the quality of life scores of patients were higher than before treatment, and the research group was higher than that of the control group (all P<0.05). CONCLUSION: Minocycline hydrochloride combined with photodynamic therapy can effectively improve the skin barrier function of patients, relieve clinical symptoms, and enhance the overall efficacy and quality of life. It is also safe and patients are highly satisfied with the cosmetic effect.

Core-Shell Structured Antimicrobial Nanofiber Dressings Containing Herbal Extract and Antibiotics Combination for the Prevention of Biofilms and Promotion of Cutaneous Wound Healing.

Burn wounds are susceptible to microbial invasion from both resident and exogenous bacteria, which becomes a critical public health issue and causes substantial economic burden. There is a perceived demand to produce new antimicrobial wound dressings that hinder bacterial colonization while accelerating the healing process and hence would provide an improved standard of care for patients. Since ancient times, herbal extracts from medicinally important plants have extensively been used for treating burn injuries. This work reports the utility of electrospun nanofibers containing plant extracts and antibiotics combination as a multifunctional scaffold for treating second-degree burns. First, we determined the various components of plant extracts from Gymnema sylvestre by two different processing methods and their synergism with minocycline antibiotics. Then, we prepared core-shell nanofibrous dressings with poly-ε-caprolactone/gelatin laden with minocycline hydrochloride as a shell and gelatin infused with G. sylvestre extracts (ultrasound-assisted extracts and cold macerated extracts) as the core using coaxial electrospinning. The electrospun nanofibers displayed a smooth, continuous, and bead-free morphology with adequate wettability. The presence of extract components in the core-shell nanofibers resulted in enhanced mechanical properties when compared to pristine mats. The core-shell structures resulted in sustained release of the bioactive components when compared to nanofiber blends. Core-shell nanofiber mats containing plant extracts and antibiotic combinations displayed potent antimicrobial and antibiofilm properties while promoting the spread and proliferation of skin cells when compared to pristine mats. In a porcine model of cutaneous second-degree burns, we showed that wounds treated with the antimicrobial dressing improved re-epithelialization and collagen organization in comparison to untreated wounds.

Evaluation of the efficacy of lycopene gel compared with minocycline hydrochloride microspheres as an adjunct to nonsurgical periodontal treatment: A randomised clinical trial.

BACKGROUND/PURPOSE: The prescription of antibiotics as an adjunct to mechanical periodontal therapy in patients with severe periodontitis is recommended; however, the side effects of antibiotics are a major concern. The aim of this study was to evaluate the efficacy of lycopene (Lyc) antioxidant gel versus minocycline hydrochloride microspheres (ARISTIN) as an adjunct to the nonsurgical treatment of periodontitis. MATERIALS AND METHODS: Three identical periodontal pockets/patient received root surface debridement followed by the random application of either ARISTIN, Lyc, or placebo gel (control, Ctrl). Clinical parameters, plaque index, bleeding on probing, probing pocket depth, and clinical attachment loss, were recorded at the baseline and after 30 days. Additionally, the levels of interleukin-8 (IL-8), matrix metallopeptidase 9, and tissue inhibitor of metalloproteinases 1 (TIMP1) in gingival crevicular fluid samples were assessed at the same time points. RESULTS: Twenty-three patients with periodontitis completed the study. Both ARISTIN and Lyc treatments showed significantly greater gains in attachment (1.94 ±â€¯1.33 and 1.72 ±â€¯0.88, respectively) than the Ctrl treatment (1.04 ±â€¯0.96). Compared with those in the Ctrl, only ARISTIN showed a significant reduction in IL-8 level, whereas TIMP1 levels were significantly upregulated in the Lyc gel and ARISTIN sites. The effect size estimation indicated that Lyc gel exhibited considerably greater efficacy than the Ctrl gel. CONCLUSION: Lyc gel and ARISTIN offer almost equal improvement in both clinical and biochemical parameters of periodontitis.

Electrosprayed minocycline hydrochloride-loaded microsphere/SAIB hybrid depot for periodontitis treatment.

Minocycline hydrochloride (MINO) has been one of the most frequently used antibiotics in the treatment of periodontitis due to its antibacterial activity and osteogenesis effects; however, high levels of MINO administered during the treatment halt the formation of new bone. Therefore, the purpose of the present study was to prepare a MINO-microsphere/sucrose acetate isobutyrate (SAIB) hybrid depot to reduce the burst release of MINO and ensure antibacterial and osteogenesis effects of MINO in the treatment of periodontitis. Uniform microspheres, approximately 5 µm size, with a slightly rough surface and different MINO loading (10, 12, and 14%) were prepared, and the microspheres were added into SAIB, after which the burst release significantly decreased from 66.18 to 2.92%, from 71.82 to 3.82%, and from 73.35 to 4.45%, respectively, and the release from all the MINO-microspheres/SAIB hybrid depots lasted for 77 days. In addition, cytotoxicity test showed that the MINO-microsphere with 12% drug loading promoted the proliferation of osteoblasts the most and was subsequently used in vivo experiments. Moreover, in the model of ligatured-induced periodontitis in SD rats, the MINO-microsphere/SAIB hybrid depot not only significantly increased the alveolar bone height and bone volume but also reduced the inflammation of the periodontal tissue. Additionally, it also inhibited the expression of the receptor activator of nuclear factor-kappa B ligand (RANKL) and promoted the expression of osteoprotegerin (OPG).. These results indicated that the MINO-microsphere/SAIB hybrid depot might be promising in the treatment of periodontitis.

Minocycline Hydrochloride Controlled-release Microsphere Preparation Process Optimization Based on the Robust Design Method.

OBJECTIVES: The objective of the present study is to establish a robust preparation method that could steadily produce minocycline hydrochloride (MCH) microspheres regardless of used polymer types. MATERIALS AND METHODS: Taguchi's Robust Experimental Design methodology was employed to optimize the process parameters for MCH-loaded poly(D,L-lactide-co-glycolide) (PLGA) microspheres. In the experimental design, seven controllable factors, i.e., preparation method, pH of the aqueous phase, volume of the aqueous phase, volume of dichloromethane, rotation speed, temperature, and amount of polyvinyl alcohol, were considered for the optimization of process parameters. PLGA types with different lactide/glycolide ratios were considered the uncontrollable (noise) factor. Based on the L18 orthogonal array, 18 experimental runs were conducted for each type of PLGA. The encapsulation efficiency (EE) and in vitro release rate were evaluated for all the prepared formulations. RESULTS: Regardless of the PLGA type with different lactic/glycolic acid ratios, microspheres prepared via the solid-in-oil-in-water (S/O/W) method, showed a much higher EE and faster drug release than the microspheres prepared via the co-solvent method. Preparation methods, pH of the aqueous phase, and volume of the aqueous phase were the most influencing parameters on the EE. The confirmation experiment results indicated that the signal-to-noise ratio increased by 5.76 db from that of an initial condition. The release of minocycline was fastest with the PLGA (50:50) microspheres, followed by PLGA (75:25) and PLGA (85:15). CONCLUSION: Although the interaction between the selected factors in the evaluation was ignored, the orthogonal array design of the experiment based on Taguchi's robust experimental design methodology was sufficient to optimize the process parameters for the PLGA microspheres of MCH. The S/O/W was the main factor affecting the EE. Microspheres prepared via the S/O/W method exhibited a higher EE and faster drug release than the microspheres prepared via co-solvent method. The pH and volume of the aqueous phase were also effective parameters on the EE. A robust experimental design has been successfully applied to the optimization of the process parameters for microsphere preparation.

Preparation and properties of injectable minocycline hydrochloride microsphere depot / 中国药科大学学报

@#To prepare a minocycline hydrochloride microsphere depot and evaluate its release performance and physicochemical properties, poly (lactic-co-glycolic acid) (PLGA) was used as raw material, the minocycline hydrochloride microspheres were prepared by electrospray, and the morphology and size distribution of the microspheres were characterized by polarizing microscopy and scanning electron microscopy (SEM). The microspheres were then mixed with sucrose acetate isobutyrate (SAIB) depot at a ratio of 1:10 to form a minocycline hydrochloride microsphere depot, and its release performance and porosity changes were evaluated. The results showed that the microspheres had smooth surface and the diameter was (5.294 ± 1.222) μm. After the microspheres were added into SAIB depot, the burst release of minocycline hydrochloride significantly decreased from 60% to 3.27% at the first day, and then the release lasted for 42 days . Additionally, the porosity of the depot increased rapidly from (12.53 ± 0.43)% to (32.53 ± 0.43)% during days 0-15, and increased slowly from (32.53 ± 0.43)% to (33.81 ± 0.54)% during days 15-45. The minocycline hydrochloride microsphere depot prepared in this study is expected to be an effective way for the application of minocycline hydrochloride for its good release performance and simple preparation process.

Utility of Zinc Oxide Nanoparticles Catalytic Activity in the Electrochemical Determination of Minocycline Hydrochloride.

The current work described the synthesis and characterization of zinc oxide nanoparticles (ZnONPs) and their electrocatalytic activity in the determination of minocycline hydrochloride (MCL). The unique features of metal oxide nanoparticles such as zinc oxide encourage the researchers to investigate the activity of metal oxide nanoparticles as remarkable semiconductor materials active in the electrochemical sensing determination. Herein, the suggested study displayed a comparative determination of minocycline hydrochloride using two conventional and modified ZnONPs-coated wire sensors. The recorded results showed the linear behavior of the enriched ZnONPs sensor over the 1.0 × 10-10-1.0 × 10-2 mol L-1 with respect to 1.0 × 10-6-1.0 × 10-2 mol L-1 for the conventional sensor. The two sensors are working in the pH range of 3-5 with regression equations EmV = (53.2 ± 0.5) log [MCL] + 448.8 and EmV = (58.7 ± 0.2) log [MCL] + 617.76 for conventional and enriched ZnONPs, respectively. The correlation coefficients were 0.9995 and 0.9998 for the previously mentioned sensors, respectively. The validity of the suggested analytical method was evaluated according to the recommended guidelines for methodology and drug analysis. The developed sensors were also used in the quantification of MCL in commercial formulations.