Dataset Information

Preparation and Evaluation of Topically Applied Azithromycin Based on Sodium Hyaluronate in Treatment of Conjunctivitis.

ABSTRACT: Azithromycin (AZI) eye drops containing sodium hyaluronate (SH) were developed to improve the bioavailability of AZI. Interaction between AZI and SH in the AZI-SH formulation was investigated by differential scanning calorimetry, X-ray diffraction, and ¹H-nuclear magnetic resonance spectroscopy analyses. Moreover, advantages of using SH as an excipient were investigated by comparing physiological properties and pharmacokinetic behaviors of SH-containing AZI eye drops with that of hydroxypropyl methylcellulose (HPMC)-containing formulation. In addition, safety of the developed AZI-SH eye drops was evaluated by in vitro 3-(4,5-dimethyl-2-Thiazyl)-2, 5-diphenyl-2H-tetrazolium bromide assay (MTT assay) and neutral red uptake assay as well as in vivo eye irritation test and acute toxicity test. The results indicated that AZI formed a complex with SH under a slightly acidic condition. The area under the curve (AUC) of AZI in SH-containing formulation was 1.58-fold higher (P<0.01) than that in HPMC-containing formulation due to the interaction between the amine group of AZI and the carboxyl group of SH, despite of the higher viscosity of HPMC-containing formulation. Safety evaluation showed that AZI-SH eye drops caused no obvious eye irritation and acute toxicity. In conclusion, the developed SH-containing AZI formulation possessing advantages of longer retention time and higher drug availability was a promising drug formulation for topical ocular therapy.

SUBMITTER: Chen Q

PROVIDER: S-EPMC6523157 | biostudies-literature | 2019 Apr

REPOSITORIES: biostudies-literature

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Preparation and Evaluation of Topically Applied Azithromycin Based on Sodium Hyaluronate in Treatment of Conjunctivitis.

Chen Qian Q Yin Chun C Ma Jiang J Tu Jiasheng J Shen Yan Y

Pharmaceutics 20190415 4

Azithromycin (AZI) eye drops containing sodium hyaluronate (SH) were developed to improve the bioavailability of AZI. Interaction between AZI and SH in the AZI-SH formulation was investigated by differential scanning calorimetry, X-ray diffraction, and ¹H-nuclear magnetic resonance spectroscopy analyses. Moreover, advantages of using SH as an excipient were investigated by comparing physiological properties and pharmacokinetic behaviors of SH-containing AZI eye drops with that of hydroxypropyl m ...[more]

PMID: 30991749

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Project description:BACKGROUND/AIM:We aimed to explore the roles of glycoproteins glycosylation in the pathogenesis of Kashin-Beck disease (KBD) and evaluated the effectiveness of sodium hyaluronate treatment. MATERIALS AND METHODS:Blood and saliva were collected from KBD patients before and after the injection of sodium hyaluronate. Normal healthy subjects were included as controls. Saliva and serum lectin microarrays and saliva and serum microarray verifications were used to screen and confirm the differences in lectin levels among the three groups. RESULTS:In saliva lectin microarray, bindings to Sophora Japonica Agglutinin (SJA), Griffonia (Bandeiraea) Simplicifolia Lectin I (GSL-I), Griffonia (Bandeiraea) Simplicifolia Lectin I (EEL), Maackia Amurensis Lectin II (MAL-II), Sambucus Nigra Lectin (SNA), Hippeastrum Hybrid Lectin (HHL) and Aleuria Aurantia Lectin (AAL) were higher in the untreated KBD patients than in the control group. Increased levels for HHL, MAL-II and GSL-I in the untreated KBD patients discriminated them in particular from the treated ones. Jacalin was lower in the untreated KBD patients compared to the treated KBD and the normal groups. In serum lectin microarray, HHL and Peanut Agglutinin (PNA) were increased in the untreated KBD group in comparison to the control one. AAL, Phaseolus vulgaris Agglutinin(E+L) (PHA-E+L) and PsophocarpusTetragonolobus Lectin I (PTL-I) were lower in the untreated KBD patients compared to the treated KBD and the normal groups. Hyaluronate treatment appeared to normalize SNA, AAL and MAL-II levels in saliva, and HHL, PNA, AAL, PTL-I and PHA-E+L levels in serum. Saliva reversed microarray verification confirmed significant differences between groups in SNA and Jacalin, in particular, GSL-I levels, while serum reversed microarray verification indicated that HHL, PNA and AAL levels returned to normal level after the hyaluronate treatment. Lectin blot confirmed significant differences in HHL, AAL and Jaclin in saliva, and HHL, PNA, PHA-E+L and AAL in serum. CONCLUSION:HHL in saliva and serum may be valuable diagnostic biomarker of KBD, and it may be used to follow-up of the hyaluronate treatment.

Project description:Background:Recent artificial tear preparations have provided 0.2% concentration of sodium hyaluronate. However, no published data exist on their potential superiority against 0.1% in alleviating dry-eye-disease symptoms in cataract extraction surgery. Methods:A total of 180 patients that underwent cataract extraction surgery were randomly divided into 2 groups according to their postoperative regime: Study group (SG) received fixed combination of tobramycin and dexamethasone (FCTD) quid for 3?weeks, and additionally 0.2% sodium hyaluronate provided in the COMOD® device quid for 6?weeks. Control group (CG) received fixed combination of tobramycin and dexamethasone (FCTD) quid for 3?weeks, and additionally 0.1% sodium hyaluronate provided in the COMOD® device quid for 6?weeks. The following indexes were evaluated at 3 postoperative checkpoints: 1) Surface discomfort index (SDI) which was derived by four direct 10-scale Likert-type questions that were addressed to the patient and pertained to: a) foreign body sensation (FBS), b) blinking discomfort (BD), c) stinging sensation (SS), d) tearing sensation (TS), 2) Tear break-up time (TBUT), 3) Schirmer's test, 4) Central corneal thickness (CCT), and 4) Central Corneal Sensitivity (CCS). Results:Both groups showed reduced CCS values at all postoperative examination points; however, SG participants had significantly better CCS (all p <?0.05). SG had better TBUT than CG at the 3rd (p =?0.03) and 6th examination points (p =?0.04). Moreover, SG had better SDI scores at the 3rd (SDI?=?9.26?±?0.55) and 6th weeks (SDI?=?9.47?±?0.48) vs. CG participants (p =?0.03 and p <?0.01, respectively). Conclusion:The increased 0.2% sodium hyaluronate concentration in the artificial tears provided in the COMOD® device seems to address dry-eye-disease symptoms better in patients who underwent phacoemulsification surgery than the 0.1% concentration. Trial registration:ClinicalTrials.gov Identifier: NCT03705949 Oct 15, 2018, retrospectively registered.

Dataset Information

Preparation and Evaluation of Topically Applied Azithromycin Based on Sodium Hyaluronate in Treatment of Conjunctivitis.

Publications

Preparation and Evaluation of Topically Applied Azithromycin Based on Sodium Hyaluronate in Treatment of Conjunctivitis.

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