دورية أكاديمية

PLGA-modified Syloid ® -based microparticles for the ocular delivery of terconazole: in-vitro and in-vivo investigations.

التفاصيل البيبلوغرافية
العنوان: PLGA-modified Syloid ® -based microparticles for the ocular delivery of terconazole: in-vitro and in-vivo investigations.
المؤلفون: Zaghloul N; Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Future University in Egypt, Cairo, Egypt., Mahmoud AA; Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Future University in Egypt, Cairo, Egypt., Elkasabgy NA; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt., El Hoffy NM; Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Future University in Egypt, Cairo, Egypt.
المصدر: Drug delivery [Drug Deliv] 2022 Dec; Vol. 29 (1), pp. 2117-2129.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: Taylor & Francis Country of Publication: England NLM ID: 9417471 Publication Model: Print Cited Medium: Internet ISSN: 1521-0464 (Electronic) Linking ISSN: 10717544 NLM ISO Abbreviation: Drug Deliv Subsets: MEDLINE
أسماء مطبوعة: Publication: 2015->: Abingdon, Oxford : Taylor & Francis
Original Publication: Orlando, FL : Academic Press, c1993-
مواضيع طبية MeSH: Lactic Acid* , Polyglycolic Acid*, Animals ; Drug Carriers ; Male ; Microspheres ; Particle Size ; Polylactic Acid-Polyglycolic Acid Copolymer ; Rabbits ; Triazoles
مستخلص: The eye is an invulnerable organ with intrinsic anatomical and physiological barriers, hindering the development of a pioneer ocular formulation. The aim of this work was to develop an efficient ocular delivery system that can augment the ocular bioavailability of the antifungal drug, terconazole. Mesoporous silica microparticles, Syloid ® 244 FP were utilized as the carrier system for terconazole. Preliminary studies were carried out using different drug:Syloid ® weight ratios. The optimum weight ratio was mixed with various concentrations (30 and 60%w/w) of poly (lactic-co-glycolic acid) (PLGA), ester or acid-capped and with different monomers-ratio (50:50 and 75:25) using the nano-spray dryer. Results revealed the superiority of drug:Syloid ® weight ratio of 1:2 in terms of yield percentage (Y%), SPAN and drug content percentage (DC%). Furthermore, incorporation of PLGA with lower glycolic acid monomer-ratio significantly increased Y%. In contrast, increasing the glycolic acid monomer-ratio resulted in higher DC% and release efficiency percentage (RE%). Additionally, doubling PLGA concentration significantly reduced Y%, DC%, drug loading percentage (DL%) and RE%. Applying desirability function in terms of increasing DC%, DL% besides RE% and decreasing SPAN, the selected formulation was chosen for DSC, XRD and SEM investigations. Results confirmed the successful loading of amorphized terconazole on PLGA-modified Syloid ® microparticles. Moreover, pharmacokinetic studies for the chosen formulation on male Albino rabbits' eyes revealed a 2, 6.7 and 25.3-fold increase in mean residence time, C max and AUC 0-24 -values, respectively, compared to the drug suspension. PLGA-modified Syloid ® microparticles represent a potential option to augment the bioavailability of ocular drugs.
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فهرسة مساهمة: Keywords: Mesoporous silica; Ocular delivery; PLGA; Syloid®; Terconazole
المشرفين على المادة: 0 (Drug Carriers)
0 (Triazoles)
0KJ2VE664U (terconazole)
1SIA8062RS (Polylactic Acid-Polyglycolic Acid Copolymer)
26009-03-0 (Polyglycolic Acid)
33X04XA5AT (Lactic Acid)
تواريخ الأحداث: Date Created: 20220715 Date Completed: 20220719 Latest Revision: 20220720
رمز التحديث: 20231215
مُعرف محوري في PubMed: PMC9291711
DOI: 10.1080/10717544.2022.2092239
PMID: 35838555
قاعدة البيانات: MEDLINE
الوصف
تدمد:1521-0464
DOI:10.1080/10717544.2022.2092239