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Injectable In-situ Forming Depot of Doxycycline Hyclate/α-cyclodextrin Complex Using PLGA for Periodontitis Treatment: Preparation, Characterization, and In-vitro Evaluation

Author(s):

Elham Khodaverdi, Farhad Eisvand, Mohammad Sina Nezami, Seyedeh Nesa Rezaeian Shiadeh, Hossein Kamali* and Farzin Hadizadeh   Pages 1 - 12 ( 12 )

Abstract:


Background: Doxycycline (DOX) is used in treating a bacterial infection, especially for periodontitis treatment. Objective: To reduce irritation of DOX for subgingival administration and increase the chemical stability and against enzy-matic, the complex of α-cyclodextrin with DOX was prepared and loaded into injectable in situ forming implant based on PLGA.

Methods: FTIR, molecular docking studies, X-ray diffraction, and differential scanning calorimetry was performed to char-acterize the DOX/α-cyclodextrin complex. Finally, the in-vitro drug release and modeling, morphological properties, and cellular cytotoxic effects were also evaluated.

Results: The stability of DOX was improved with complex than pure DOX. The main advantage of the complex is the al-most complete release (96.31 ± 2.56 %) of the drug within 14 days of the implant, whereas in the formulation containing the pure DOX and the physical mixture the DOX with α-cyclodextrin release is reached to 70.18 ± 3.61 % and 77.03 ± 3.56 %, respectively. This trend is due to elevate of DOX stability in the DOX/ α-cyclodextrin complex form within PLGA implant that confirmed by the results of stability.

Conclusion: Our results were indicative that the formulation containing DOX/α-cyclodextrin complex was biocompatible and sustained-release with minimum initial burst release.

Keywords:

Doxycycline hyclate, α-cyclodextrin, Complex, Initial burst release, In-situ implant.Doxycycline hyclate, α-cyclodextrin, Complex, Initial burst release, In-situ implant.

Affiliation:

Targeted Drug Delivery Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sci-ences, Mashhad,, Department of Pharmacodynamics and Toxicology, School of Pharmacy, Mashhad University of Medi-cal Sciences, Mashhad,, Department of Pharmaceutics, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad,, Department of Pharmaceutics, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad,, Targeted Drug Delivery Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sci-ences, Mashhad,, Department of Medicinal Chemistry, School of Pharmacy, Mashhad Universi-ty of Medical Sciences, Mashhad



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