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

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Author(s): Elham Khodaverdi, Farhad Eisvand, Mohammad Sina Nezami, Seyedeh Nesa Rezaeian Shiadeh, Hossein Kamali*, Farzin Hadizadeh

Journal Name: Current Drug Delivery

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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.

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(E-pub Ahead of Print)
DOI: 10.2174/1567201817999201103195104
Price: $95

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