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Screening of ionically crosslinked chitosan-tripolyphosphate microspheres using Plackett-Burman factorial design for the treatment of intrapocket infections.
Drug Dev Ind Pharm. 2017 Nov; 43(11):1801-1816.DD

Abstract

OBJECTIVE

Application of Plackett-Burman factorial design to investigate the effect of processing factors in the fabrication of ionically crosslinked chitosan-tripolyphosphate (CS-TPP) microspheres.

SIGNIFICANCE

Microspheres were screened and optimized to provide maximum process yield (PY), encapsulation efficiency (EE), and time for 80% drug release (T80%) and minimum burst and particles size (PS), for successful application in periodontitis.

METHODS

Processing factors viz. method of preparation (MOP), CS, TPP, crosslinking time (CT), agitation (AS), and drying technique (DT) were selected. Solid state characterization was performed by Fourier-Transform infrared (FTIR), differential scanning calorimetry (DSC), X-ray diffraction (XRD), and scanning electron microscopy (SEM). Mucoadhesion, cytocompatibility, and stability of microspheres were also evaluated.

RESULTS

Pareto analysis and analysis of variance, screened most significantly (p < .05) impacting process factors on selected responses. The optimized microspheres demonstrated: o/w emulsification method, CS (2.5%), TPP (5%), CT (120 min), AS (2000 rpm), and DT (freeze-dried), and provided PY- 95.67%, PS- 168.45%, EEOZ- 85.56%, EEDX- 91.34%, BOZ- 15.26%, BDX- 12.91%, TOZ- 47.09 and TDX- 67.95 minutes. FTIR illustrated compatibility between excipients and complexation of CS and TPP. XRD and DSC showed loss of crystallinity of entrapped drugs in microspheres. Biphasic drug release was observed for four days with non-Fickian kinetics. Furthermore, microspheres exhibited good mucoadhesivity (82.51%), antimicrobial activity against Staphylococcus aureus and Escherichia coli, cytocompatibility for L929 cells, and long-term stability.

CONCLUSIONS

Therefore, CS-TPP microspheres were found mucoadhesive, safe, stable and provided controlled and prolonged release of drugs. These properties confirmed its high potential and applicability in chronic periodontitis.

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Publisher Full Text

Authors+Show Affiliations

Yadav SK
a Department of Pharmaceutics , Indian Institute of Technology, Banaras Hindu University , Varanasi , Uttar Pradesh , India. b Department of Pharmacy , Moti Lal Nehru Medical College , Allahabad , Uttar Pradesh , India.
Khan G
a Department of Pharmaceutics , Indian Institute of Technology, Banaras Hindu University , Varanasi , Uttar Pradesh , India.
Bansal M
c Faculty of Dental Sciences , Institute of Medical Sciences, Banaras Hindu University , Varanasi , India.
Vardhan H
a Department of Pharmaceutics , Indian Institute of Technology, Banaras Hindu University , Varanasi , Uttar Pradesh , India.
Mishra B
a Department of Pharmaceutics , Indian Institute of Technology, Banaras Hindu University , Varanasi , Uttar Pradesh , India.

MeSH

Anti-Infective AgentsChitosanDelayed-Action PreparationsMicroscopy, Electron, ScanningMicrospheresParticle SizeSpectroscopy, Fourier Transform InfraredStaphylococcus aureusX-Ray Diffraction

Pub Type(s)

Journal Article

Language

eng

PubMed ID

28673095

Citation

Yadav, Sarita Kumari, et al. "Screening of Ionically Crosslinked Chitosan-tripolyphosphate Microspheres Using Plackett-Burman Factorial Design for the Treatment of Intrapocket Infections." Drug Development and Industrial Pharmacy, vol. 43, no. 11, 2017, pp. 1801-1816.
Yadav SK, Khan G, Bansal M, et al. Screening of ionically crosslinked chitosan-tripolyphosphate microspheres using Plackett-Burman factorial design for the treatment of intrapocket infections. Drug Dev Ind Pharm. 2017;43(11):1801-1816.
Yadav, S. K., Khan, G., Bansal, M., Vardhan, H., & Mishra, B. (2017). Screening of ionically crosslinked chitosan-tripolyphosphate microspheres using Plackett-Burman factorial design for the treatment of intrapocket infections. Drug Development and Industrial Pharmacy, 43(11), 1801-1816. https://doi.org/10.1080/03639045.2017.1349782
Yadav SK, et al. Screening of Ionically Crosslinked Chitosan-tripolyphosphate Microspheres Using Plackett-Burman Factorial Design for the Treatment of Intrapocket Infections. Drug Dev Ind Pharm. 2017;43(11):1801-1816. PubMed PMID: 28673095.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Screening of ionically crosslinked chitosan-tripolyphosphate microspheres using Plackett-Burman factorial design for the treatment of intrapocket infections. AU - Yadav,Sarita Kumari, AU - Khan,Gayasuddin, AU - Bansal,Monika, AU - Vardhan,Harsh, AU - Mishra,Brahmeshwar, Y1 - 2017/07/24/ PY - 2017/7/5/pubmed PY - 2017/10/21/medline PY - 2017/7/5/entrez KW - Chitosan KW - cytocompatibility KW - factorial design KW - microspheres KW - tripolyphosphate SP - 1801 EP - 1816 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 43 IS - 11 N2 - OBJECTIVE: Application of Plackett-Burman factorial design to investigate the effect of processing factors in the fabrication of ionically crosslinked chitosan-tripolyphosphate (CS-TPP) microspheres. SIGNIFICANCE: Microspheres were screened and optimized to provide maximum process yield (PY), encapsulation efficiency (EE), and time for 80% drug release (T80%) and minimum burst and particles size (PS), for successful application in periodontitis. METHODS: Processing factors viz. method of preparation (MOP), CS, TPP, crosslinking time (CT), agitation (AS), and drying technique (DT) were selected. Solid state characterization was performed by Fourier-Transform infrared (FTIR), differential scanning calorimetry (DSC), X-ray diffraction (XRD), and scanning electron microscopy (SEM). Mucoadhesion, cytocompatibility, and stability of microspheres were also evaluated. RESULTS: Pareto analysis and analysis of variance, screened most significantly (p < .05) impacting process factors on selected responses. The optimized microspheres demonstrated: o/w emulsification method, CS (2.5%), TPP (5%), CT (120 min), AS (2000 rpm), and DT (freeze-dried), and provided PY- 95.67%, PS- 168.45%, EEOZ- 85.56%, EEDX- 91.34%, BOZ- 15.26%, BDX- 12.91%, TOZ- 47.09 and TDX- 67.95 minutes. FTIR illustrated compatibility between excipients and complexation of CS and TPP. XRD and DSC showed loss of crystallinity of entrapped drugs in microspheres. Biphasic drug release was observed for four days with non-Fickian kinetics. Furthermore, microspheres exhibited good mucoadhesivity (82.51%), antimicrobial activity against Staphylococcus aureus and Escherichia coli, cytocompatibility for L929 cells, and long-term stability. CONCLUSIONS: Therefore, CS-TPP microspheres were found mucoadhesive, safe, stable and provided controlled and prolonged release of drugs. These properties confirmed its high potential and applicability in chronic periodontitis. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/28673095/Screening_of_ionically_crosslinked_chitosan_tripolyphosphate_microspheres_using_Plackett_Burman_factorial_design_for_the_treatment_of_intrapocket_infections_ L2 - https://www.tandfonline.com/doi/full/10.1080/03639045.2017.1349782 DB - PRIME DP - Unbound Medicine ER -