Browsing by Author "Gayasuddin Khan"

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Design, optimization and characterizations of chitosan fortified calcium alginate microspheres for the controlled delivery of dual drugs
(Taylor and Francis Ltd., 2018) Sarita Kumari Yadav; Gayasuddin Khan; Gunjan Vasant Bonde; Monika Bansal; Brahmeshwar Mishra
Periodontal disease is chronic, highly prevalent infectious disease that requires prolonged and controlled delivery of antimicrobial agents into pockets. To achieve this objective, dual antimicrobials encapsulated chitosan fortified calcium alginate (CS-Ca-SA) microspheres were formulated by application of Plackett-Burman factorial design. The microspheres were optimized for particle size (PS), entrapment efficiency (EE) and drug release. The optimized microspheres presented average PS of 74–461 µm and EE of 62.45–86.20% with controlled drug delivery for 120 hours. FTIR disclosed successful complexation between SA and CS. DSC and XRD studies showed changes in the crystallinity of drugs in microspheres. Shape factor and SEM demonstrated spherical to pear-shaped microspheres. Release exponent >0.43 and high diffusion coefficients revealed non-Fickian-based diffusion-limited drug release. CS-Ca-SA microspheres exhibited surface pH of 6.5 ± 0.5, moderate swelling, less erosion and improved mucoadhesion over Ca-SA microspheres. Also, significant antimicrobial activity against Escherichia coli and Staphylococcus aureus and cytocompatibility with L929 cell lines were observed. Further, microspheres exhibited long-term stability on refrigeration. The outcomes of study supported the potential of dual polymer and dual drug-based biodegradable, stable, non-toxic, mucoadhesive, controlled and prolonged drug release microspheres as more patient compliant by administration into periodontal pockets for the management of periodontal disease. © 2017 Informa UK Limited, trading as Taylor & Francis Group.
Development and Evaluation of Biodegradable Chitosan Films of Metronidazole and Levofloxacin for the Management of Periodontitis
(Springer New York LLC, 2016) Gayasuddin Khan; Sarita K. Yadav; Ravi R. Patel; Gopal Nath; Monika Bansal; Brahmeshwar Mishra
Metronidazole (MZ) and levofloxacin (LF) are widely employed for treatment of periodontitis, but high oral dose and resistance development after long-term oral administration limit their use. The aim of this study was to alleviate shortcomings in the treatment of periodontitis by fabrication of intrapocket, biodegradable films of chitosan (CS) loaded with MZ and LF meant for inserting into periodontal pockets to treat infections. The films were developed by solvent casting technique using propylene glycol as plasticizer and glutaraldehyde as crosslinking agent. Their physical characteristics, such as drug content, surface pH, swelling index, and folding endurance, exhibited results within limit. Further, FTIR and DSC studies revealed stability of films and compatibility between drugs and excipients. SEM images of films showed the presence of free drug particles on the surface causing burst effect. In vitro release in McIlvaine buffer pH 6.6 was of sustained nature assisted by the burst effect. CS and crosslinking agent concentrations negatively affected drug release and positively affected T90 (time for releasing 90% of the drug) due to altered matrix density. In contrast, the plasticizer concentration increases membrane permeability and hence increased drug release, lowering T90. Crosslinked films demonstrated sustained release up to 7 days. The antibacterial efficacy of films was tested on Staphylococcus aureus and Escherichia coli, indicating good antibacterial activity. Clinical trials on patients proved the therapeutic efficacy of the films by a significant (p < 0.05) decrease in the clinical markers of periodontitis, i.e. gingival index, plaque index and pocket depth. Conclusively, the films of MZ and LF were successful tools for the management of periodontitis. © 2015, American Association of Pharmaceutical Scientists.
Development, optimization and evaluation of curcumin loaded biodegradable crosslinked gelatin film for the effective treatment of periodontitis
(Taylor and Francis Ltd., 2018) Sheetal Chauhan; Monika Bansal; Gayasuddin Khan; Sarita K. Yadav; Ashish K. Singh; Pradyot Prakash; Brahmeshwar Mishra
Objective: Aim of the present study was to prepare curcumin (CUR) loaded biodegradable crosslinked gelatin (GE) film to alleviate the existing shortcomings in the treatment of periodontitis. Significance: Gelatin film was optimized to provide anticipated mucoadhesive strength, mechanical properties, folding endurance, and prolonged drug release over treatment duration, for successful application in the periodontitis. Methods: The film was developed by using solvent casting technique and “Design of Experiments” approach was employed for evaluating the influence of independent variables on dependent response variables. Solid-state characterization of the film was performed by FTIR, XRD, and SEM. Further, prepared formulations were evaluated for drug content uniformity, surface pH, folding endurance, swelling index, mechanical strength, mucoadhesive strength, in vitro biodegradation, and in vitro drug release behavior. Results: Solid state characterization of the formulation showed that CUR is physico-chemically compatible with other excipients and CUR was entrapped in an amorphous form inside the smooth and uniform film. The optimized film showed degree of crosslinking 51.04 ± 2.4, swelling index 138.10 ± 1.25, and folding endurance 270 ± 3 with surface pH around 7.0. Crosslinker concentrations positively affected swelling index and biodegradation of film due to altered matrix density of the polymer. Results of in vitro drug release demonstrated the capability of the developed film for efficiently delivering CUR in a sustained manner up to 7 days. Conclusions: The developed optimized film could be considered as a promising delivery strategy to administer medicament locally into the periodontal pockets for the safe and efficient management of periodontitis. © 2018 Informa UK Limited, trading as Taylor & Francis Group.
Multiparticulate based thermosensitive intra-pocket forming implants for better treatment of bacterial infections in periodontitis
(Elsevier B.V., 2018) Sarita Kumari Yadav; Gayasuddin Khan; Monika Bansal; Sathish Thokala; Gunjan Vasant Bonde; Mansi Upadhyay; Brahmeshwar Mishra
Considering alarming projections in the prevalence of periodontitis, following study was undertaken to develop chitosan-vanillin crosslinked microspheres loaded in-situ gel (MLIG) implants containing ornidazole and doxycycline hyclate for the treatment of pocket infections. Firstly, microspheres were formulated and optimized using response surface methodology for particle size <50 μm, entrapment efficiency >80%, in-vitro drug release (T80%) >7 days and acceptable mucoadhesion. Further, MLIG were optimized for gelation temperature of 34–37 °C and viscosity <1000 cps respectively. FTIR, DSC and XRD graphs disclosed compatibility and alterations in crystallinity of drugs. In-vitro dissolution study demonstrated non-Fickian type of drug release mechanism for twelve days. Stability studies ascertained MLIG implants were sterilizable and stable for about 11.29 months on refrigeration. The formulations exhibited significant (p < 0.001) antimicrobial activity against Staphylococcus aureus, Escherichia coli, and Enterococcus faecalis, and were found biocompatible and biodegradable during preclinical studies. Ligature-induced periodontal rat model, corroborated significant growth (p < 0.05) of gingival tissue after two weeks. Clinical trials revealed, intra-pocket administration of MLIG along with SRP provided significant reduction in clinical parameters as compared to SRP alone. Conclusively, antimicrobials incorporated thermosensitive, biodegradable, mucoadhesive and syringeable MLIG implants appeared as better option for the treatment of periodontitis. © 2017
Periodontal thermoresponsive, mucoadhesive dual antimicrobial loaded in-situ gel for the treatment of periodontal disease: Preparation, in-vitro characterization and antimicrobial study
(Elsevier B.V., 2018) Monika Bansal; Neelam Mittal; Sarita Kumari Yadav; Gayasuddin Khan; Pooja Gupta; Brahmeshwar Mishra; Gopal Nath
Background: This study aimed to formulate and characterize in-situ gel containing levofloxacin and metronidazole to release drugs in controlled manner for treatment of periodontitis. Material and Methods: Medicated in-situ gel with levofloxacin (10% w/v), metronidazole (25% w/v) and vehicle in-situ gel without drugs having poloxamer 407 (20% w/v) and chitosan (0.5%, 1%, 1.5%, 2.0% 2.5% w/v) were prepared and characterized for physicochemical, mechanical properties, stability and in-vitro drug release. Fourier transform infrared spectroscopy and differential scanning calorimetery studies were done. Optimized formulation was evaluated by scanning electron microscope (SEM) and in-vitro antimicrobial activity against 5 bacterial strains. Results: The results revealed that drugs and polymers were compatible to formulate. All formulations were light yellow, clear and syringeable except formulation having 2.5% w/v chitosan. pH was in the range of 6.20 to 6.74. 1.0% w/v and 1.5% w/v chitosan formulations showed gelation temperature 37 ± 0.32 °C and 34 ± 0.21 °C. Further, mucoadhesive strength indicated mucoadhesivity of gel. In-vitro release study of 1.5% w/v chitosan formulation showed initial burst where about 55–60% MZ and 60–70% LVF got released within 6–7 hrs followed by sustained release upto 48 hrs. SEM images of 1.5% w/v chitosan optimized medicated in-situ and vehicle in-situ gel appeared similar indicating homogeneous mixing of polymers with drugs. In-vitro antimicrobial study showed that medicated in-situ gel was more effective than vehicle. Conclusions: In conclusion, optimized 1.5% w/v chitosan in-situ gel was thermoresponsive, mucoadhesive, syringeable, and released drugs in slow and controlled manner with effectiveness against broad range of microbes. © 2017 Craniofacial Research Foundation
Screening of ionically crosslinked chitosan-tripolyphosphate microspheres using Plackett–Burman factorial design for the treatment of intrapocket infections
(Taylor and Francis Ltd., 2017) Sarita Kumari Yadav; Gayasuddin Khan; Monika Bansal; Harsh Vardhan; Brahmeshwar Mishra
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. © 2017 Informa UK Limited, trading as Taylor & Francis Group.
Tinidazole functionalized homogeneous electrospun chitosan/poly (ε-caprolactone) hybrid nanofiber membrane: Development, optimization and its clinical implications
(Elsevier B.V., 2017) Gayasuddin Khan; Sarita K. Yadav; Ravi R. Patel; Nagendra Kumar; Monika Bansal; Brahmeshwar Mishra
We have prepared tinidazole (TNZ) functionalized biodegradable chitosan (CH)/poly (ε-caprolactone) (PCL) mucoadhesive hybrid nanofiber membrane (TNZ-PCHNF) to alleviate existing shortcomings in treatment of periodontitis. Box-Behnken design was employed for evaluating influence of formulation and processing variables on quality of final formulation. Optimized nanofiber membrane was subjected to solid-state and surface characterization studies using FTIR, DSC, XRD, SEM and AFM, which revealed that TNZ was entrapped in an amorphous form inside smooth and uniform cylindrical nanofibers without any physicochemical interaction with excipients. The optimized TNZ-PCHNF membrane had a diameter of 143.55 ± 8.5 nm and entrapment efficiency of 83.25 ± 1.8%. In vitro drug release and antibacterial study demonstrated capability of the developed nanofiber membranes for efficiently delivering TNZ in a sustained manner up to 18 days, and its ability to inhibit bacterial growth, respectively. Further, reduction of contact angle (from 123.4 ± 2.5 to 27.4 ± 2.3) revealed that blending of CH with PCL increases hydrophilicity of the nanofiber membrane. MTT assay and CLSM study suggested that nanofiber membrane was devoid of cytotoxicity on mouse fibroblasts. Moreover, preliminary clinical trials on patients proved therapeutic efficacy of the nanofiber membrane by eliciting a significant (p < 0.05) decrease in clinical markers of periodontitis. © 2017 Elsevier B.V.