Rajiv gandhi university of health sciences



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6.

7.


Brief Resume of Intended Work:
6.1: Need for the Study:


  • Periodontitis is an inflammatory disease of the supporting tissue of the teeth caused by group of specific microorganisms.

  • This can be treated by conventional dosage forms, but the disadvantage associated with this is low oral bioavailability due to extensive first pass metabolism and also have potential danger of inducing resistant strains and super imposed infection.

  • Periodontitis also treated by local drug delivery appears attractive as the antimicrobial agent is delivered within the periodontal pockets.

  • The efficacy of conventional treatments of oral disease is often reduced by the limited retention of the applied formulation within the oral cavity.

  • Therefore to overcome this drawback, microspheres with bioadhesive property can be formulated which increases the residence time resulting in better bioavailability.

  • Delivery of mucoadhesive microspheres by oral route for periodontal diseases would have several advantages like better retention of formulation in periodontal pocket. The rate and extent of absorption and the plasma concentration v/s time profiles are relatively comparable to that obtained by IV administration.

  • Administration of the formulation in the form of mucoadhesive microspheres has the advantage of prolonged drug residence time, thereby reduced dosing frequency and improved patient compliance.



6.2: Review of literature

1. Abd El-Hameed MD, Kellaway IW1., Have studied the preparation and in-vitro characterization of mucoadhesive polymeric microspheres as Intranasal delivery systems. The microspheres were prepared by solvent Evaporation technique. The invitro study demonstrated that carbopol 934P adhered to the mucus to a greater extent when compared with other polymers like Chitosan, HPMC and PVA
2. Naoki Nagahara, Yohko Akiyama, Masafumi Nakoa, Mayumi Tada,

Megumi Kitano, et al2, Have prepared mucoadhesive microspheres which have the ability to reside in the gastrointestinal tract for an extended period. The microspheres contained antimicrobial agent and an adhesive polymer (carboxy vinyl polymer) powder dispersed in waxy hydrogenated castor oil. The in vivo clearance of H. pylori following oral administration of the mucoadhesive microspheres and the 0.5% methyl cellulose suspension to Infected Mongolian gerbils were examined under fed condition. They found that mucoadhesive microspheres more effectively cleared H.pylori from gastrointestinal tract than 0.5% methyl cellulose suspension due to prolonged gastrointestinal residence time resulting from mucoadhesion.


3. D. Patel, A.W. Smith, N. Grist, P. Barnett, J.D. Smart3 ., Have developed an invitro system to investigate the binding of bioadhesive macromolecules to buccal epithelial cells, without altering their physicochemical properties by the addition of ‘marker’ entities. In this innovative approach a lectin binding inhibition technique, involving an avidin-biotin complex and a colorimetric detection system, was used to evaluate polymer binding. They have found that chitosan gave the greatest inhibition of lectin binding to the surface of buccal cells, while methylcellulose, gelatin, carbopol 934P and polycarbophil also produced substantial reduction.
4. Luana Perioli, Valeria Ambrogi, Daniela Rubini, Stefano Giovangnoli , Maurizio

Ricci, et al4 ., Have prepared tablets using different mixtures of cellulose and polyacrylic derivatives in order to obtain new formulation containing metronidazole for periodontal disease treatment. The best mucoadhesive performance and best invitro drug release profile were achieved by using hydroxyl ethyl cellulose (HEC) and carbomer 940 2:2 ratios.


5. Myung-Kwan Chun , Chong-Su Cho, Hoo-Kyun Choi7., Have prepared mucoadhesive microspheres to increase gastric residence time using an interpolymer complexation of poly(acrylic acid) (PAA) with poly(vinyl pyrollidone) (PVP) , the complexation between PAA and PVP as a result of hydrogen bonding was confirmed by the shift in the carbonyl absorption bands of poly(acrylic acid) using FT-IR. They found that release rate of acetaminophen from the complex microspheres was slower than the PVP microspheres at pH 2 and 6.8 .
6. Myung-Kwan Chun, Hongku Sah, Hoo-Kyun Choi8., Have prepared mucoadhesive microspheres containing either amoxicillin or clarithromycin via the interpolymer complexation of PAA (polyacrylic acid) with PVP (polyvinyl pyrollidone) and solvent diffusion method. The release Mechanism of amoxicillin was mainly by a diffusion process and that of clarithromycin was via dissolution process. They found that the drug release rate from the complex microspheres was significantly lower than that from the PVP microspheres.
7. Sandra Kockisch, Gareth D. Rees, John Tsibouklis, John D. Smart9., They have developed mucoadhesive microspheres that can be utilized for the controlled release of triclosan in oral care formulations, specifically dental pastes, using a double emulsion solvent evaporation technique the release of triclosan from micsrospheres suspended in a non aqueous paste, was found to be sustained over considerable time- periods. The work has demonstrated that these polymeric microspheres, particularly those of chitosan, are promising candidates for the sustained release of triclosan in the oral cavity.

6.3 Main objective of the study:

The present work is an attempt,



  • To formulate a mucoadhesive microspheres containing anti bacterial agent for periodontitis.

  • Preparation of mucoadhesive microspheres

The mucoadhesive microspheres can be prepared by any one of the following methods:


  1. Solvent Evaporation method

  2. Emulsion cross linking method

  3. Solvent removal method

  4. Hydrogel microspheres

  5. O/W/O double emulsion method

  • Evaluation of the formulation consists of:

  • Physical characterization of the microspheres which includes:

  • Analysis of Particle size

  • Determination of Particle shape and

  • Surface morphology.

  • Drug entrapment efficiency

  • Percentage yield

  • In-vitro mucoadhesion

  • In-vitro release studies

  • Stability studies on the selected formulations.



Materials & Methods:
7.1 Source of the data:

The data required for the work will be collected from different books , Journals

and articles available in the Library of Govt. college of Pharmacy, Journals

available at Jgate – Helinet of the Rajiv Gandhi University of Health sciences



Website and through various internet sources.
7.2 Method of collection of data:
The data will be collected from the prepared formulation, then subjecting the formulation to different evaluation parameters like physical characterization which includes determination of particle size, particle shape and surface morphology, drug entrapment efficiency, in-vitro mucoadhesion, in-vitro drug release studies, percentage yield, stability studies on the selected formulation and other tests as necessary during the evaluation part of the formulation.
7.3 Does the study require any investigations or interventions to be

Conducted on patients or other humans or animals? If so, please

Describe in brief.

Not applicable
7.4 Has ethical clearance been obtained from your institute in case 7.3?

Not applicable.


8.

List of references:

  1. Abd El- Hameed MD, Kellaway IW., Preparation and in vitro characterization of mucoadhesive polymeric microspheres as intra nasal delivery system. European Journal of Pharmaceutics and Biopharmaceutics 1997; 44: 53-60.

  2. Naoki Nagahara, Yohko Akiyama, Masafumi Nakao, Mayumi Tada, Megumi Kitano et al., Mucoadhesive microspheres containing amoxicillin for clearance of helicobacter pylori. Antimicrobial Agents and Chemotherapy 1998; 42(10): 2492-494.

  3. D. Patel, A. W. Smith, N. Grist, P. Barnett, J.D. Smart., An in vitro mucosal model predictive of bioadhesive agents in the oral cavity. Journal of Controlled Release 1999; 61: 175-83.

  4. Luana Perioli, Valeria Ambrogi , Danelia Rubini, Stefano Giovagnoli, Maurizio Ricci, et al., Novel mucoadhesive buccal formulation containing metronidazole for the treatment of periodontal disease. Journal Of Controlled Release 2004; 95: 521-33.

  5. Marta Roldo, Margit Hornof, Paolo Caliceti, Andreas Bernkop- Schnurch., Mucoadhesive thiolated chitosans as platforms for oral controlled drug delivery: synthesis and in vitro evaluation. European Journal of Pharmaceutics and Biopharmaceutics 2004; 57: 115-21.

  6. Sanju Dhavan, Anil Kumar Single, and Ranjan Sinha., Evaluation of mucoadhesive properties of chitosan microspheres prepared by different methods. AAPS PharmSciTech 2004; 5(4): 1-7.

  7. Myung- Kwan Chun, Chong-Su Cho, Hoo-Kyun Choi., Mucoadhesive microspheres prepared by interpolymer complexation and solvent diffusion method. International Journal of Pharmaceutics 2005; 288: 295-303.

  8. Myung –Kwan Chun, Hongkee Sah, Hoo-Kyun Choi., preparation of mucoadhesive microspheres containing antimicrobial agents for eradication of H, pylori. International Journal Of Pharmaceutics 2005; 297: 172-79

  9. Sandra Kockisch, Gareth D. Rees, John Tsibouklis, John D. Smart., Mucoadhesive , triclosan-loaded polymer microspheres for application to the oral cavity: preparation and controlled release characteristics.

European Journal of Pharmaceutics and Biopharmaceutics 2005; 59: 207-16.

  1. Sakchai Wittaya-Areekul, Jittiporn Kruenate, Chureerat Prahsarn., Preparation and in vitro evaluation of mucoadhesive properties of alginate/chitosan microparticles containing prednisolone. International Journal of Pharmaceutics 2006; 312: 113-18.

  2. Amal Hassan El-Kamel, Lubna Y. Ashri, Ibrahim A. Alsarra., Micromatricial metronidazole benzoate film as a local mucoadhesive delivery for treatment of periodontal disease. AAPS PharmSciTech 2007; 8(3): E1-E11.




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