Targeted retentive device for oro-dental infections: formulation and development

Int J Pharm. 2003 Jun 18;259(1-2):47-55. doi: 10.1016/s0378-5173(03)00204-7.

Abstract

Fibers loaded with amoxycillin trihydrate were prepared for oro-dental infections using melt spinning technique. Ethylene vinyl acetate, a biocompatible polymer was used for providing controlled release effect over a period of several days. The fibers were evaluated for in vitro release in alkaline borate buffer pH 8.1 in a biological shaker which was rotated at 50 rpm at 37 degrees C. In situ studies were carried out in continuous flow through apparatus which simulated the conditions of periodontal pocket. Microbiological evaluation was carried out on strains commonly implicated in oro-dental infections namely S. aureus, S. mutans, and Bacteroides cereus. Results of in vitro release studies revealed that the effect was sustained over a period of 6 days and followed Fickian diffusion mechanism. In situ release study samples were well above the minimum inhibitory concentration of the drug. These samples were effective in inhibiting the growth of the above-mentioned strains. The optimized formulation was characterized for general appearance, content uniformity, and SEM. Stability studies carried out on the formulation showed the degradation rate constant value of 2.79 x 10(-4) per day. Retentive fibers were found to be very effective in controlled delivery of amoxycillin, and hence can be feasible alternative to systemic administration.

MeSH terms

  • Amoxicillin / administration & dosage*
  • Amoxicillin / chemistry
  • Amoxicillin / metabolism
  • Amoxicillin / pharmacology
  • Animals
  • Bacterial Infections / drug therapy
  • Bacteroides / drug effects
  • Cattle
  • Colony Count, Microbial
  • Drug Delivery Systems
  • Drug Stability
  • Escherichia coli / drug effects
  • In Vitro Techniques
  • Kinetics
  • Microscopy, Electron, Scanning
  • Mouth Mucosa / metabolism
  • Penicillins / administration & dosage*
  • Penicillins / chemistry
  • Penicillins / metabolism
  • Penicillins / pharmacology
  • Periodontal Diseases / drug therapy
  • Periodontal Diseases / microbiology
  • Permeability
  • Polyvinyls / chemistry*
  • Solubility
  • Staphylococcus / drug effects
  • Temperature

Substances

  • Penicillins
  • Polyvinyls
  • ethylenevinylacetate copolymer
  • Amoxicillin