Abstract

 
 
 
 Purpose: To design parenteral in-situ gel of ceftriaxone using poloxamer as a thermosensitive agent, Carbopol as a pH-sensitive polymer and hydroxypropyl methylcellulose as a viscosity enhancer.
 Method: Lyophilized ceftriaxone was added in solution form to enhance its solubility and stability. Several formulations were designed using poloxamer (P 188, F 127 and P 407) and Carbopol (934P and 940) in varying concentrations, out of which an optimized formulation was chosen on the basis of its gelling capacity and respective transit time. Drug content uniformity, sterility and stability were studied. Drug-polymer and polymer-polymer interaction were determined by differential scanning calorimetry (DSC). Characterization of optimized formulation was carried out by Fourier transform infrared spectroscopy (FTIR). In-vitro release profile was determined by a modified Franz diffusion method.
 Results: Optimized formulation Q2 was characterized for various physicochemical parameters and found to be stable. In-vitro release study showed first order release pattern. DSC thermograms revealed that the polymers were compatible with each other as no physicochemical interactions were observed. The results were expressed as mean ± standard deviation (SD, p ≤ 0.05).
 Conclusion: Optimized formulation Q2 provided sustained release up to 10 days following first order release kinetics, and thus can be further developed for large-scale production.
 
 
 
Highlights
Bacterial meningitis caused by Streptococcus pneumoniae, enters the subarachnoid space causing inflammation not restricting to meninges only and spreads into brain and spinal cord
Treatment strategy for bacterial meningitis include ceftriaxone monotherapy or in combination with corticosteroids that might continue up to 10-14 days or extending up to 3-4 weeks depending on severity of condition [1]
Fourier transform infrared spectroscopy (FTIR) peaks of in-situ gel of ceftriaxone were comparable to active pharmaceutical ingredient (Figure 1 A)
Summary
Bacterial meningitis caused by Streptococcus pneumoniae, enters the subarachnoid space causing inflammation not restricting to meninges only and spreads into brain and spinal cord. These formulations were tested for their compatibility with ceftriaxone, gelling capacity and respective transit time. Formulation Q2 (PVA 15%, Carbopol 934P 1%, HPMC K15-M 20% and Poloxamer P 407 15%) formed optimized gel prolonged transit time. In vitro release study was determined using modified Franz diffusion cell (EMFDC 06) and UV-visible spectrophotometer (UV-1601) Donor compartment was filled with gel formulation, and recipient compartment with immersed magnetic stirrer was filled with phosphate buffer pH 6. Significant differences were determined using one-way ANOVA with p 0.05 considered statistically significant
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