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[Display omitted] • A spectrophotometric method to quantify chloramphenicol (CHL) was developed. • The analytical method was validated according to ICH guidelines. • Formulation of dissolving microneedle (DMN) loaded microparticles CHL was developed. • Validated method was applied in in vitro release study of microparticles CHL. • The validated method was applied in ex vivo dermatokinetic study of DMN. Cellulitis is a common dermis/subcutaneous tissue skin infection and shared global disease burden, with a higher incidence for males and people aged 45–64 years. Application therapy of chloramphenicol (CHL) has been hindered because of its toxicity and limited penetration into the skin. In this research, CHL was developed into a bacterially sensitive microparticles which were further incorporated into a microneedle system to increase penetration. To support this formulation, in this study, UV–vis spectrophotometry method was validated in methanol, polyvinyl alcohol (PVA) 1%, phosphate buffered saline (PBS), tryptic soy broth (TSB) (fluid-mimicking infection), and skin tissue to quantify amount of CHL. The developed analytical method was subsequently validated according to ICH guidelines. The results obtained showed that the correlation coefficients were linear ≥0.9934. The values of LLOQ inside the methanol, PVA 1%, PBS, TSB, and skin tissue were 7.20 µg/mL, 4.40 µg/mL, 8.18 µg/mL, 387.48 µg/mL, and 7.27 µg/mL, respectively. The accuracy and precision of the developed method were prominent. These methods were successfully applied to quantify the amount of CHL in microparticle and microneedle system in fluid and tissue skin infection. The result showed the high drug release microparticle sensitive bacteria, and high drug retention in ex vivo dermatokinetic evaluation in rat skin tissue containing bacterial infection. This was due to the presence of Staphylococcus aureus bacteria culture that produced lipase enzymes, playing a role in lysing microparticle matrix to develop selectively delivery antimicrobials. A further analytical method needs to be matured to quantify CHL inside the in vivo studies. [ABSTRACT FROM AUTHOR]