In current research work, locally grown citrus wastes (peel and bagasse) were characterized through compositional analysis followed by preparation of citrus waste enriched fruit leather. After that, biokinetic trial was carried out to evaluate the prophylatic potential of citrus waste with special reference to hypercholesterolemia and hyperglycemia on Sprague Dawley rats. In this context, chemical analysis proved that citrus peel is an excellent source of inorganic matter. Regarding the phytochemical profiling, citrus peel as well as bagasse showed highest activity in methanol extract followed by ethanol and water. On the other hand grapefruit peel and bagasse proved to have maximum polyphenols followed by oranges and musami. The methanolic extract of grapefruit peel showed maximum values of TPC 206.53±6.82 mg GAE/ 100 g, Flavonoids 83.06±2.74 mg QE/100 g, DPPH 62.80±2.07%, antioxidant activity 58.13±1.92%, ABTS 10.35±0.34 µmole TE/g, iron chelation 18.54±0.61%, superoxide anion 34.62±1.14% and hydrogen peroxide 55.90±1.84%. The same trend was observed in the methanolic extract of grapefruit bagasse. Furthermore, the bioactive entities, hesperidin and nobiletin quantified through HPLC showed maximum hesperidin in methanolic extract of grapefruit peel and bagasse i.e. 28.51 and 7.40 mg/g in peel and bagasse respectively. Similarly, the nobiletin was maximum 9.92 mg/g in methanolic extract of grapefruit peel and 2.78 mg/g in methanolic extract of grapefruit bagasse. On the basis of in vitro analyses and HPLC quantification methanolic extract of grapefruit peel and bagasse were selected for the preparation of citrus enriched fruit leather that was further used in bio-efficacy trail. Accordingly two types of fruit leathers were prepared using methanolic extract of citrus peel and bagasse @ 5% against control. The prepared fruit leather was assessed for physico-chemical analysis, antioxidant activity and sensory evaluation on monthly basis during storage of four months. During storage interval pH, acidity, TPC and DPPH changed significantly however, all other parameters changed non-momentously. The hedonic response of citrus enriched fruit leather showed that the best results were obtained by T1 (fruit leather with 5% grapefruit peel extract) followed by T2 (fruit leather with 5% grapefruit bagasse extract) and T0 (control fruit leather). After that, the valuation of hesperidin was evaluated by the biokinetic trial of experimental rat modeling. The biokinetic study was comprised of three studies i.e. normal study (study 1) fed on chow diet, hypercholesterolemic study (study II) fed on chow diet with 1.5% cholesterol and hyperglycemic study (study III) feeding on chow diet with 40% sucrose. All the studies were further divided into three groups categorized on the basis of diet. 1st group fed on control fruit leather, 2nd on fruit leather prepared with 5% grapefruit peel extract and 3rd on fruit leather prepared with 5% grapefruit bagasse extract. During the 60 days efficacy trials, the feed intake & drink intakes along with body weight changed significantly. Moreover, in hypercholesterolemic study (study II) the cholesterol level decreased momentously as 14.42% and 10.65% by grapefruit peel extract (T1) and grapefruit bagasse extract enriched fruit leather (T2). Likewise, the LDL level was 60.62±2.24 mg/dL in control group that reduced to 51.93±1.92 in T1 and 54.05±2.00 mg/dL in T2. Moreover, the grapefruit waste impart non-significant effect on HDL however, triglycerides level decreased 11.34% by T1 and 10.40% by T2. The same trend was observed in hyperglycemic study (study III) in which glucose level decreased from 141.53±4.95 to 116.90±4.09 mg/dL by grapefruit peel extract enriched fruit leather and 128.52±4.15 mg/dL by grapefruit bagasse extract enriched fruit leather. Similarly, the insulin level increased 10.32 and 5.07% in T1 and T2. The liver functioning tests as AST, ALT & ALP and kidney functioning tests (urea and creatinine levels) remained non-significant in all the studies by the supplementation of both fruit leathers. Moreover, neither grapefruit peel extract enriched fruit leather nor grapefruit bagasse enriched fruit leather impart any harmful effect on the biochemistry of blood as proved by the hematological analyses. Conclusively, it is stated that citrus wastes based fruit leathers are effectual to mitigate health related disorders.