The aim of this study was to investigate pharmaceutical potentialities of a polymeric microparticulate drug delivery system for modulating the drug profile of poorly water-soluble quercetin. In this research work two cost effective polymers sodium alginate and chitosan were used for entrapping the model drug quercetin through ionic cross linking method. In vitro drug release, swelling index, drug entrapment efficiency, Fourier Transforms Infrared Spectroscopy (FTIR), Scanning Electron Microscopy (SEM), X-ray Diffraction (XRD) and Differential Scanning Calorimetric (DSC) studies were also done for physicochemical characterization of the formulations. Swelling index and drug release study were done at a pH of 1.2, 6.8 and 7.4 to evaluate the GI mimetic action which entails that the swelling and release of the all the Formulation1 (F1), Formulation2 (F2) and Formulation3 (F3) at pH 1.2 were minimal confirming the prevention of drug release in the acidic environment of stomach. Comparatively more sustained release was seen from the formulations F2 & F3 at pH 6.8 and pH 7.4 after 7 h of drug release profiling. Drug entrapment efficiency of the formulations shows in F1 (D:C:A = 2:5:30) was approximately 70% whereas the increase in chitosan concentration in F2 (D:C:A = 2:10:30) has shown an entrapment efficiency of 81%. But the comparative further increase of chitosan concentration in F3 (D:C:A = 2:15:30) has shown a entrapment of 80% which is not having any remarkable difference from F2. The FTIR analysis of drug, polymers and the formulations indicated the compatibility of the drug with the polymers. The smoothness of microspheres in F2 & F3 was confirmed by Scanning Electron Microscopy (SEM). However F1 microsphere has shown more irregular shape comparatively. The DSC studies indicated the absence of drug-polymer interaction in the microspheres. Our XRD studies have revealed that when pure drug exhibits crystalline structure with less dissolution profile, formulated microparticles can help us to obtain amorphous form of the same drug that is likely to have more dissolution property. The findings of the study suggest that the microsphere formulations were a promising carrier for quercetin delivery and can be considered as a favorable oral controlled release dosage form for hydrophobic drug quercetin.

BACKGROUNDTopical adapalene and tretinoin, are comedolytic, anti-comedogenic and anti-inflammatory, on RAR (α, β, ℽ) receptors binding. Due to higher chemical stability, lipophilicity and lesser photo-lability, adapalene enables quicker follicular penetration, by lesser anti-AP-1 (c-Jun, c-Fos) and no CRBPII mRNA action, thus producing lesser photosensitivity and no skin irritation, unlike tretinoin; in which, these are reducible by overnight application, combination therapy, slow-release polymers or emollients. Topical nadifloxacin is bactericidal, anti-inflammatory and comedolytic, with inhibitory effect on DNA gyrase, DNA topoisomerase IV and IL-1α, IL-6, IL-8. The Global Alliance to Improve Outcomes in Acne guidelines recommend synergistic and additive combination therapies, which enhance therapeutic efficacy and reduce adverse effects. Due to inadequacy of data, this study was conducted, to compare the safety between topical 1% nadifloxacin and 0.1% adapalene combination therapy and topical 1% nadifloxacin and 0.025% tretinoin combination therapy, in mild to moderate acne, in tertiary care hospitals, in India. METHODSGroups A and B (50 patients each), applied topical 1% nadifloxacin and 0.1% adapalene combination therapy and 1% nadifloxacin and 0.025% tretinoin combination therapy, respectively, over their mild to moderate facial acne lesions, once daily overnight; and adverse effects, like erythema, scaling, dryness, pruritus, burning or stinging, were assessed on 0, 15, 30, 60, 90 days and follow-ups, by Local Irritation Scale. This is a multi-centre, prospective, randomised, open-labelled, comparative, rational pharmacotherapeutic study. Data was statistically analysed, with the calculation of Z values and p values, along with the Z test for proportions. RESULTSIn both groups, no adverse effects were observed, with no statistically significant difference among the observations. CONCLUSIONSThe therapies were well tolerated and safe among both groups.

Background: Topical adapalene and tretinoin, are comedolytic, anti-comedogenic and anti-inflammatory, on RAR (α, β, γ) receptors binding. Adapalene enables quicker follicular penetration, by lesser anti-AP-1 (c-Jun, c-Fos) and no CRBPII mRNA actions, causing chemical stability, lipophilicity and less photo-lability, producing lesser photosensitivity and no skin irritation, unlike tretinoin; wherein reducible by overnight application and combination therapy, slow-release polymers or emollients, respectively. Topical nadifloxacin is bactericidal, anti-inflammatory and comedolytic, with inhibitory effect on DNA gyrase, DNA topoisomerase IV and IL-1α, IL-6, IL-8. The Global Alliance to Improve Outcomes in Acne Guidelines recommend synergistic and additive combination therapies, which enhance therapeutic efficacy and reduce adverse effects. Due to inadequacy of data, this study was conducted, to compare the safety among topical anti-acne monotherapies and combination therapies, and to easily detect any adverse effect producing component in the topical combination therapy.Methods: In this multi-centre, prospective, randomised, open-labelled, comparative study, groups A, B, C, D and E (20 patients each), applied topical 1% nadifloxacin monotherapy, 0.1% adapalene monotherapy, 0.025% tretinoin monotherapy, 1% nadifloxacin and 0.1% adapalene combination therapy and 1% nadifloxacin and 0.025% tretinoin combination therapy, respectively, over their facial mild to moderate acne lesions, once daily overnight; and adverse effects, like erythema, scaling, dryness, prutitus, burning, or stinging, were assessed on 0, 15, 30, 60, 90 days and follow-ups, by Local Irritation Scale.Results: In all 5 groups, no adverse effects were observed, with no statistically significant difference among the observations.Conclusions: The therapies were well tolerated and safe among all 5 groups.

Background: Topical pharmacotherapeutic modalities would minimalize systemic adverse effects. Ofloxacin, the bactericidal racemic mixture, has inhibitory effects on DNA gyrase, DNA topoisomerase IV and IL-1α, IL-6, and IL-8. This was a comparative study for pharmacovigilance scoring of causality assessment grading and staging of topical ofloxacin pharmacotherapy in bacterial conjunctivitis and otitis externa.Methods: Group A=50 bacterial conjunctivitis patients were prescribed topical ophthalmic 0.3% ofloxacin, 2 drops in each eye after every 3 hours for 2 days, and 2 drops in each eye after every 6 hours for next 5 days; and group B=50 otitis externa patients were prescribed topical otic 0.3% ofloxacin, 3 drops in each ear after every 6 hours for first 2 days, and 5 drops in each ear after every 12 hours for next 5 days. Comparative adverse drug reactions occurrence, like transient ocular burning or discomfort, ocular irritation, redness, stinging, pruritis, photophobia, ocular watering and dryness in group A, and pruritis, headache, dizziness, mild ear pain, rashes, and hypersensitivity reactions in group B, were analysed with adverse event case report forms, on days 0, 3, 5, 7, 10, 15, 30, and on follow-ups, with causality assessment scores, from adverse drug reactions grading and staging.Results: The occurrence of adverse effects were statistically non-significant, in both groups, with causality assessment scoring for group A: -11, none on average=Unlikely causality, and group B: -11, none on average= Unlikely causality.Conclusions: Topical ofloxacin therapy in group A and group B patients, were safe and tolerable; with nil causality of association of adverse drug reactions.

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