Ophthalmic Delivery of Riboflavin Loaded Nanoparticulate Suspension in Keratoconus: A Preclinical Study in Rabbit Model

The present investigation undertakes the formulation of nanoparticulate suspension of Riboflavin to treat keratoconus disease by applying it to the infected mice corneas. The nanoparticles of Riboflavin were prepared using single solvent evaporation method and later formulated as suspension using continuous probe sonication method. Then, both riboflavin nanoparticles and suspension were evaluated for various parameters. The nanoparticles showed smooth and spherical surface with in vitro drug release up to 77.89%. The drug content was found to be 97.23%–98.89%. The suspension was found to be visually clear with pH ranging from 6 to 7. The drug entrapment was found to be from 76.37% to 97.34%. Since there was no hemolytic activity, this formulation was suitable for ophthalmic administration. The Draize test confirmed the non-irritant, non-itchy nature of formulation. The prepared formulations, such as nanoparticulate gel and suspension, were found to be significantly efficacious in experimental animals.

STUDY OF ISOTONICITY AND OCULAR IRRITATION OF CHLORAMPHENICOL IN SITU GEL

Objective: The objective of this study was to find out the isotonicity of chloramphenicol ophthalmic in situ gel and to know the irritating effect of its in the eyes of test animals, so it can be to maximize absorption of the drug in the eye, minimize drug loss before corneal penetration and safe to used. Methods: This study were started by making four aseptic formulations of in situ gel preparations with a comparison of the baseline concentrations of different Poloxamer 407 and HPMC, F1 (5: 0.45), F2 (10: 0.45), F3 (5: 1) and F4 (10: 1). Four aseptic of in situ gel preparations, followed by a qualitative isotonicity test using blood cells to see the comparison between control and test preparations, and ocular irritation test using the draize test method to determine the presence or absence of the irritation. Results: The results obtained from the isotonicity test showed that the four preparations have normal blood cells that similar with isotonic control solution; therefore, it can be said that the preparations have been made isotonic. The results of the ocular irritation test using the draize test method showed for each category, such as cornea, iris, conjunctiva and edema were zero. A zero value on the cornea indicates no ulceration or opacity, and the iris, conjunctiva and edema were normal. Conclusion: Chloramphenicol in situ gel are isotonic and do not cause irritation to the rabbit's eyes, so they are safe to use and the formulation can be used for further research until the final goal is obtained.

Naringin derivatives as glucosamine-6-phosphate synthase inhibitors based preservatives and their biological evaluation

Glucosamine-6-Phosphate synthase enzyme has been targeted for development of better and safe preservative due to its role in microbial cell wall synthesis. In recent year’s demand of preservatives for the food, cosmetics and pharmaceuticals have increased. Although, the available synthetic preservatives have associated unwanted adverse effects, soa chain of naringin derivatives were schemed synthesized and judged for antioxidant, antimicrobial, preservative efficacy, stability study and topical evaluation. Molecular docking resulted with excellent dock score and binding energy for compound 7, compound 6 and compound 1 as compared to standard drugs. Resultant data of antimicrobial activity revealed compound 7as most potent antimicrobial compound for P. mirabilis, P. aeruginosa, S. aureus, E. coli, C. albicans, and A. niger, respectively, as compared to the standard drugs. The preservative efficacy test of compound 7 in White Lotion USP showed the log cfu/mL value within prescribed limit of USP standard. Compound 7 stabilize the White lotion USP from microbial growth for a period of six months under accelerated storage condition. Compound 7 was further evaluated for toxicity by using the Draize test in rabbits and showed no sign of eye and skin irritation. The outcome demonstrated that synthesized naringin compounds showed glorious antioxidant, antimicrobial, preservative efficacy, stable and safe as compared to standards.

Uji Iritasi dan Uji Sifat Fisik Sediaan Gel Minyak Atsiri Daun Cengkeh (Syzygium aromaticum (L.) Merr. & L.M.Perry) dengan Variasi Konsentrasi HPMC

Inflamasi merupakan respon protektif normal terhadap luka jaringan yang disebabkan oleh trauma fisik, zat kimia yang merusak, atau zat-zat mikrobiologi. Salah satu bahan alam yang memiliki khasiat antiinflamasi adalah minyak atsiri daun cengkeh (Syzygium aromaticum (L.) Merr. & L.M.Perry). Penelitian ini bertujuan untuk mengetahui kualitas minyak atsiri daun cengkeh, formulasi gel minyak atsiri, serta uji sifat fisik dan uji iritasinya. Minyak atsiri diperoleh dengan destilasi uap dan air. Minyak atsiri yang didapat digunakan dalam sediaan gel dengan konsentrasi hidroksipropil metilselulose (HPMC) 3% (FI), HPMC 3% dan minyak atsiri 6% (FII), HPMC 6% (FIII), HPMC 6% dan minyak atsiri 6% (FIV), HPMC 10% (FV), serta HPMC 10% dan minyak atsiri 6% (FVI). Pengamatan terhadap gel meliputi uji organoleptik, homogenitas, pH, uji daya lekat, dan uji daya sebar. Gel yang telah diuji sifat fisiknya, dievaluasi iritasinya terhadap kulit dengan metode Draize test. Data hasil pengujian dianalisis statistik dengan ANAVA satu arah dengan taraf kepercayaan 95%. Dari penelitian yang telah dilakukan diperoleh hasil minyak atsiri daun cengkeh yaitu berwarna kuning kecoklatan dan berbau khas daun cengkeh dengan nilai rendemen sebesar 1,6%, indeks bias sebesar 1,525, dan bobot jenis sebesar 1,02. Gel daun cengkeh memenuhi standar kualitas gel yaitu homogenitas, daya sebar, pH, dan daya lekat. Analisis statistik terhadap masing-masing percobaan tidak menunjukkan perbedaan yang signifikan. Hasil percobaan terhadap uji iritasi menunjukkan bahwa sediaan gel tidak menimbulkan iritasi pada kulit marmut.

APPLICATION AND CHARACTERIZATION OF IN SITU GEL

Applications of in situ gel have been used for a variety of drug delivery routes, such as oral, ocular, rectal, vaginal and injection. Characterization of in situ gel was determined to ensure that the prepared preparation met the standard and it safe. This review describes every aspects of this novel application and characterization of in situ gel preparations, which present the readers an exhaustive detail and might contribute to research and development. In the chemical evaluation in situ gel determined the diffusion of the active substance of a compound by measuring its concentration. In physical evaluation of isotonic calculated by osmotic pressure, drug release was determined by melting point of the substance polymer, gel strength as measured by rheometer, homogenecity test determined by under the light, and stability test with environmental conditions setting. In microbiology evaluation determine if the preparations was contaminated or not, also be effective and safe. Ocular irritation studies-Draize Test us an animal mice or rabbit and determination of visual appearance, clarity, and pH is required. In situ gels offer the primary requirement of a successful controlled release product that is increasing patient compliance.