Physical study of Chloramphenicol <i>In Situ</i> Gel with Base Hydroxypropyl Methylcellulose and Poloxamer 188

Kurniawansyah, Insan Sunan; Sopyan, Iyan; Iqbal, Muhammad; Subarnas, Anas

doi:10.4103/jpbs.jpbs_201_19

Cited by 13 publications

(9 citation statements)

References 10 publications

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“…In testing of in situ ophthalmic gel with chloramphenicol active agent, it is known that if a pH value of less than 5.5 can cause chloramphenicol in the gel in situ to become unstable due to the pH stability of chloramphenicol preparations between 5.5 and 7.4 [15].…”

Section: Measurement Of Phmentioning

confidence: 99%

Physical Characterization of in Situ Ophthalmic Gel: A Concise Review

2022

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In situ ophthalmic gel is a type of eye drug preparation that has a higher bioavailability value and has a longer contact time with maximum therapeutic effect and with minimal side effects compared to conventional eye preparations. The preparation of ophthalmic in situ gel is required characterization to make sure that the prepared preparations meet the standards and are safe when used. This journal review aims to look at the methods used in characterizing physical properties in in situ ophthalmic gel formulations with different active substances such as rheology studies, organoleptic tests, pH, clarity, and gelling capacity. In order to get the best formulation of in situ ophthalmic gel preparations so as to provide maximum therapeutic effect.

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Section: Measurement Of Phmentioning

confidence: 99%

Physical Characterization of in Situ Ophthalmic Gel: A Concise Review

2022

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“…22,23 Hydroxypropyl methyl cellulose (HPMC) can be added to reduce the required P407 concentration and improve the mucoadhesive properties of the final preparation. 21,24 The present work focused on developing a liposomal thermosensitive hydrogel loaded with fasudil-phospholipid complex, in the form of ophthalmic eye drops, aiming to tackle the root cause of glaucoma. Characterizing the optimized formulation in vitro, ex vivo, and investigating its safety and efficacy against glaucomatous rabbit eyes was carried out.…”

Section: Introductionmentioning

confidence: 99%

Exploring a Novel Fasudil-Phospholipid Complex Formulated as Liposomal Thermosensitive in situ Gel for Glaucoma

Khallaf¹,

El‐Moslemany²,

Ahmed

et al. 2022

IJN

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Purpose: Fasudil hydrochloride (Fas), a rho-associated protein kinase inhibitor, proved to be promising for glaucoma management owing to its IOP lowering and antioxidant effects. However, its highly hydrophilic nature limits ocular permeation and bioavailability. Hence, the study objective was the development of Fas loaded vesicular system with high entrapment efficiency formulated as a thermosensitive gel for local administration aiming to enhance ocular retention and permeation and hence therapeutic efficacy. Methods: Fasudil complex with phospholipid (Fas/PL) was prepared by solvent evaporation technique and characterized by Fourier transform infrared spectroscopy (FT-IR) and X-ray diffraction (XRD). Fas/PL was further formulated as liposomes by methanol injection method and characterized regarding colloidal properties, entrapment efficiency (EE%) and in vitro drug release. The prepared liposomes were incorporated into an optimized thermosensitive in situ gel (Fas/PL-Lipo P407/HPMCgel ) selected based on gelling time and temperature and rheological properties. The effect of incorporation into gel on the in vitro characteristics of liposomes was investigated. The in vitro mucoadhesive potential, ex vivo permeation, irritability and efficacy in a glaucoma rabbit model were also assessed. Results: FT-IR and XRD suggested interactions between Fas and PL, proposing complexation. Fas/PL liposomal dispersions showed good colloidal properties (particle size: 132.5 ± 1.6 nm, zeta potential: −21.6 ± 0.9 and %EE 78.6 ± 0.3%) with sustained drug release. In situ thermosensitive gel (20% poloxamer 407 and 0.5% HPMC) showed optimum gelling properties. The selected gel formulation reduced burst release of the drug, enhanced mucoadhesive properties and prolonged corneal permeation ex vivo. HET-CAM test confirmed that the prepared formulations were non-irritant. In vivo pharmacodynamic study indicated improved bioavailability and significantly lower intraocular pressure (IOP) of Fas/PL-Lipo P407/HPMC gel compared to drug solution and liposomal dispersion. Conclusion:The results present Fas/PL-Lipo P407/HPMC gel as a potential platform for ophthalmic delivery of fasudil with improved pharmaceutical attributes and enhanced bioavailability and efficacy in glaucoma.

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“…As a small member of PL family, the molecular weight of PL124 ranges from 2090 to 2360 [2]. Owing to the characteristics of polymer micelles, PL188 and PL407 have been widely used in eye and rectum preparations, burn, cosmetic, anti-tumor, as well as cell membrane repair [3][4][5][6][7][8][9][10].…”

Section: Introductionmentioning

confidence: 99%

Ultra‐high‐performance liquid chromatography coupled with quadrupole time of flight mass spectrometry method for quantifying polymer poloxamer 124 and its application to pharmacokinetic study

Cui

et al. 2021

J of Separation Science

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Poloxamer is a commonly used pharmaceutical excipient. It is a high molecular polymer formed using polypropylene oxide and polyethylene oxide units. Specifically, poloxamer 124 is one of the smaller molecular weight in the poloxamer series; however, its pharmacokinetic behaviors in vivo are still unclear.In this study, a method for quantifying poloxamer 124 in rat plasma through ultra-high-performance liquid chromatography coupled with quadrupole time of flight mass spectrometry was developed. The intravenous dosage of PL124 was 10 mg/kg. Plasma was collected at different times. The calibration curve was linear in the range of 0.1-5 μg/mL for the poloxamer 124 (r ≥ 0.9956) with the lower limit of quantitation of 0.1 μg/ml. The relative standard deviation of the intraday and interday precisions was below 8.0%, and the relative error of the accuracy was within ±12.0%. The extraction recovery, matrix effect, and stability were satisfactory in rat plasma. The validated method was successfully applied to a pharmacokinetic study of poloxamer 124 in rats. Results indicated that poloxamer 124 could be rapidly absorbed and eliminated through caudal vein injection. This study is helpful for the further study of poloxamer 124.

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Physical study of Chloramphenicol In Situ Gel with Base Hydroxypropyl Methylcellulose and Poloxamer 188

Cited by 13 publications

References 10 publications

Physical Characterization of in Situ Ophthalmic Gel: A Concise Review

Physical Characterization of in Situ Ophthalmic Gel: A Concise Review

Exploring a Novel Fasudil-Phospholipid Complex Formulated as Liposomal Thermosensitive in situ Gel for Glaucoma

Ultra‐high‐performance liquid chromatography coupled with quadrupole time of flight mass spectrometry method for quantifying polymer poloxamer 124 and its application to pharmacokinetic study

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