Formulation and characterization of pH induced in situ gels containing sulfacetamide sodium for ocular drug delivery: A combination of Carbopol^®/HPMC polymer

© 2019, Association of Pharmaceutical Teachers of India. All rights reserved. Introduction: Topical delivery of eye drops which currently accounts to 90% of available ocular dosage forms are ideal for the treatment of eye diseases but having limitations of poor therapeutic response and low bioavailability. Objectives: The objectives of present research was to develop and characterize sustained release in situ ocular gels containing sufacetamide sodium using pH induced gelling polymers for improved therapeutic response and patient compliance. Methods: In situ gel formulations prepared by dispersion method using Carbopol® 940/Carbopol® 934 alone or in combination with hydroxypropyl methylcellulose (HPMC E4M). Formultaions were evaluated for appearance, pH, viscosity, gelling capacity, drug content and in vitro drug release. The optimized formulation was assessed for sterility and antimicrobial efficacy using disk diffusion technique in comparison to commercial eye drops (Albucid®10%). Results: The appearance of in situ gels were clear and free flowing in nature however, a viscous clear solution with no flow was produced for formulations consisting of 0.8% w/v Carbopol® 940/Carbopol® 934 and 2% w/v HPMC E4M. pH of all the formulations was within the range of 5.9 to 6.7. In situ gels with Carbopol® 940 demonstrated higher viscosity compared to Carbopol® 934 and drug release was sustained over a period of 8 hr. The selected formulation containing 0.8% w/v Carbopol® 940 and 1.5% w/v HPMC E4M passed sterility test and demonstrated similar antimicrobial efficiency compared to commercial product. Conclusion: Carbopol®/HPMC-based in situ gels have potential to improve patient’s compliance by reducing the dosing frequency and could be a viable alternative to commercial product

Formulation, characterization, in vitro, in vivo, and histopathological evaluation of transdermal drug delivery containing norfloxacin and Curcuma longa.

OBJECTIVE: In an attempt for better treatment of bacterial infections and burn wounds, semisolid formulations containing norfloxacin (NF) and natural wound healing agent Curcuma longa were prepared. The rationale behind employing combination of NF and Curcuma longa is to obtain synergistic wound healing effect. The prepared formulations were compared with silver sulfadiazine cream 1%, USP. MATERIALS AND METHODS: Various ointments containing NF and C. longa were prepared using standard procedures. These formulations were evaluated for antimicrobial activity against various strains of aerobic and anaerobic microorganisms. The wound healing property was evaluated by histopathological examination and by measuring the wound contraction. RESULTS: The significant antimicrobial and wound healing effects were demonstrated by formulations which are comparable with silver sulfadiazine 1% cream (P < 0.05). Various morphological changes were observed by histopathology during the study period (days 1, 4, 8, and 12) which also supported the wound healing process. CONCLUSION: Based on the observed antimicrobial and wound healing effects, the formulations containing combination of NF and Curcuma longa could be employed as an alternative to commercial silver sulfadiazine 1% cream. This innovative mode of formulation can be employed for making burn wound healing process more effective

Development and anti-microbial potential of topical formulations containing Cocos nucifera Linn

In order to achieve better treatment for local wounds and bacterial infections, topical formulations containing Cocos nucifera Linn. were developed. These formulations were evaluated for their physicochemical properties and antimicrobial efficacy against various strains of microorganisms. Semisolid formulations containing 5% w/w of Cocos nucifera Linn. were prepared by employing different dermatological bases and were evaluated for their physical appearance, pH, rheological properties, FTIR-spectroscopic analysis, thermodynamic stability and stability studies. The antimicrobial activity of each prepared formulation was determined using disk-diffusion method against various strains of microorganisms. All the prepared formulations were found to be stable and exhibited suitable physicochemical characteristics including pH, viscosity and spreadability which are necessary for an ideal topical preparation, in addition to strong antimicrobial activity. Carbopol gel base was found to be the most suitable dermatological base for Cocos nucifera Linn. in comparsion to other bases. Cocos nucifera Linn. formulations showed great potential for wounds and local bacterial infections. Moreover, carbopol gel base with its aesthetic appeal was found to be a suitable dermatological base for Cocos nucifera Linn. semisolid formulation as it had demonstrated significant physicochemical properties and greater diffusion when assessed using disk-diffusion method. © 2013 Bentham Science Publishers

Anti-inflammatory, antibacterial and analgesic potential of cocos nucifera linn.: A review

At present, approximately 25% of drugs in modern pharmacopoeia are derived from plant sources (phytomedicines) that can be developed for the treatment of diseases and disorders. Many other drugs are synthetic analogues built on the prototype compounds isolated from plants. Cocos nucifera Linn. (Arecaceae), which is commonly known as coconut, is a plant possessing a lot of potential as an ingredient in traditional medicines for the treatment of metabolic disorders and particularly as an anti-inflammatory, antimicrobial and analgesic agent. This review emphasizes on the recent literature and research findings that highlight the significant biological activities of C. nucifera Linn. such as its anti-inflammatory, antimicrobial and analgesic properties. This review can help researchers keen on exploiting the therapeutic potential of C. nucifera Linn. which may motivate them to further explore their commercial viability. © 2013 Bentham Science Publishers

Moxifloxacin loaded chitosan gel formulations for the treatment of periodontal diseases

For treatment of periodontal diseases, the local delivery of antimicrobials into periodontal pocket has been shown to be more effective than the systemic delivery. However, the major challenge for the formulators is the removal of the delivery system from the application side due to the salivation as well as the movement of the tongue. Mucoadhesive polymers have been successfully utilized to go over this obstacle. In recent years, particularly chitosan has been widely investigated for periodontal delivery systems not only for its mucoadhesive properties but also for its antimicrobial activity. In our study, we developed a local delivery system for an antimicrobial drug, moxifloxacin hydrochloride (MF), at 0.5% w/v, using chitosan for the treatment of periodontal diseases. For comparison, formulations based on two other mucoadhesive polymers, carbomer (Carbopol 940®) and hydroxypropyl methylcellulose(HPMC) were also prepared. Viscosity, mucoadhesion, drug release and permeation properties as well as the antimicrobial activity of the gel formulations was evaluated in vitro. The developed formulations with a suitable viscosity for application were found to remain on the mucosa and release the drug in a prolonged fashion. Drug release from the formulations was found to be dependent on the viscosity of the formulations. A relative correlation was found between viscosity and mucoadhesion for the polymers investigated, with an order of HPMC>Carbopol®=Chitosan. Permeation of the drug was increased in presence of chitosan. The antimicrobial activity of MF against Staphylococcus aureus and Streptococcus mutans were found to be enhanced with the developed formulations. The highest antimicrobial activity was observed with the chitosan-based formulations, due to the synergic effect of chitosan itself. Our results showed that chitosan based formulation is a promising local delivery system for treatment of periodontal disease by increasing the effect of the drug due to its mucoadhesive and penetration enhancing effect as well its antimicrobial activity Furthermore, with these properties the developed formulations will provide reduced frequency of administration, which result in higher patient compliance