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1.
Iran J Pharm Res ; 17(4): 1550-1562, 2018.
Article in English | MEDLINE | ID: mdl-30568711

ABSTRACT

A number of ways have been investigated for administration of antibacterial agents in dealing withplaque-initiated periodontal disease. These include prolonged release intrapocket devices which are inserted at diseased sites. Intrapocket drug delivery system was designed which contain Doxycycline Hyclate; an antibacterial agent. The formulations were so developed with an aim to reduce the dose of a drug, to target the drug to the specific site and to maintain dosage at its absorption site for an extended period of time thereby improves the patient compliance. The study was aimed towards by formulating the periodontal in situ gels by temperature induced gelation technique with the utilization of polymer Pluronic F127 which is synthetically prepared. The Pluronic F127 showed the sol-gel transition phenomenon in between 27-37 °C. In situ gels were prepared and characterized/evaluated for its physico-chemical properties such as pH, gelation properties, rheology, gel strength, mucoadhesion, drug content, in-vitro, and ex-vivo drug release rate, texture analysis and Differential Scanning Colorimetry etc. The formulation found to be solution at room temperature and forms gel after installation into periodontal pocket hence leadingto increase in retention time and to slowly release the drug into pocket. The results of characterization of formulation were found to be satisfactory and hence significant bioavailability can be increased, so these in situ gelling systems will be useful in future for improving therapeutic efficacy of Doxycycline hyclate in treatment of Periodontitis. Owing to these properties it can be used as an effective delivery system for the intrapocket route.

2.
Pharm Dev Technol ; 15(1): 46-52, 2010.
Article in English | MEDLINE | ID: mdl-19552545

ABSTRACT

The eye presents unique opportunities and challenges when it comes to the delivery of pharmaceuticals. In the present study, ocular inserts of levofloxacin were prepared using chitosan and gelatin by solvent casting technique with an aim to improve therapeutic efficacy in the treatment of conjunctivitis. Prepared ocular inserts were then evaluated for film thickness, weight variation, content uniformity, percentage moisture loss and absorption. In vitro drug release studies were carried out using flow through apparatus that simulated the eye conditions. Optimized formulations were subjected to in vivo and stability studies to assess the effectiveness of the formulations. Finally in vitro in vivo correlation was established. Plasticizer like PEG was found to influence their effect on drug release. Prepared ocular inserts exhibited zero order kinetics which was confirmed by strong and positive correlation. The in vitro and in vivo drug release studies revealed that the formulations provide a best alternative to prolong the drug release at the end of 24 h and remained stable with intact at ambient conditions.


Subject(s)
Anti-Bacterial Agents/administration & dosage , Chitosan , Conjunctiva , Drug Delivery Systems , Gelatin , Levofloxacin , Ofloxacin/administration & dosage , Animals , Anti-Bacterial Agents/pharmacokinetics , Conjunctivitis/drug therapy , Drug Compounding , Drug Design , Drug Stability , Humans , Male , Ofloxacin/pharmacokinetics , Plasticizers , Polyethylene Glycols , Polymers/chemistry , Rabbits
3.
Chem Pharm Bull (Tokyo) ; 57(9): 914-9, 2009 Sep.
Article in English | MEDLINE | ID: mdl-19721251

ABSTRACT

The objective of the present study was to prepare ocular inserts of Gatifloxacin. The inserts were fabricated by solvent casting technique, with an aim by achieving once a day administration in the treatment of conjunctivitis. Inserts were evaluated for film thickness, weight variation, drug content, percentage moisture absorption and loss. In-vitro drug release studies were done using bi-chambered donar receiver compartment model. The optimized formulations were subjected to in-vivo studies using rabbits as an animal model and stability studies to assess the effectiveness of the formulations. Finally in-vitro and in-vivo correlation was established. In-vitro drug release data was treated according to zero, first, Korsemeyer Peppas and Higuchi kinetics to access the mechanism of drug release. Formulations were found to be uniform in physicochemical parameter with a fewer variations. Plasticizer was found to influence in mechanical properties as well as modify the drug release rate of the films. Prepared ocular inserts exhibited desired release within 24 h and found to be strongly revealing the efficacy of in vitro-in vivo correlation. From stability studies inserts were remained stable both physically and chemically. No burst effect but a prolonged drug release was observed from all formulations. Thus it achieves target such as increased residence time, prolonged drug release, reduction in frequency of administration and may improve the patient compliance.


Subject(s)
Anti-Infective Agents/administration & dosage , Drug Delivery Systems/methods , Fluoroquinolones/administration & dosage , Polymers/chemistry , Animals , Anti-Infective Agents/pharmacology , Conjunctivitis/drug therapy , Drug Compounding , Drug Design , Drug Stability , Fluoroquinolones/pharmacology , Gatifloxacin , Kinetics , Plasticizers/chemistry , Plasticizers/pharmacology , Rabbits
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