Studies on Formulation Development of Mucoadhesive Sustained Release Itraconazole Tablet Using Response Surface Methodology

Conventional vaginal formulations are associated with disadvantages of low retention in the vaginal epithelium, leakage and messiness, thereby causing inconvenience to the user. To circumvent these problems, bioadhesive drug delivery systems are propagated (1). The aim of the present investigation was to prepare and evaluate novel bioadhesive vaginal tablets containing clotrimazole loaded microspheres in order to provide long-term therapeutic activity at the site of infection. Tablets were prepared by incorporating drug loaded microspheres and using bioadhesive polymers hydroxypropylmethylcellulose, sodium carboxymethylcellulose and Carbopol. Microspheres were prepared by the spray drying technique using Eudragit RS-100 and Eudragit RL-100. Microspheres were characterized by SEM, DSC, FTIR, particle size analysis and evaluated for percentage yield, drug loading, encapsulation efficiency and in vitro drug release. To achieve bioadhesion to the mucosal tissue, optimized microspheres were incorporated into bioadhesive tablets and were evaluated for in vitro drug release, in vitro and in vivo mucoadhesion. FTIR and DSC studies showed that no chemical interaction occurred between the drug and polymers. The sphericity factor indicated that the prepared microspheres were spherical. Formulation Mt6 indicated a controlled in vitro drug release and good bioadhesive strength. The in vivo images confirmed the bioadhesion and retention property of tablets up to 24 h. The results indicated that this drug delivery system can be explored for controlled intravaginal drug release.

show abstract

“…Thickness, average mass, hardness and percentage friability of the prepared tablets were found to be satisfactory (14).…”

Section: Drug Loading and Encapsulation Efficiencymentioning

confidence: 84%

Bioadhesive vaginal tablets containing spray dried microspheres loaded with clotrimazole for treatment of vaginal Candidiasis

et al. 2013

View full text Add to dashboard Cite

show abstract

“…A 3 2 full factorial design was constructed where the polymer ratio (HPMC K100M, sodium alginate) was selected as independent variables. The levels of the two factors were selected on the basis of the preliminary studies carried out before implementing the experimental design [10]. All other formulations and processing variables were kept constant throughout the study.…”

Section: Formulation Of Floating Tabletsmentioning

confidence: 99%

Investigation and Optimization of the Effect of Polymers on Drug Release of Norfloxacin from Floating Tablets

2017

View full text Add to dashboard Cite

Oral delivery of drugs is by far the preferable route of drug delivery due to the ease of administration, patient compliance and flexibility in formulation, etc [1]. The majority of formulations available on the market are oral drug delivery systems. Oral drug delivery systems have developed from immediate release to targeted or site specific delivery over a predefined period. An ideal drug delivery system possess two important characteristics that are with single dose frequency and ability to release the active drug directly at the site of action [2]. Thus, the objective of the pharmacist is to develop systems that release an optimal quantity of drug to a desired site of action. Attempts to develop a single-dose therapy for the whole duration of treatment has lead to the development of controlled or sustained release drug delivery systems.Oral controlled release systems have been developed to achieve optimal drug delivery to the systemic circulation. Although such systems can precisely control the drug release for a prolonged period of time, even over a number of days, some drugs have a narrow absorption window due to them not being absorbed through the gastrointestinal tract, as the dosage formulation will pass through the absorption window. Thus, there was the need to develop a formulation which will prolong the gastric residence time of the system to achieve complete drug release in the gastrointestinal tract (stomach and small intestine) and which will modulate the drug release rate as predicted by the system.Norfloxacin is amongst the most prescribed fluoroquinolone antiinfective for urinary tract infections, prostatitis, gonorrhea and genital tract infection Objectives. The objective of this study was to investigate the effect of release-retarding polymers on the drug release of norfloxacin from floating tablets. Material and Methods. Norfloxacin was procured as a gift sample from Concept Pharma Ltd. Aurangabad (India) and HPMC K100M was procured as a gift sample from Colorcon Asia Pvt. Ltd., Goa (India). The tablets were prepared by direct compression method and various pharmaceutical parameters were evaluated. Results. It was observed that all tablet formulations F1-F9 retained the drug release up to 12 h with good floating property but only Batch-F4 complies with the USP dissolution limits with a minimum floating lag time. The drug release kinetics were evaluated by the model-dependent (curve fitting) method using PCP Disso v3 software shows Batch-F4 shows to best fit with Peppas model for which R2 value was 0.9921 and the release exponent value was 0.6892. Conclusions. The drug release kinetics study indicates that the floating tablets release the drug by diffusion followed by erosion mechanism. Obtained in-vitro drug release data was analyzed by design expert software for drug release at first hour and at 12 th h values and found that release the selected independent variables like HPMC K100M and sodium alginate concentration has a significant effect on drug release (Polim. Med. 2016, 46, 2, 117-127).

show abstract

“…Under biopharmaceutical classification system (BCS), it is categorized as a class-II drug with low water solubility and high permeability. All these attributes of itraconazole are favourable in its incorporation in a GRDDS 62 . Table 3 summarizes the list of drugs preferably incorporated in the GRDDS along with their brand name and company name.…”

Section: Preformulation Studies In Grddsmentioning

confidence: 99%

Technologies, Optimization and Analytical Parameters in Gastroretentive Drug Delivery Systems

Chordiya¹,

Gangurde²,

Borkar³

2017

Current Science

View full text Add to dashboard Cite

Gastroretentive drug delivery systems (GRDDS) can overcome drawbacks associated with oral drug delivery, by defeating natural physiological principles. Various gastroretentive technologies have been developed in the past, but few of them achieved commercial success. Numerous mechanisms like floating, sinking, effervescence, swelling, bioadhesion, magnetic, etc. have been proposed over the years. At present, the polymeric swellings monolithic systems are popular. Dual working technology would be a possible way to overcome drawbacks associated with different GRDDS. Before development of a drug product, the principles of scale-up and process validation must be considered to improve the quality and market availability of GRDDS. Knowledge of all regulatory aspects will help deliver a product to the market within a reasonable time-frame and in a cost-effective manner.

show abstract

Studies on Formulation Development of Mucoadhesive Sustained Release Itraconazole Tablet Using Response Surface Methodology

Cited by 31 publications

References 14 publications

Bioadhesive vaginal tablets containing spray dried microspheres loaded with clotrimazole for treatment of vaginal Candidiasis

Bioadhesive vaginal tablets containing spray dried microspheres loaded with clotrimazole for treatment of vaginal Candidiasis

Investigation and Optimization of the Effect of Polymers on Drug Release of Norfloxacin from Floating Tablets

Technologies, Optimization and Analytical Parameters in Gastroretentive Drug Delivery Systems

Contact Info

Product

Resources

About