Development of long-acting bioadhesive vaginal gels of oxybutynin: Formulation, in vitro and in vivo evaluations

Tuğcu-Demiröz, Fatmanur; Acartürk, Füsun; Erdoğan, Deniz

doi:10.1016/j.ijpharm.2013.09.003

Cited by 94 publications

(54 citation statements)

References 74 publications

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“…Since the viscosity of the F1 formulation is higher than F4, the drug release may be less. Similar results were obtained in our previous study [21,23]. F1, F2, F3 and when F4 hydrogel formulations were released about 65.3±5.1, 80.6±3.8, 88.1±7.3 and 100.4±4.8 % of BNZ at 6h respectively.…”

Section: Drug Content Ph Measurements and Viscosity Studiessupporting

confidence: 91%

“…The mucosa was dipped into the vaginal fluid simulant [25] and kept for 10 min until the start of the experiment. The instrumental parameters specified in a previous study [21] were used to evaluate the mucoadhesive potential of the vaginal gel formulations. The area under the curve was calculated from a force-distance plot as the work of mucoadhesion.…”

Section: Ex-vivo Mucoadhesion Studiesmentioning

confidence: 99%

“…The hydrogels were heated within a range of 4-50°C during the procedure. The temperature at which the rotation of the magnetic bar stopped was measured as the gelation temperature [21]. …”

mentioning

confidence: 99%

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Development of in situ poloxamer-chitosan hydrogels for vaginal drug delivery of benzydamine hydrochloride: Textural, mucoadhesive and in vitro release properties

Tuğcu-Demiröz¹

2017

mpj

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The use of in situ hydrogel systems for vaginal drug delivery is an important strategy in the treatment of vaginitis. The aim of this study was to develop in situ vaginal hyrogels for benzydamine hydrochloride (BNZ) which were composed of poloxamer and chitosan. The reason for development of these hydrogels was to obtain a vaginal delivery system with improved mechanical and mucoadhesive properties that could provide prolonged retention time for the treatment of vaginits. The hydrogels were also designed for once a day dosage of the drug and to obtain a controlled release of the BNZ. For this purpose BNZ containing hydrogel formulations using thermosensitive polymer (Poloxamer 407) and mucoadhesive polymer (Chitosan H, Chitosan M and Chitosan L) were developed. The hydrogels are composed of polymers which have promising potential for vaginal delivery systems. These formulations were evaluated by rheology, texture, mucoadhesive profiles and drug diffusion with a Franz diffusion cell. It was observed that the diffusion of BNZ from the in situ poloxamer-chitosan hydrogel was more sustained and controlled than with the poloxamer gel. The hydrogel formulations diffused about 65.3±5.1, 80.6±3.8, 88.1±7.3 and 100.4±4.8% of BNZ at 6h. The formulation containing Poloxamer 407 and Chitosan H has the best controlled release profile and mucoadhesive properties, results which indicate that it could suitable for use once a day on the vaginal route. Moreover, the hydrogels higher mucoadhesion exhibited by this formulation prolongs the drug residence time compared with the poloxamer gel and may increase the BNZ efficacy. These BNZ mucoadhesive vaginal hydrogel formulations may be a promising alternative to conventional dosage forms for vaginal topical therapy.Key words: Mucoadhesion; poloxamer; chitosan; hydrogel; benzydamine hydrochloride; vaginal drug delivery. INTRODUCTIONThe vagina is the site of various pathologies such as vaginitis caused by bacteria, fungi, protozoa or virus and has been traditionally employed for the delivery of several drugs. Lately, the vagina has been utilized as a possible alternative to the parenteral administration route for the delivery of drugs [1]. Vaginal dosage forms have been developed for many drugs because of the vagina presents several advantages as a site for drug delivery, such as having large surface area, rich blood supply, avoidance of the first-pass effect, relatively high permeability to several drugs, and self-insertion [2]. It should also allow self-administration with minimal interference on body functioning and daily life, and obtain high bioavailability with other medications. The rate and extent of drug absorption after intravaginal administration may vary, depending on formulation factors, vaginal physiology, age of the patient and menstrual cycle. Suppositories, creams, gels, tablets and vaginal rings are commonly used as vaginal [3]. Gel formulations are frequently preferred for the vaginal application of various drugs with different effects, such as moisturizing ...

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Section: Drug Content Ph Measurements and Viscosity Studiessupporting

confidence: 91%

Section: Ex-vivo Mucoadhesion Studiesmentioning

confidence: 99%

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Development of in situ poloxamer-chitosan hydrogels for vaginal drug delivery of benzydamine hydrochloride: Textural, mucoadhesive and in vitro release properties

Tuğcu-Demiröz¹

2017

mpj

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“…The mucosa was dipped into the vaginal fluid simulant 24) and kept for 10 min until the start of the experiment. The instrumental parameters specified in a previous study 21) were used to evaluate the mucoadhesive potential of the vaginal gel formulations.…”

Section: Characterization Of Gels and Lipogelsmentioning

confidence: 99%

Vaginal Delivery of Benzydamine Hydrochloride through Liposomes Dispersed in Mucoadhesive Gels

Tuğcu-Demiröz

2017

Chem. Pharm. Bull.

Self Cite

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Liposomal vaginal drug delivery systems are important strategy in the treatment of both topical and systemic diseases. The aim of this study was to develop a vaginal delivery system for benzydamine hydrochloride (BNZ) loaded liposomes dispersed into mucoadhesive gels. The delivery system was also designed for a once a day dosage and to obtain controlled release of the BNZ. For this purpose BNZ containing gel formulations using hydroxypropyl methylcellulose (

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“…22,23 This polymer plays a role as the carrier, which loads a drug perfectly. It is easy to move for absorption in the body because amorphous was generated.…”

Section: -21mentioning

confidence: 99%

Improved Dissolution Behavior of Aceclofenac Loadings with Kollidon VA 64 Using Spray Drying and Rotary Evaporation Process

Yang¹,

Park²,

Lee³

et al. 2015

Polymer Korea

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In order to improve the poor water solubility of aceclofenac, it was loaded into solid Kollidon VA 64 dispersion prepared by spray drying and rotary evaporation methods using different drug and polymer ratios. Morphology and physicochemical behavior of the aceclofenac loaded solid dispersions was analyzed by scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), X-ray diffractometry (XRD), and differential scanning calorimetry (DSC). Encapsulation efficiency and dissolution behavior in a simulated intestinal juice of aceclofenac in the solid dispersions was measured using HPLC and the latter was compared with that of the active pharmaceutical ingredient (API) and Airtal ® . It was demonstrated that two methods could significantly improve the dissolution behavior of aceclofenac.

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Development of long-acting bioadhesive vaginal gels of oxybutynin: Formulation, in vitro and in vivo evaluations

Cited by 94 publications

References 74 publications

Development of in situ poloxamer-chitosan hydrogels for vaginal drug delivery of benzydamine hydrochloride: Textural, mucoadhesive and in vitro release properties

Development of in situ poloxamer-chitosan hydrogels for vaginal drug delivery of benzydamine hydrochloride: Textural, mucoadhesive and in vitro release properties

Vaginal Delivery of Benzydamine Hydrochloride through Liposomes Dispersed in Mucoadhesive Gels

Improved Dissolution Behavior of Aceclofenac Loadings with Kollidon VA 64 Using Spray Drying and Rotary Evaporation Process

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