Nano and Microparticulate Chitosan Based System for Formulation of Carvedilol Rapid Melt Tablet

Rv, Patil; Pande,; Sonawane, Raju Onkar

doi:10.15171/apb.2015.024

Cited by 18 publications

(16 citation statements)

References 22 publications

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“…The CVD release profile from nanoparticles showed a biphasic release pattern with an initial burst release in the first 2 h followed by a controlled release throughout 72 h, with higher bioavailability than marketed tablet formulation in phosphate buffer saline (PBS) pH 7.4 [ 14 ]. Chitosan nanoparticles using a spray-drying method were characterized by prolonged and controlled release, which may provide an increased clinical value compared to conventional formulations, which results from the reduced dosing frequency and prolonged therapeutic effect as well as increased bioavailability [ 16 ]. Except for oral tablets, intranasal carvedilol–chitosan microspheres with good mucoadhesive properties were able to increase drug absorption and consequently significantly improve the carvedilol bioavailability [ 17 ].…”

Section: Introductionmentioning

confidence: 99%

Chitosan as Valuable Excipient for Oral and Topical Carvedilol Delivery Systems

Sip

Paczkowska-Walendowska

Rosiak

et al. 2021

Pharmaceuticals

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Chitosan is a valued excipient due to its biocompatibility properties and increasing solubility of poorly water-soluble drugs. The research presented in this paper concerns the preparation of binary combinations of chitosan (deacetylated chitin) with carvedilol (beta-blocker) to develop a formulation with a modified carvedilol release profile. As part of the research, six physical mixtures of chitosan with carvedilol were obtained and identified by spectral (PXRD, FT-IR, and Raman), thermal (DSC), and microscopic (SEM) methods. The next stage of the research estimated the profile changes and the dissolution rate for carvedilol in the obtained drug delivery systems; the reference sample was pure carvedilol. The studies were conducted at pH = 1.2 and 6.8, simulating the gastrointestinal tract conditions. Quantitative changes of carvedilol were determined using the developed isocratic UHPLC-DAD method. Established apparent permeability coefficients proved the changes in carvedilol’s permeability after introducing a drug delivery system through membranes simulating the gastrointestinal tract and skin walls. A bioadhesive potential of carvedilol–chitosan systems was confirmed using the in vitro model. The conducted research and the obtained results indicate a significant potential of using chitosan as an excipient in modern oral or epidermal drug delivery systems of carvedilol.

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Section: Introductionmentioning

confidence: 99%

Chitosan as Valuable Excipient for Oral and Topical Carvedilol Delivery Systems

Sip

Paczkowska-Walendowska

Rosiak

et al. 2021

Pharmaceuticals

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“…Psychological barriers, on the other hand, are attributed to patient resistance or previous experience with a tablet sticking in the esophagus 6 . As a result, different tablet dosage forms had been developed to overcome swallowing difficulties in which drugs are administrated orally without the need of chewing or prior dispersion or dissolution in water in order to produce a systemic effect like buccal, sublingual and orodispersible tablets (ODTs) 7 .…”

Section: Introductionmentioning

confidence: 99%

New Easily Swallowed Tablets with Slippery Coating for the Antihypertensive Drug Valsartan

Mahdi

Maraie

2015

PBJ

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Different tablet dosage forms were prepared to be administered for patients with dysphagia (swallowing difficulties) like buccal, sublingual and orodispersible tablets, however, they possesses certain constrains like taste masking difficulties, limitations in drug and dose selection and friability. Hence, in an attempt to overcome these constrains, a new easily swallowed immediate release tablets containing (160mg) Valsartan were prepared, and designed to be slippery upon contact with saliva giving an easy swallowing of the intact tablet (without water) with efficient taste masking effect, thus, they called Oroslippery tablets (OSTs). Core tablets were prepared by direct compression using different superdisintegrants, followed by dipping in special coating dispersion containing different proportion of kollicoat IR (film former) and xanthan gum (slipperiness inducer) at different coating levels. These OSTs were optimized for their physical properties, in-vitro disintegration and release in addition to in-vivo slipperiness and taste masking effect. It was found that F12 containing 6% crosscarmellose sodium double coated with 15% kollicoat IR and 0.3% xanthan gum possessed a good mechanical strength (hardness=5.69±0.58 Kg/cm 2 , friability=0.09%±0.79), suitable in-vivo slipperiness and taste masking times (8±1.45 and 58±2.18 seconds) respectively, with longer disintegration time (5.57±1.36 minutes) but similar release profile to the commercial conventional tablet Diovan ® with similarity factor (f2= 68.4±1.07) and difference factor (f1= 1.39± 0.95). Therefore, this study developed a new easily swallowed tablet with an efficient taste masking property, high loading capacity and adequate mechanical strength that can be used as an alternative to buccal, sublingual and orodispersible tablets.

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“…This process depends on the use of complexation between positively charged chitosan and negatively charged TPP by electrostatic forces [ 70 ]. Neither harmful chemicals nor critical operations are required in this process and it is very simple and mild [ 70 ]; thus, this method is one of the most common methods described for the formation of chitosomes in the literature [ 43 , 71 , 72 , 73 ].…”

Section: Resultsmentioning

confidence: 99%

Investigation of the Potential of Nebivolol Hydrochloride-Loaded Chitosomal Systems for Tissue Regeneration: In Vitro Characterization and In Vivo Assessment

et al. 2021

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In this study, we evaluated the synergistic effect of nebivolol hydrochloride (NVH), a third-generation beta-blocker and NO donor drug, and chitosan on the tissue regeneration. Ionic gelation method was selected for the preparation of NVH-loaded chitosomes using chitosan lactate and sodium tripolyphosphate. The effect of different formulation variables was studied using a full factorial design, and NVH entrapment efficiency percentages and particle size were selected as the responses. The chosen system demonstrated high entrapment efficiency (73.68 ± 3.61%), small particle size (404.05 ± 11.2 nm), and good zeta potential value (35.6 ± 0.25 mV). The best-achieved formula demonstrated spherical morphology in transmission electron microscopy and amorphization of the crystalline drug in differential scanning calorimetry and X-ray diffraction. Cell culture studies revealed a significantly higher proliferation of the fibroblasts in comparison with the drug suspensions and the blank formula. An in vivo study was conducted to compare the efficacy of the proposed formula on wound healing. The histopathological examination showed the superiority of NVH-loaded chitosomes on the wound proliferation and the non-significant difference in the collagen deposition after 15 days of the injury to that of intact skin. In conclusion, NVH-loaded chitosomes exhibited promising results in enhancing skin healing and tissue regeneration.

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Nano and Microparticulate Chitosan Based System for Formulation of Carvedilol Rapid Melt Tablet

Cited by 18 publications

References 22 publications

Chitosan as Valuable Excipient for Oral and Topical Carvedilol Delivery Systems

Chitosan as Valuable Excipient for Oral and Topical Carvedilol Delivery Systems

New Easily Swallowed Tablets with Slippery Coating for the Antihypertensive Drug Valsartan

Investigation of the Potential of Nebivolol Hydrochloride-Loaded Chitosomal Systems for Tissue Regeneration: In Vitro Characterization and In Vivo Assessment

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