Dissolution improvement of nebivolol hydrochloride using solid dispersion adsorbate technique

Shah, Harsh; Shah, Vidip; Bhutani, Shital; Parikh, Dhaivat; Mehta, Tejal

doi:10.4103/0973-8398.150039

Cited by 14 publications

(9 citation statements)

References 31 publications

(31 reference statements)

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“…In other words, the diminishing of certain drug peaks in the XRD of the formulation, compared with the NVH:CSL physical mixture, and NVH pure drug could indicate the conversion of NVH from the crystalline state to the amorphous state in the optimal NVH-loaded chitosomes (F6). This could be due to the encapsulation of NVH inside the optimal formula in amorphous form [ 95 , 98 ].…”

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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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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“…The SDs containing 75 mg of CPG dissolved in 5 mL dissolution media, followed by filtration through a filter (0.45 μ) at varying time intervals suitably diluted and assayed at 240 nm, and the drug release was compared with the marketed formulation. [19,20]…”

Section: In Vitro Drug Dissolution Of Cpg Sdmentioning

confidence: 99%

Enhancement of Solubility And Dissolution Profile of Clopidogrel By Various Solid Dispersion Formulations

Khader

Salfi

2020

Int. J. Pharm. Sci. Drug Res.

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The present research is aimed at enhancing solubility and drug dissolution of clopidogrel (CPG) used as oral antiplatelet agent by employing solid dispersion (SD) technique. Total 40 SDs formulated with drug: polymers (pluronic F127, poloxamer 407, labrafil PG, PEG 6000, gelucire 50/13), in varying ratios (1:0.5, 1:1, 1:2, 1:3, 1:4) of which CPG1 to CPG20 and CPG21 to CPG40 prepared by adopting solvent evaporation method fusion (melt) method respectively. The formulation CPG40 containing pluronic F127 as polymer showed highest solubility of 6.57±0.04 mg/ml) that is 45 folds than pure drug. Similar results reflected in the dissolution studies where CPG40 containing CPG: pluronic F127 in 1:4 ratio showed maximum % drug content, % practical yield and drug dissolution of 99.14% in 60 minutes when compared with other formulations and pure drug (32.76%) obtained by fusion melt method. From FTIR studies the optimized formulation CPG40 showed the compatibility between drug and polymers. XRD and SEM studies showed CPG40 exists in amorphous form that fetched in better drug release from the SD formulation in comparison to pure drug.

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“…The amount of carriers used was within IIG limits. The SDAs were then passed through sieve #40 ASTM to obtain free flowing powder of uniform size 18 . FTIR spectra of FEB, SDA of batch FEB7 and LLT (blank formulation without drug) were obtained using Shimadzu Biorad FT-IR system (Kyoto, Japan).…”

Section: Preparation Of Solid Dispersion Adsorbate (Sda)mentioning

confidence: 99%

Untitled

2015

IJPSR

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The objective of the present investigation was to improve dissolution characteristics of febuxostat, a BCS class-II drug, by formulating it as solid dispersion adsorbate. Solid dispersion adsorbate(SDA) was prepared using labrasol, transcutol and lutrol F127 as carriers and neusilin as adsorbent. Formulation was prepared using combination of melt and adsorption technique. Optimized formulation was characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and X-ray diffraction (XRD). In-vitro dissolution profile was compared with the marketed product. SDA comprising of febuxostat, neuslin and the three carriers in a ratio of 1:2:4 was considered as optimized formulation. FTIR spectroscopy revealed intermolecular hydrogen bonding with neusilin. DSC scan showed absence of melting peak of febuxostat, which indicates solubilization of drug in carriers and conversion of crystalline to amorphous form. This point was further confirmed by XRD. The percentage yield obtained was 90% and there was 10% increase in the dissolution rate of the optimized formulation compared to the marketed product. The dissolution efficiency was found to be 37% of the optimized formulation. Significant increase in the dissolution characteristics of febuxostat was noticed. The enhancement in dissolution rate of febuxostat can be due to hydrogen bonding between the drug and neusilin, micellar solubilisation of drug in carrier, improved wettability and amorphization as confirmed by FTIR, DSC and XRD studies. The results indicated that the SDA is a promising approach for the dissolution enhancement of febuxostat and can be used for the development of suitable solid dosage form for commercialization.

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Dissolution improvement of nebivolol hydrochloride using solid dispersion adsorbate technique

Cited by 14 publications

References 31 publications

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

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

Enhancement of Solubility And Dissolution Profile of Clopidogrel By Various Solid Dispersion Formulations

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