23 Full factorial design for optimization of stable amorphous host–guest-based mirabegron complex for extended-release action

Mandpe, Pankaj; Prabhakar, Bala; Shende, Pravin

doi:10.1007/s10847-019-00955-1

Cited by 6 publications

(3 citation statements)

References 26 publications

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“…Viewing the in vitro release profiles, these drug behaviors by the formulations have been previously obtained by other authors [77]. As expected, AczHP-L delayed the Acz release compared to AczHP-S in which the release of Acz was more pronounced [92,93]. The same behavior was observed with the CLL batch, especially in the first stage, in which the release rate of Acz was more noticeable in the CLL formulation than AczHP-L.…”

Section: Discussionsupporting

confidence: 78%

Synergistic Effect of Acetazolamide-(2-hydroxy)propyl β-Cyclodextrin in Timolol Liposomes for Decreasing and Prolonging Intraocular Pressure Levels

et al. 2021

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The purpose of this study was to design, for the first time, a co-loaded liposomal formulation (CLL) for treatment of glaucoma including timolol maleate (TM) in the lipid bilayer and acetazolamide (Acz)-(2-hydroxy)propyl β-cyclodextrin (HPβCD) complexes (AczHP) solubilized in the aqueous core of liposomes. Formulations with TM (TM-L) and AczHP (AczHP-L), separately, were also prepared and characterized. A preliminary study comprising the Acz/HPβCD complexes and their interaction with cholesterol (a component of the lipid bilayer) was realized. Then, a screening study on formulation factors affecting the quality of the product was carried out following the design of the experiment methodology. In addition, in vitro release and permeation studies and in vivo lowering intraocular pressure (IOP) studies were performed. The results of the inclusion complexation behavior, characterization, and binding ability of Acz with HPβCD showed that HPβCD could enhance the water solubility of Acz despite the weak binding ability of the complex. Ch disturbed the stability and solubility parameters of Acz due to the fact of its competence by CD; thus, Chems (steroid derivative) was selected for further liposome formulation studies. The optimization of the lipid bilayer composition (DDAB, 0.0173 mmol and no double loading) and the extrusion as methods to reduce vesicle size were crucial for improving the physico-chemical properties and encapsulation efficiency of both drugs. In vitro release and permeation studies demonstrated that the CLL formulation showed improvement in in vitro drug release and permeation compared to the liposomal formulations with a single drug (TM-L and AczHP-L) and the standard solutions (TM-S and AczHP-S). CLL showed high efficacy in reducing and prolonging IOP, suggesting that the synergistic effect of TM and Acz on aqueous humor retention and the presence of this cyclodextrin and liposomes as permeation enhancers are responsible for the success of this strategy of co-loading for glaucoma therapy.

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Section: Discussionsupporting

confidence: 78%

Synergistic Effect of Acetazolamide-(2-hydroxy)propyl β-Cyclodextrin in Timolol Liposomes for Decreasing and Prolonging Intraocular Pressure Levels

et al. 2021

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“…In the case of TBPB, the absorption peak at 3,133.56 cm −1 , 2,900 cm −1 , 1,372 cm −1 and 690–528 cm −1 were attributed to the stretching vibrations of OH, C–H and C–Br groups, respectively. Small but significant shifts of peaks and discrete variations of their relative intensities were observed for the blank and dye-loaded cyclodextrin dispersion, suggesting a host–guest interaction (Mandpe et al , 2020).…”

Section: Resultsmentioning

confidence: 99%

Impregnation of dye-conjugated miniaturized system on paper strip for detection of biomarker in renal cancer

Takke

Shende²

2022

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Purpose The purpose of this study was to design a paper strip-based non-invasive urine analysis system for the qualitative detection of biomarker aquaporin-1 (AQP1) in renal cancer (RC). RC accounts for 3% of all cancers and 85% of all kidney tumors and mainly originates from the kidney cortex. In recent times, higher urine concentration of AQP1 in patients with RC was confirmed as a specific biomarker of the disease. Hence, the noninvasive, user-friendly and self-diagnostic method is required for the detection of aquaporin biomarkers in RC. Design/methodology/approach The present research work was focused on the development and characterization of a dye conjugated cyclodextrin-based miniaturized system for impregnation on Whatman filter paper to identify RC using AQP1 biomarker present in urine samples. Findings It was observed that the test strip dipped into the urine sample, and the yellow color intensity increased with a decrease in AQP1 concentration due to the transformation of the dye system of free basic form into bound acidic form. The Hue-Saturation-Value profiling was used to observe the effect of color change using a smartphone application. The paper strip-based urine analysis system is highly sensitive for the detection of AQP1 in the range of 10 to 1,000 ng. Originality/value The successful validation indicated that this biosensor is likely to contribute to the development of point-of-care, novel, personalized diagnostics and ensure prolonged survival of RC patients in the near future.

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“…Of note, inclusion cocrystals are a specific form of cocrystals that are based host-guest inclusion between guest drug molecules and host co-formers (typically cyclodextrin). This differs from the commonly employed solubilization approach using cyclodextrin-based inclusion complexes, where the resulting product is in an amorphous state with excess cyclodextrins [ 19 , 20 ]. Apart from the host-guest interaction, the formation of inclusion cocrystals involves various intermolecular forces, including hydrogen bonds and van der Waals forces [ 16 ].…”

Section: Introductionmentioning

confidence: 99%

Asiatic acid cyclodextrin inclusion micro-cocrystal for insoluble drug delivery and acute lung injury therapy enhancement

Shen,

Pan,

Ning

et al. 2024

J Nanobiotechnol

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Background Acute lung injury (ALI) is a fatal respiratory disease caused by overreactive immune reactions (e.g., SARS-CoV-2 infection), with a high mortality rate. Its treatment is often compromised by inefficient drug delivery barriers and insufficient potency of the currently used drugs. Therefore, developing a highly effective lung-targeted drug delivery strategy is a pressing clinical need. Results In this study, the micro-sized inclusion cocrystal of asiatic acid/γ-cyclodextrin (AA/γCD, with a stoichiometry molar ratio of 2:3 and a mean size of 1.8 μm) was prepared for ALI treatment. The dissolution behavior of the AA/γCD inclusion cocrystals followed a “spring-and-hover” model, which meaned that AA/γCD could dissolve from the cocrystal in an inclusion complex form, thereby promoting a significantly improved water solubility (nine times higher than free AA). This made the cyclodextrin-based inclusion cocrystals an effective solid form for enhanced drug absorption and delivery efficiency. The biodistribution experiments demonstrated AA/γCD accumulated predominantly in the lung (Cmax = 50 µg/g) after systemic administration due to the micron size-mediated passive targeting effect. The AA/γCD group showed an enhanced anti-inflammatory therapeutic effect, as evidenced by reduced levels of pro-inflammatory cytokines in the lung and bronchoalveolar lavage fluids (BALF). Histological examination confirmed that AA/γCD effectively inhibited inflammation reactions. Conclusion The micro-sized inclusion cocrystals AA/γCD were successfully delivered into the lungs by pulmonary administration and had a significant therapeutic effect on ALI. Graphic abstract

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23 Full factorial design for optimization of stable amorphous host–guest-based mirabegron complex for extended-release action

Cited by 6 publications

References 26 publications

Synergistic Effect of Acetazolamide-(2-hydroxy)propyl β-Cyclodextrin in Timolol Liposomes for Decreasing and Prolonging Intraocular Pressure Levels

Synergistic Effect of Acetazolamide-(2-hydroxy)propyl β-Cyclodextrin in Timolol Liposomes for Decreasing and Prolonging Intraocular Pressure Levels

Impregnation of dye-conjugated miniaturized system on paper strip for detection of biomarker in renal cancer

Asiatic acid cyclodextrin inclusion micro-cocrystal for insoluble drug delivery and acute lung injury therapy enhancement

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