Solid dispersion of β-lapachone in PVP K30 and PEG 6000 by spray drying technique

Santos, Klécia M.; Barbosa, Raquel de Melo; Meirelles, Lyghia Maria Araújo; Vargas, Fernanda Grace A.; Lins, Antônio Cláudio da Silva; Câmara, Celso A.; Aragão, Cícero Flávio Soares; Moura, Tulio Flavio de Lima; Raffin, Fernanda Nervo

doi:10.1007/s10973-020-10473-9

Cited by 7 publications

(3 citation statements)

References 42 publications

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“…Spray drying is a typical encapsulation technique for bioactive substances in polymers. , It is based on atomizing a solution into droplets and drying them in gas at high temperatures to produce dry particles. During drying, base materials including PVP form stable complexes with core materials through intermolecular interactions. , Several spray dryer operating parameters are known to affect complex formation, such as inlet air temperature and feed flow rate. , In this study, to understand the suitable spray drying conditions for the encapsulation of carotenoids in PVP, the effects of carotenoid and PVP feed ratio, inlet air temperature, feed flow rate, and PVP average molecular weight on the carotenoid concentration encapsulated in PVP, E / Z -isomer ratio of encapsulated carotenoid, and mean particle size of the resulting complexes were evaluated (Figure ). The evaluation was performed using astaxanthin treated by the heated flow reactor.…”

Section: Resultsmentioning

confidence: 99%

Formation and Characterization of Z-Isomer-Enriched Carotenoid-Loaded Microparticles with Poly(vinylpyrrolidone) Using a Spray Drying Technique

Honda,

Zhang,

Kageyama

et al. 2023

Ind. Eng. Chem. Res.

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Carotenoid Z-isomers exhibit higher bioavailability and potentially beneficial biological activities than their all-Eisomers, which predominate in nature. However, they are chemically unstable and poorly soluble in water, which hinder the practical use of Z-isomer-enriched carotenoid materials. Encapsulating carotenoid Z-isomers in water-soluble carriers can overcome these problems. Here, we successfully prepared Zisomer-enriched carotenoids (lycopene, β-carotene, and astaxanthin)/poly(vinylpyrrolidone) (PVP, a water-soluble polymer) inclusion complexes using a continuous-flow system which is constituted of a heated flow reactor and a spray dryer. Processing in the flow reactor at 200 °C for 15 s prior to spray drying improved the total Z-isomer ratio of the encapsulated carotenoids (>55%) and encapsulation efficiency of carotenoids in PVP. Furthermore, storage tests of the resulting complexes demonstrated that formulating (Z)-carotenoids with PVP stabilized their Z-structures. The results of this study contribute to the realization of industrial applications of Z-isomer-enriched carotenoids with great utility and health benefits.

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Section: Resultsmentioning

confidence: 99%

Formation and Characterization of Z-Isomer-Enriched Carotenoid-Loaded Microparticles with Poly(vinylpyrrolidone) Using a Spray Drying Technique

Honda,

Zhang,

Kageyama

et al. 2023

Ind. Eng. Chem. Res.

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“…The main objective of the present study is to explore the concept of mixed solvency to formulate the solid dispersion of model drug, amlodipine besylate and also to propose mixed solvency concept as a tool to overcome the situation of limiting resources to increase solubility of poorly soluble substances. [19][20][21][22] As per mixed solvency concept, each and every substance present on earth has solubilizing power. A concentrated aqueous solution containing various water-soluble substances may act as good solvent for PWS drugs.…”

Section: Discussionmentioning

confidence: 99%

Untitled

2023

AJP

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Introduction:In recent generation, the difficult task is to overcome solubility problems in the formulation development of the drug. The lower water solubility of drugs causes various challenges in developing formulations and the use of harmful organic solvents produces toxicity. So, this problem is overcome by the mixed solvency concept proposed by Dr R.K. Maheshwari in 2009. In this work, amlodipine besylate was chosen as a model drug and solubilizers selected were sodium benzoate, sodium acetate, sodium citrate, sodium caprylate, poloxamer 407, l-lysine, β-cyclodextrins and niacinamide. The solid dispersions are proposed to be formulated using these expectedly safe water-soluble additives as per mixed solvency concept. Materials and Methods: Solid dispersions were prepared using solvent evaporation method, amlodipine besylate was chosen as a model drug and solubilizers selected were sodium benzoate, sodium acetate, sodium citrate, sodium caprylate, poloxamer 407, l-lysine, β-cyclodextrins and niacinamide. The amlodipine besylate used for the preparation of solid dispersion was characterized and identified by UV spectrophotometric analysis, melting range determination and comparative dissolution studies. Results and Discussions: The amlodipine besylate used for the preparation of solid dispersion was characterized and identified by UV spectrophotometric analysis and melting range determination. The observed values were in accordance with the reported values in the literatures. For pre-formulation studies, the solubility studies of the drug were done in different blends. Also, calibration curves in water and 0.1N HCl were prepared. Interaction studies of drug-solubilizers have shown no interaction and incompatibility between drugs and solubilizers. Solubility of amlodipine besylate drug sample was reported in different blends. UV spectrophotometric study of drugs and solubilizers indicated no drug-solubilizer interference at 368 nm. Different blends of solubilizers were prepared by varying their concentrations. Out of these prepared blends, blend V, blend O and blend C were selected on the basis of the drug solubility at 80-90. Different solid dispersions were prepared with different drug and solubilizers ratios. One of three trail batches of solid dispersions were selected for comparative dissolution studies. The formulated solid dispersions were compared with marketed tablet (tablet powder) and pure drug. Summary and Conclusion: The main objective of the present study is to explore the concept of mixed solvency to formulate the solid dispersion of model drug, amlodipine besylate and also to propose mixed solvency concept as a tool to overcome the situation of limiting resources to increase solubility of poorly soluble substances. The drug content and drug release studies were assessed. Based on the above findings, it may be concluded that the solubility and release of a poorly water-soluble drug can be enhanced using various

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“…Chen Zhen et al concluded that poloxamerbased CSDs are able to simultaneously regulate crystallite size, crystal morphology, and crystallization rate, which is a remarkably promising capability in the improvement of dissolution of oral formulations [26]. Intermolecular interactions are believed to affect drug solubility by altering drug crystallite size [27,28]. The interactions between drugs and polymers mainly occur through hydrogen bonding [29], coupling [30], and acid-base interactions [31], with hydrogen bonding being the most common [32].…”

Section: Introductionmentioning

confidence: 99%

Influence of Intermolecular Interactions on Crystallite Size in Crystalline Solid Dispersions

Huang,

Zhang,

Liu

et al. 2023

Pharmaceutics

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Crystalline solid dispersions (CSDs) represent a thermodynamically stable system capable of effectively reducing the crystallite size of drugs, thereby enhancing their solubility and bioavailability. This study uses flavonoid drugs with the same core structures but varying numbers of hydroxyl groups as model drugs and poloxamer 188 as a carrier to explore the intrinsic relationships between drug–polymer interactions, crystallite size, and in vitro dissolution behavior in CSDs. Initially, we investigate the interactions between flavonoid drugs and P188 by calculating Hansen solubility parameters, determination of Flory–Huggins interaction parameters, and other methods. Subsequently, we explore the crystallization kinetics of flavonoid drugs and P188 in CSD systems using polarized optical microscopy and powder X-ray diffraction. We monitor the domain size and crystallite size of flavonoids in CSDs through powder X-ray diffraction and a laser-particle-size analyzer. Finally, we validate the relationship between crystallite size and in vitro dissolution behavior through powder dissolution. The results demonstrate that, as the number of hydroxyl groups increases, the interactions between drugs and polymers become stronger, making drug crystallization in the CSD system less likely. Consequently, reductions in crystalline domain size and crystallite size become more pronounced, leading to a more significant enhancement in drug dissolution.

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Solid dispersion of β-lapachone in PVP K30 and PEG 6000 by spray drying technique

Cited by 7 publications

References 42 publications

Formation and Characterization of Z-Isomer-Enriched Carotenoid-Loaded Microparticles with Poly(vinylpyrrolidone) Using a Spray Drying Technique

Formation and Characterization of Z-Isomer-Enriched Carotenoid-Loaded Microparticles with Poly(vinylpyrrolidone) Using a Spray Drying Technique

Untitled

Influence of Intermolecular Interactions on Crystallite Size in Crystalline Solid Dispersions

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