Use of a temperature ramp approach (TRA) to design an optimum and robust freeze-drying process for pharmaceutical formulations

Assegehegn, Getachew; Fuente, Edmundo Brito-de la; Franco, J.M.; Gallegos, C.

doi:10.1016/j.ijpharm.2020.119116

Cited by 9 publications

(6 citation statements)

References 62 publications

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“…T′g value obtained by DSC analysis for Lip + L + M + A was considered for selecting the target product temperature during primary drying ( target T p ). The ramp temperature approach previously described by Assegehegn et al [ 31 ] was applied to select the fluid temperature (T f ) and the duration of primary drying. The first experiment was performed under the following conditions: freezing temperature at −60 °C, primary drying at −30 °C for 24 h and secondary drying for 12 h at 10 °C followed by 6 h at 18 °C.…”

Section: Methodsmentioning

confidence: 99%

“…T g value obtained by DSC analysis for Lip + L + M + A was considered for selecting the target product temperature during primary drying (target T p ). The ramp temperature approach previously described by Assegehegn et al [31] was applied to select the fluid temperature (T f ) and the duration of primary drying. The first experiment was performed under the following conditions: freezing temperature at −60 • C, primary drying at −30 • C for 24 h and secondary drying for 12 h at 10 • C followed by 6 h at 18 • C. Another run was performed under the following conditions: freezing temperature at −45 • C, staggered temperatures (−25 • C, −22 • C, −20 • C and −17 • C) for 4 h each for primary drying and secondary drying for 12 h at 15 • C. A third run was performed under the following conditions: freezing temperature at −40 • C, primary drying at −17 • C for 24 h preceded by 2 h at −20 • C and secondary drying for 18 h at 17 • C. A pressure of 100 µBar was selected for the first period of primary drying (4 h) and 25 µBar for the rest of the process.…”

Section: Optimization Of the Freeze-drying Processmentioning

confidence: 99%

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Development of a Mucoadhesive Vehicle Based on Lyophilized Liposomes for Drug Delivery through the Sublingual Mucosa

et al. 2022

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A pharmaceutical vehicle based on lyophilized liposomes is proposed for the buccal administration of drugs aimed at systemic delivery through the sublingual mucosa. Liposomes made of egg phosphatidylcholine and cholesterol (7/3 molar ratio) were prepared and lyophilized in the presence of different additive mixtures with mucoadhesive and taste-masking properties. Palatability was assayed on healthy volunteers. The lyophilization cycle was optimized, and the lyophilized product was compressed to obtain round and capsule-shaped tables that were evaluated in healthy volunteers. Tablets were also assayed regarding weight and thickness uniformities, swelling index and liposome release. The results proved that lyophilized liposomes in unidirectional round tablets have palatability, small size, comfortability and buccal retention adequate for sublingual administration. In contact with water fluids, the tablets swelled, and rehydrated liposomes were released at a slower rate than permeation efficiency determined using a biomimetic membrane. Permeability efficiency values of 0.72 ± 0.34 µg/cm2/min and 4.18 ± 0.95 µg/cm2/min were obtained for the liposomes with and without additives, respectively. Altogether, the results point to the vehicle proposed as a liposomal formulation suitable for systemic drug delivery through the sublingual mucosa.

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Section: Methodsmentioning

confidence: 99%

Section: Optimization Of the Freeze-drying Processmentioning

confidence: 99%

Development of a Mucoadhesive Vehicle Based on Lyophilized Liposomes for Drug Delivery through the Sublingual Mucosa

et al. 2022

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“…Approximately 2 mg of crushed cake were crimped into aluminum crucibles and sealed hermetically. Samples were scanned from 25 °C to 150 °C at a ramp rate of 10 °C/min, as previously reported by Assegehegn et al with a slight modification (Assegehegn et al., 2020 ). The DSC thermogram of the lyophilizate were inspected for occurrence of crystallization exotherms and endothermic transitions indicative of glass transition temperature (Tg) of the lyophilizate.…”

Section: Methodsmentioning

confidence: 99%

“…The DSC thermogram of the lyophilizate were inspected for occurrence of crystallization exotherms and endothermic transitions indicative of glass transition temperature (Tg) of the lyophilizate. The Tg was determined as the midpoint of the endothermic transition using Origin, 2021, OriginLab Corporation, Northampton, MA, USA (Assegehegn et al., 2020 ).…”

Section: Methodsmentioning

confidence: 99%

Chitosan-dipotassium orthophosphate lyophilizate: a novel in situ thermogel carrier system of allogeneic platelet lysate growth factors

et al. 2022

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The clinical success of platelet-rich plasma (PRP) is constrained by its limited mechanical strength, rapid disintegration by lytic enzymes, and the consequent short-term release of bioactive growth factors (GFs). Recently, attempts to formulate PRP and other hemoderivatives, such as platelet lysate (PL) have been underway. The current study aimed to formulate allogeneic freeze-dried human platelet lysate (HPL) onto lyophilized chitosan - dipotassium hydrogen orthophosphate (CS/DHO) thermo-sensitive scaffolds. A systemic approach was employed to optimize freeze-drying (FD) procedures targeting predefined critical quality attributes (CQAs). Thermal behavior, vibrational spectroscopy, morphological and moisture content analyses were used to detect possible protein destabilization during formulation and suboptimal cake properties. The effect of CS/DHO concentrations on thermo-responsiveness and release kinetics were investigated. Finally, six-months stability and cytotoxicity studies were carried out. An optimized lyophilizate was attainable with residual moisture of less than 5% and thermoresponsive to 33 °C in less than 3 min. HPL proteins were sustainedly released over five days in a pH-sensitive manner. The stability study indicated plausible physical and biochemical stability. Cell viability testing supported the cytocompatibility of the system. Finally, the lyophilizate variant of CS/DHO thermogel overcomes limited storage stability previously posed as a challenge in freshly prepared thermogels. The developed system overcomes the drawbacks of currently used PRP treatment and provides a novel GF-rich scaffold for wound repair.

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“…During the freezing stage, most of the water is converted into a solid, where ice crystal networks are formed. It is at this stage that the morphology of materials, the size and the size distribution of the ice crystals are determined, which in turn influence several critical parameters, such as dry product resistance, primary and secondary drying rates, extent of product crystallinity, surface area, and dry product reconstitutability (39)(40)(41).…”

Section: Freeze-dryingmentioning

confidence: 99%

Methods of Microencapsulation of Vegetable Oil: Principles, Stability and Applications - A Minireview

Silva

Castelo

Cheng

et al. 2022

Food Technol. Biotechnol. (Online)

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In addition to being used in food, fuel, and lubricants, vegetable oils are promising in many other applications such as food additives, nutritional supplements, cosmetics, and biomedicine; however, their low oxidative stability can limit their use. Microencapsulation is a well-established methodology for the preservation of oils against degradation, controlled release of active ingredients, protection against external factors during storage, and enhanced durability. In this article, microencapsulation methods for vegetable oils are reviewed, including physical methods (spray drying and freeze-drying), physical-chemical methods (complex coacervation, ionic gelation and electrostatic layer-by-layer deposition), and chemical methods (interfacial/in situ polymerization). This article also provides information on the principles, parameters, advantages, disadvantages, and applications of these methods.

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Use of a temperature ramp approach (TRA) to design an optimum and robust freeze-drying process for pharmaceutical formulations

Cited by 9 publications

References 62 publications

Development of a Mucoadhesive Vehicle Based on Lyophilized Liposomes for Drug Delivery through the Sublingual Mucosa

Development of a Mucoadhesive Vehicle Based on Lyophilized Liposomes for Drug Delivery through the Sublingual Mucosa

Chitosan-dipotassium orthophosphate lyophilizate: a novel in situ thermogel carrier system of allogeneic platelet lysate growth factors

Methods of Microencapsulation of Vegetable Oil: Principles, Stability and Applications - A Minireview

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