The use of polymorphic state modifiers in solid lipid microparticles: The role of structural modifications on drug release performance
This study investigates the correlation between the structural and release properties of solid lipid microparticles (MPs) of tristearin containing 5 % w/w of four different liquid additives used as crystal modifiers: isopropyl myristate (IM), ethyl oleate (EO), oleic acid (OA) and medium chain triglycerides (MCT). All additives accelerated the conversion of the unstable α-form of tristearin, formed after the MPs manufacturing, to the stable β-polymorph and the transformation was completed within 24 h (for IM and EO) or 48 h (for OA and MCT). The kinetic of polymorphic transition at 25 °C was investigated by simultaneous...
Source: European Journal of Pharmaceutical Sciences - November 23, 2023 Category: Drugs & Pharmacology Authors: Serena Bertoni Elena Simone Stefano Sangiorgi Beatrice Albertini Nadia Passerini Source Type: research

The use of polymorphic state modifiers in solid lipid microparticles: the role of structural modifications on drug release performance
This study investigates the correlation between the structural and release properties of solid lipid microparticles (MPs) of tristearin containing 5% w/w of four different liquid additives used as crystal modifiers: isopropyl myristate (IM), ethyl oleate (EO), oleic acid (OA) and medium chain triglycerides (MCT). All additives accelerated the conversion of the unstable α-form of tristearin, formed after the MPs manufacturing, to the stable β-polymorph and the transformation was completed within 24 h (for IM and EO) or 48 h (for OA and MCT). The kinetic of polymorphic transition at 25°C was investigated by simultaneous s...
Source: European Journal of Pharmaceutical Sciences - November 23, 2023 Category: Drugs & Pharmacology Authors: Serena Bertoni Elena Simone Stefano Sangiorgi Beatrice Albertini Nadia Passerini Source Type: research

The use of polymorphic state modifiers in solid lipid microparticles: the role of structural modifications on drug release performance
This study investigates the correlation between the structural and release properties of solid lipid microparticles (MPs) of tristearin containing 5% w/w of four different liquid additives used as crystal modifiers: isopropyl myristate (IM), ethyl oleate (EO), oleic acid (OA) and medium chain triglycerides (MCT). All additives accelerated the conversion of the unstable α-form of tristearin, formed after the MPs manufacturing, to the stable β-polymorph and the transformation was completed within 24 h (for IM and EO) or 48 h (for OA and MCT). The kinetic of polymorphic transition at 25°C was investigated by simultaneous s...
Source: European Journal of Pharmaceutical Sciences - November 23, 2023 Category: Drugs & Pharmacology Authors: Serena Bertoni Elena Simone Stefano Sangiorgi Beatrice Albertini Nadia Passerini Source Type: research

Fibrous matrices facilitate pleurocidin killing of wound associated bacterial pathogens
Eur J Pharm Sci. 2023 Nov 20:106648. doi: 10.1016/j.ejps.2023.106648. Online ahead of print.ABSTRACTConventional wound infection treatments neither actively promote wound healing nor address the growing problem of antibacterial resistance. Antimicrobial peptides (AMPs) are natural defense molecules, released from host cells, which may be rapidly bactericidal, modulate host-immune responses, and/or act as endogenous mediators for wound healing. However, their routine clinical use has hitherto been hindered due to their instability in the wound environment. Here we describe an electrospun carrier system for topical applicati...
Source: European Journal of Pharmaceutical Sciences - November 22, 2023 Category: Drugs & Pharmacology Authors: Celia Ramos Kairi Lorenz Marta Putrin š Charlotte K Hind Andres Meos Ivo Laidm äe Tanel Tenson J Mark Sutton A James Mason Karin Kogermann Source Type: research

A comprehensively validated IVRT method reliably discriminates sameness and differences between several topical clotrimazole creams
Eur J Pharm Sci. 2023 Nov 20:106649. doi: 10.1016/j.ejps.2023.106649. Online ahead of print.ABSTRACTIn vitro release testing (IVRT) has gained increasing acceptance for use as a biowaiver for topical products intended for local action. Whereas the United States Food and Drug Administration (US FDA) has issued product specific guidances (PSGs) recommending IVRT for several products, the PSG for clotrimazole cream does not include an IVRT option. However, an important requirement to include supplemental selectivity in the validation process as described in the recent FDA draft guidance on IVRT studies for topical drug produc...
Source: European Journal of Pharmaceutical Sciences - November 22, 2023 Category: Drugs & Pharmacology Authors: Hannah Wellington Seeprarani Rath Isadore Kanfer Source Type: research

Fibrous matrices facilitate pleurocidin killing of wound associated bacterial pathogens
Eur J Pharm Sci. 2023 Nov 20:106648. doi: 10.1016/j.ejps.2023.106648. Online ahead of print.ABSTRACTConventional wound infection treatments neither actively promote wound healing nor address the growing problem of antibacterial resistance. Antimicrobial peptides (AMPs) are natural defense molecules, released from host cells, which may be rapidly bactericidal, modulate host-immune responses, and/or act as endogenous mediators for wound healing. However, their routine clinical use has hitherto been hindered due to their instability in the wound environment. Here we describe an electrospun carrier system for topical applicati...
Source: European Journal of Pharmaceutical Sciences - November 22, 2023 Category: Drugs & Pharmacology Authors: Celia Ramos Kairi Lorenz Marta Putrin š Charlotte K Hind Andres Meos Ivo Laidm äe Tanel Tenson J Mark Sutton A James Mason Karin Kogermann Source Type: research

A comprehensively validated IVRT method reliably discriminates sameness and differences between several topical clotrimazole creams
Eur J Pharm Sci. 2023 Nov 20:106649. doi: 10.1016/j.ejps.2023.106649. Online ahead of print.ABSTRACTIn vitro release testing (IVRT) has gained increasing acceptance for use as a biowaiver for topical products intended for local action. Whereas the United States Food and Drug Administration (US FDA) has issued product specific guidances (PSGs) recommending IVRT for several products, the PSG for clotrimazole cream does not include an IVRT option. However, an important requirement to include supplemental selectivity in the validation process as described in the recent FDA draft guidance on IVRT studies for topical drug produc...
Source: European Journal of Pharmaceutical Sciences - November 22, 2023 Category: Drugs & Pharmacology Authors: Hannah Wellington Seeprarani Rath Isadore Kanfer Source Type: research

In Vitro and In Vivo Evaluation of Dark Chocolate as Age-appropriate Oral Matrix
Eur J Pharm Sci. 2023 Nov 19:106646. doi: 10.1016/j.ejps.2023.106646. Online ahead of print.ABSTRACTSwallowing difficulties encountered by geriatric patients who undergo polypharmacy represent a significant challenge that hampers patient compliance and therapeutic management. As an appealing and sensory-pleasing, chocolate-based formulations have emerged as a potential alternative oral dosage form suitable for both the elderly and paediatric populations. However, the extent to which the incorporation of drugs into a chocolate matrix affects their oral availability remains unclear. Therefore, the objective of this investiga...
Source: European Journal of Pharmaceutical Sciences - November 21, 2023 Category: Drugs & Pharmacology Authors: Aya Y Al-Kabariti Basel T Arafat Ghaleb Ali Oriquat Petra Mo žná Hadeal Jaidy Asma Rehmani Kausar Patel Nidal Al-Qinna Mohamed A Alhnan Source Type: research

Targeting fusion proteins of the interleukin family: a promising new strategy for the treatment of autoinflammatory diseases
Eur J Pharm Sci. 2023 Nov 18:106647. doi: 10.1016/j.ejps.2023.106647. Online ahead of print.ABSTRACTAs a means of communication between immune cells and non-immune cells, Interleukins (ILs) has the main functions of stimulating the proliferation and activation of inflammatory immune cells such as dendritic cells and lymphocytes, promote the development of blood cells and so on. However, dysregulation of ILs expression is a major feature of autoinflammatory diseases. The drugs targeting ILs or IL-like biologics have played an important role in the clinical treatment of autoinflammatory diseases. Nevertheless, the widespread...
Source: European Journal of Pharmaceutical Sciences - November 20, 2023 Category: Drugs & Pharmacology Authors: Yuchen Zhao Han Wang Lin Jin Ziwei Zhang Lianghu Liu Mengqi Zhou Xianzheng Zhang Lingling Zhang Source Type: research

Towards personalized drug delivery via semi-solid extrusion: exploring poly(vinyl alcohol-co-vinyl acetate) copolymers for hydrochlorothiazide-loaded films
This study explored the effect of vinyl alcohol (VA) and vinyl acetate (VAc) monomer ratio on the properties of hydrochlorothiazide (HCT) films. Five copolymers with different VA/VAc ratios were selected and characterized. Semi-solid extrusion was employed as a method for preparation of HCT-PVA/PVAc films to address the challenges of HCT´s low water solubility, high melting point, and low permeability. All copolymers were suitable for semi-solid extrusion, however, the mechanical properties of films with higher VA proportions were more suitable. The drug was found to be homogenously distributed on a micrometer level throu...
Source: European Journal of Pharmaceutical Sciences - November 20, 2023 Category: Drugs & Pharmacology Authors: Karin Korelc Bjarke Str øm Larsen Anna-Lena Heintze Åke Henrik-Klemens Jakob Karlsson Anette Larsson Ingunn Tho Source Type: research

Targeting fusion proteins of the interleukin family: a promising new strategy for the treatment of autoinflammatory diseases
Eur J Pharm Sci. 2023 Nov 18:106647. doi: 10.1016/j.ejps.2023.106647. Online ahead of print.ABSTRACTAs a means of communication between immune cells and non-immune cells, Interleukins (ILs) has the main functions of stimulating the proliferation and activation of inflammatory immune cells such as dendritic cells and lymphocytes, promote the development of blood cells and so on. However, dysregulation of ILs expression is a major feature of autoinflammatory diseases. The drugs targeting ILs or IL-like biologics have played an important role in the clinical treatment of autoinflammatory diseases. Nevertheless, the widespread...
Source: European Journal of Pharmaceutical Sciences - November 20, 2023 Category: Drugs & Pharmacology Authors: Yuchen Zhao Han Wang Lin Jin Ziwei Zhang Lianghu Liu Mengqi Zhou Xianzheng Zhang Lingling Zhang Source Type: research

Towards personalized drug delivery via semi-solid extrusion: exploring poly(vinyl alcohol-co-vinyl acetate) copolymers for hydrochlorothiazide-loaded films
This study explored the effect of vinyl alcohol (VA) and vinyl acetate (VAc) monomer ratio on the properties of hydrochlorothiazide (HCT) films. Five copolymers with different VA/VAc ratios were selected and characterized. Semi-solid extrusion was employed as a method for preparation of HCT-PVA/PVAc films to address the challenges of HCT´s low water solubility, high melting point, and low permeability. All copolymers were suitable for semi-solid extrusion, however, the mechanical properties of films with higher VA proportions were more suitable. The drug was found to be homogenously distributed on a micrometer level throu...
Source: European Journal of Pharmaceutical Sciences - November 20, 2023 Category: Drugs & Pharmacology Authors: Karin Korelc Bjarke Str øm Larsen Anna-Lena Heintze Åke Henrik-Klemens Jakob Karlsson Anette Larsson Ingunn Tho Source Type: research

A randomized double-blind phase Ib clinical trial of SY-009 in patients with type 2 diabetes mellitus
CONCLUSION: Plasma exposure of SY-009 and its metabolites was fairly low in T2DM patients at doses of 1.0-4.0 mg. SY-009 reduced postprandial glucose, C-peptide, and insulin levels, showing relative safety and tolerability in the dose range of 1.0-4.0 mg.TRIALS REGISTRATION: ClinicalTrials.gov Identifier: NCT04345107.PMID:37981049 | DOI:10.1016/j.ejps.2023.106644 (Source: European Journal of Pharmaceutical Sciences)
Source: European Journal of Pharmaceutical Sciences - November 19, 2023 Category: Drugs & Pharmacology Authors: Lei Huang Bei Cao Yan Geng Xiaoli Zhou Yuanxun Yang Tingting Ma Hui Lin Zhijiang Huang Lang Zhuo Juan Li Source Type: research

A randomized double-blind phase Ib clinical trial of SY-009 in patients with type 2 diabetes mellitus
CONCLUSION: Plasma exposure of SY-009 and its metabolites was fairly low in T2DM patients at doses of 1.0-4.0 mg. SY-009 reduced postprandial glucose, C-peptide, and insulin levels, showing relative safety and tolerability in the dose range of 1.0-4.0 mg.TRIALS REGISTRATION: ClinicalTrials.gov Identifier: NCT04345107.PMID:37981049 | DOI:10.1016/j.ejps.2023.106644 (Source: European Journal of Pharmaceutical Sciences)
Source: European Journal of Pharmaceutical Sciences - November 19, 2023 Category: Drugs & Pharmacology Authors: Lei Huang Bei Cao Yan Geng Xiaoli Zhou Yuanxun Yang Tingting Ma Hui Lin Zhijiang Huang Lang Zhuo Juan Li Source Type: research

Do the enantiomers of ketamine bind enantioselectively to human serum albumin?
Eur J Pharm Sci. 2023 Nov 17:106640. doi: 10.1016/j.ejps.2023.106640. Online ahead of print.ABSTRACTThe binding of drugs to plasma proteins is an important process in the human body and has a significant influence on pharmacokinetic parameter. Human serum albumin (HSA) has the most important function as a transporter protein. The binding of ketamine to HSA has already been described in literature, but only of the racemate. The enantiomerically pure S-ketamine is used as injection solution for induction of anesthesia and has been approved by the Food and Drug Administration for the therapy of severe depression as a nasal sp...
Source: European Journal of Pharmaceutical Sciences - November 18, 2023 Category: Drugs & Pharmacology Authors: Sebastian Schmidt Ulrike Holzgrabe Source Type: research