QbD based development of proliposome of lopinavir for improved oral bioavailability

Patel, Grishma M.; Shelat, Pragna K.; Lalwani, Anita

doi:10.1016/j.ejps.2016.08.057

Cited by 61 publications

(30 citation statements)

References 37 publications

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“…The use of unsaturated lipids was shown to have a similar effect, the unsaturated lipids forming pockets inside the lipid bilayer where lipophilic drugs can be entrapped [50]. By increasing lipid-to-drug ratio from 1:1 to 10:1, the EE of ritonavir, a lipophilic drug, was doubled from 45 to 90% [43]. The ratio between phospholipid concentration and drug concentration was demonstrated to have a significant impact on EE in the case of simvastatin.…”

Section: Drug Contentmentioning

confidence: 96%

“…Regarding the lipids, their physicochemical characteristics are also important. For example, lipids that contain unsaturated fatty acids are predisposed to degradation reactions like oxidation or hydrolysis and those which contain saturated fatty acids have a higher transition temperature (T m ) [43]. Another specific characteristic of lipids is their chain length.…”

Section: The Critical Materials Attributes and Critical Process Paramementioning

confidence: 99%

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Pharmaceutical Development of Liposomes Using the QbD Approach

Porfire¹,

Achim²,

Barbălată³

et al. 2019

Liposomes - Advances and Perspectives

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Quality by Design (QbD) is a systematic, risk-based approach to pharmaceutical product and manufacturing development, which uses quality-improving scientific methods upstream in the research, development, and design phases, in order to assure that quality and safety are designed into product at as early stage as possible. This work focuses on the state-of-the-art applications of the QbD principles in the development of liposomes. The QbD approach has recently been proposed as a useful tool to obtain higher-quality liposomal products, as their development is a challenging task, involving intricate formulation and manufacturing processes. Thus, the current strategies to define the relationship between the critical material attributes or process parameters and product critical quality attributes and to establish the design space are overviewed. Additionally, the current characterization methodologies are described, as part of the control strategy required within the QbD paradigm.

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Section: Drug Contentmentioning

confidence: 96%

Section: The Critical Materials Attributes and Critical Process Paramementioning

confidence: 99%

Pharmaceutical Development of Liposomes Using the QbD Approach

Porfire¹,

Achim²,

Barbălată³

et al. 2019

Liposomes - Advances and Perspectives

View full text Add to dashboard Cite

show abstract

“…Lipidbased drug delivery systems are considered a promising formulation strategy as well. Solid phospholipid dispersions (SPDs), also termed "proliposomes" (Hiremath et al, 2009, Patel et al, 2017, are of great interest as they may combine the advantages of ASDs, the amorphous solid state of the drug substance, with the solubilization potential of lipid based-formulations, as recently hypothesized by Fong (Fong et al, 2016). The mechanism of oral bioavailability enhancement via phospholipid-based formulations is, however, controversially debated.…”

Section: Introductionmentioning

confidence: 99%

A dynamic in vitro permeation study on solid mono- and diacyl-phospholipid dispersions of celecoxib

Jacobsen

Elvang

Bauer‐Brandl

et al. 2019

European Journal of Pharmaceutical Sciences

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“…Even though lopinavir is marketed as a fixed-dose combination tablet with sub-therapeutic dose of ritonavir, there has been a need for ritonavir-free formulation because ritonavir has adverse effects such as glucose intolerance, gastrointestinal intolerance, lipid elevation and perioral paresthesia. Patel et al developed pro-liposomal formulations for lopinavir based on the quality-by-design approach [44]. Their optimized pro-liposomes for lopinavir consisted of 3.75 µmol of lipid mixture (HSPC:CH 7:3), lopinavir at a ratio of lipid:drug 8.9:1 and 2250 mg of spray-dried mannitol.…”

Section: Lopinavirmentioning

confidence: 99%

Liposomes for Enhanced Bioavailability of Water-Insoluble Drugs: In Vivo Evidence and Recent Approaches

Lee

2020

Pharmaceutics

189

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It has been known that a considerable number of drugs in clinical use or under development are water-insoluble drugs with poor bioavailability (BA). The liposomal delivery system has drawn attention as one of the noteworthy approaches to increase dissolution and subsequently absorption in the gastrointestinal (GI) tract because of its biocompatibility and ability to encapsulate hydrophobic molecules in the lipid domain. However, there have been several drawbacks, such as structural instability in the GI tract and poor permeability across intestinal epithelia because of its relatively large size. In addition, there have been no liposomal formulations approved for oral use to date, despite the success of parenteral liposomes. Nevertheless, liposomal oral delivery has resurged with the rapid increase of published studies in the last decade. However, it is discouraging that most of this research has been in vitro studies only and there have not been many water-insoluble drugs with in vivo data. The present review focused on the in vivo evidence for the improved BA of water-insoluble drugs using liposomes to resolve doubts raised concerning liposomal oral delivery and attempted to provide insight by highlighting the approaches used for in vivo achievements.Pharmaceutics 2020, 12, 264 2 of 30 However, there have been several drawbacks to be overcome, such as instability in the GI tract and poor permeability across the intestinal epithelia because of liposomes' relatively large size [8]. Moreover, it seemed that liposomal oral delivery was faltering during 1980s due to some disappointing results for insulin [9]. However, liposomal oral delivery resurged with a rapid increase in the number of papers published, as shown in Pubmed search results, mainly due to various advanced modification technologies, even though liposomal oral delivery-related papers account for only 5-6% of the total number of liposomes-related studies (Figure 1). In addition, there was an encouraging meta-analysis report in which phospholipid-based solid formulations were analyzed as being effective for BA enhancement [10]. Although liposomal delivery does not seem to achieve satisfactory improvement of oral BA for peptides and protein drugs yet, it looks more promising for oral delivery of hydrophobic drugs because liposomes can solubilize poorly water-soluble drugs, protect the drug from degradation in the GI tract and enhance permeability through the epithelial cell membrane, consequently increasing oral BA. However, most published papers performed in vitro studies only, thus lacking in vivo pharmacokinetic results. The present review focuses on the in vivo evidence for the improved BA of water-insoluble drugs and highlights the approaches used for in vivo achievements.

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QbD based development of proliposome of lopinavir for improved oral bioavailability

Cited by 61 publications

References 37 publications

Pharmaceutical Development of Liposomes Using the QbD Approach

Pharmaceutical Development of Liposomes Using the QbD Approach

A dynamic in vitro permeation study on solid mono- and diacyl-phospholipid dispersions of celecoxib

Liposomes for Enhanced Bioavailability of Water-Insoluble Drugs: In Vivo Evidence and Recent Approaches

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