Biosurfactants as Multifunctional Ingredients for Emerging Pharmaceutical Formulations

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Physical Pharmacy and Formulation".

Deadline for manuscript submissions: closed (31 October 2021) | Viewed by 38533

Special Issue Editors


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Guest Editor
Department of Pharmacy and Biotechnology, University of Bologna, Via San Donato 19/2, 40127 Bologna, Italy
Interests: drug delivery; formulation of "health promoting" bacteria; hydrogels; liposomes; transmucosal and transcutaneous permeation

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Guest Editor
Department of Pharmacy and Biotechnology, University of Bologna, Via San Donato 19/2, 40127 Bologna, Italy
Interests: drug delivery; nanoparticles; microparticles; films; hydrogels; liposomes; transmucosal and transcutaneous permeation

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Guest Editor
Department of Pharmacy and Biotechnology Alma Mater Studiorum, University of Bologna, 40126 Bologna (BO), Italy
Interests: microbial ecology; human health microbiology; cellular biochemistry; cancer; human microbial ecosystems; molecular microbiology; applied microbiology; lactobacillus bacteria; probiotics
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Special Issue Information

Dear Colleagues,

Biosurfactants (BS) are surface-active compounds produced by microbial metabolism. They are safe, biodegradable and environment friendly and they have versatile applications as ingredients in pharmaceutical products. Due to their amphiphilic nature, they can be exploited as pharmaceutical excipients to enhance aqueous solubility of lipophilic molecules, to optimize release and permeation profiles of active substances, and to stabilize disperse systems. Due to intrinsic antimicrobial and antiadhesive properties, they can be also proposed as active ingredients or as adjuvants to counteract microbial or viral infections. In addition, recent findings suggest their capacity to act as anticancer, immunomodulating, and wound healing agents.

This Special Issue aims to cover different applications of BS as pharmaceutical excipients and/or active molecules and will include papers describing the preparation and characterization of innovative pharmaceutical formulations containing BS.

Prof. Barbara Luppi
Dr. Angela Abruzzo
Dr. Carola Parolin
Guest Editors

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Keywords

  • biosurfactants
  • pharmaceutical formulations
  • modified release
  • solubility and permeation enhancers
  • emulsifying and dispersing agents
  • antimicrobials
  • anticancer agents
  • immunomodulators
  • wound healing agents

Published Papers (8 papers)

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Research

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17 pages, 2073 KiB  
Article
Antiviral Activity of the Rhamnolipids Mixture from the Antarctic Bacterium Pseudomonas gessardii M15 against Herpes Simplex Viruses and Coronaviruses
by Rosa Giugliano, Carmine Buonocore, Carla Zannella, Annalisa Chianese, Fortunato Palma Esposito, Pietro Tedesco, Anna De Filippis, Massimiliano Galdiero, Gianluigi Franci and Donatella de Pascale
Pharmaceutics 2021, 13(12), 2121; https://doi.org/10.3390/pharmaceutics13122121 - 08 Dec 2021
Cited by 16 | Viewed by 2985
Abstract
Emerging and re-emerging viruses represent a serious threat to human health at a global level. In particular, enveloped viruses are one of the main causes of viral outbreaks, as recently demonstrated by SARS-CoV-2. An effective strategy to counteract these viruses could be to [...] Read more.
Emerging and re-emerging viruses represent a serious threat to human health at a global level. In particular, enveloped viruses are one of the main causes of viral outbreaks, as recently demonstrated by SARS-CoV-2. An effective strategy to counteract these viruses could be to target the envelope by using surface-active compounds. Rhamnolipids (RLs) are microbial biosurfactants displaying a wide range of bioactivities, such as antibacterial, antifungal and antibiofilm, among others. Being of microbial origin, they are environmentally-friendly, biodegradable, and less toxic than synthetic surfactants. In this work, we explored the antiviral activity of the rhamnolipids mixture (M15RL) produced by the Antarctic bacteria Pseudomonas gessardii M15 against viruses belonging to Coronaviridae and Herpesviridae families. In addition, we investigated the rhamnolipids’ mode of action and the possibility of inactivating viruses on treated surfaces. Our results show complete inactivation of HSV-1 and HSV-2 by M15RLs at 6 µg/mL, and of HCoV-229E and SARS-CoV-2 at 25 and 50 µg/mL, respectively. Concerning activity against HCoV-OC43, 80% inhibition of cytopathic effect was recorded, while no activity against naked Poliovirus Type 1 (PV-1) was detectable, suggesting that the antiviral action is mainly directed towards the envelope. In conclusion, we report a significant activity of M15RL against enveloped viruses and demonstrated for the first time the antiviral effect of rhamnolipids against SARS-CoV-2. Full article
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20 pages, 2160 KiB  
Article
Diverse Effects of Natural and Synthetic Surfactants on the Inhibition of Staphylococcus aureus Biofilm
by Gianna Allegrone, Chiara Ceresa, Maurizio Rinaldi and Letizia Fracchia
Pharmaceutics 2021, 13(8), 1172; https://doi.org/10.3390/pharmaceutics13081172 - 29 Jul 2021
Cited by 13 | Viewed by 2370
Abstract
A major challenge in the biomedical field is the creation of materials and coating strategies that effectively limit the onset of biofilm-associated infections on medical devices. Biosurfactants are well known and appreciated for their antimicrobial/anti-adhesive/anti-biofilm properties, low toxicity, and biocompatibility. In this study, [...] Read more.
A major challenge in the biomedical field is the creation of materials and coating strategies that effectively limit the onset of biofilm-associated infections on medical devices. Biosurfactants are well known and appreciated for their antimicrobial/anti-adhesive/anti-biofilm properties, low toxicity, and biocompatibility. In this study, the rhamnolipid produced by Pseudomonas aeruginosa 89 (R89BS) was characterized by HPLC-MS/MS and its ability to modify cell surface hydrophobicity and membrane permeability as well as its antimicrobial, anti-adhesive, and anti-biofilm activity against Staphylococcus aureus were compared to two commonly used surfactants of synthetic origin: Tween® 80 and TritonTM X-100. The R89BS crude extract showed a grade of purity of 91.4% and was composed by 70.6% of mono-rhamnolipids and 20.8% of di-rhamnolipids. The biological activities of R89BS towards S. aureus were higher than those of the two synthetic surfactants. In particular, the anti-adhesive and anti-biofilm properties of R89BS and of its purified mono- and di-congeners were similar. R89BS inhibition of S. aureus adhesion and biofilm formation was ~97% and 85%, respectively, and resulted in an increased inhibition of about 33% after 6 h and of about 39% after 72 h when compared to their chemical counterparts. These results suggest a possible applicability of R89BS as a protective coating agent to limit implant colonization. Full article
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14 pages, 1652 KiB  
Article
Influence of Lactobacillus Biosurfactants on Skin Permeation of Hydrocortisone
by Angela Abruzzo, Carola Parolin, Elisa Corazza, Barbara Giordani, Massimiliano Pio di Cagno, Teresa Cerchiara, Federica Bigucci, Beatrice Vitali and Barbara Luppi
Pharmaceutics 2021, 13(6), 820; https://doi.org/10.3390/pharmaceutics13060820 - 31 May 2021
Cited by 5 | Viewed by 2687
Abstract
One of the most widely used strategies to improve drug diffusion through the skin is the use of permeation enhancers. The aim of this work was to investigate the effect of two biosurfactants (BS), produced by Lactobacillus crispatus BC1 and Lactobacillus gasseri BC9, [...] Read more.
One of the most widely used strategies to improve drug diffusion through the skin is the use of permeation enhancers. The aim of this work was to investigate the effect of two biosurfactants (BS), produced by Lactobacillus crispatus BC1 and Lactobacillus gasseri BC9, on the skin permeation profile of hydrocortisone (HC, model drug). HC aqueous solubility and in vitro diffusion studies through porcine skin were performed in the presence of BC1-BS and BC9-BS at concentrations below and above critical micellar concentrations (CMC). Moreover, skin hydration tests and differential scanning calorimetry (DSC) analysis were performed to further investigate BS interaction with the outermost layer of the skin. Both BS increased HC solubility, especially at concentrations above their CMC. At concentrations below the CMC, drug permeation through the skin was improved, as the result of a dual effect: a) the formation of a superficial lipophilic environment, as confirmed by the reduction in skin hydration and b) the interaction between BS and the stratum corneum (SC), as demonstrated by the DSC curves. From the obtained data, it appears that BC1-BS and BC9-BS could represent new promising green excipients for drug permeation enhancement through the skin. Full article
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Review

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34 pages, 17326 KiB  
Review
Nanoemulsions: A Review on the Conceptualization of Treatment for Psoriasis Using a ‘Green’ Surfactant with Low-Energy Emulsification Method
by Ignatius Julian Dinshaw, Noraini Ahmad, Norazlinaliza Salim and Bey Fen Leo
Pharmaceutics 2021, 13(7), 1024; https://doi.org/10.3390/pharmaceutics13071024 - 06 Jul 2021
Cited by 14 | Viewed by 4042
Abstract
Psoriasis is a skin disease that is not lethal and does not spread through bodily contact. However, this seemingly harmless condition can lead to a loss of confidence and social stigmatization due to a persons’ flawed appearance. The conventional methods of psoriasis treatment [...] Read more.
Psoriasis is a skin disease that is not lethal and does not spread through bodily contact. However, this seemingly harmless condition can lead to a loss of confidence and social stigmatization due to a persons’ flawed appearance. The conventional methods of psoriasis treatment include taking in systemic drugs to inhibit immunoresponses within the body or applying topical drugs onto the surface of the skin to inhibit cell proliferation. Topical methods are favored as they pose lesser side effects compared to the systemic methods. However, the side effects from systemic drugs and low bioavailability of topical drugs are the limitations to the treatment. The use of nanotechnology in this field has enhanced drug loading capacity and reduced dosage size. In this review, biosurfactants were introduced as a ‘greener’ alternative to their synthetic counterparts. Glycolipid biosurfactants are specifically suited for anti-psoriatic application due to their characteristic skin-enhancing qualities. The selection of a suitable oil phase can also contribute to the anti-psoriatic effect as some oils have skin-healing properties. The review covers the pathogenic pathway of psoriasis, conventional treatments, and prospective ingredients to be used as components in the nanoemulsion formulation. Furthermore, an insight into the state-of-the-art methods used in formulating nanoemulsions and their progression to low-energy methods are also elaborated in detail. Full article
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25 pages, 2114 KiB  
Review
Recent Advances in Biomedical, Therapeutic and Pharmaceutical Applications of Microbial Surfactants
by Chiara Ceresa, Letizia Fracchia, Emanuele Fedeli, Chiara Porta and Ibrahim M. Banat
Pharmaceutics 2021, 13(4), 466; https://doi.org/10.3390/pharmaceutics13040466 - 30 Mar 2021
Cited by 52 | Viewed by 5088
Abstract
The spread of antimicrobial-resistant pathogens typically existing in biofilm formation and the recent COVID-19 pandemic, although unrelated phenomena, have demonstrated the urgent need for methods to combat such increasing threats. New avenues of research for natural molecules with desirable properties to alleviate this [...] Read more.
The spread of antimicrobial-resistant pathogens typically existing in biofilm formation and the recent COVID-19 pandemic, although unrelated phenomena, have demonstrated the urgent need for methods to combat such increasing threats. New avenues of research for natural molecules with desirable properties to alleviate this situation have, therefore, been expanding. Biosurfactants comprise a group of unique and varied amphiphilic molecules of microbial origin capable of interacting with lipidic membranes/components of microorganisms and altering their physicochemical properties. These features have encouraged closer investigations of these microbial metabolites as new pharmaceutics with potential applications in clinical, hygiene and therapeutic fields. Mounting evidence has indicated that biosurfactants have antimicrobial, antibiofilm, antiviral, immunomodulatory and antiproliferative activities that are exploitable in new anticancer treatments and wound healing applications. Some biosurfactants have already been approved for use in clinical, food and environmental fields, while others are currently under investigation and development as antimicrobials or adjuvants to antibiotics for microbial suppression and biofilm eradication strategies. Moreover, due to the COVID-19 pandemic, biosurfactants are now being explored as an alternative to current products or procedures for effective cleaning and handwash formulations, antiviral plastic and fabric surface coating agents for shields and masks. In addition, biosurfactants have shown promise as drug delivery systems and in the medicinal relief of symptoms associated with SARS-CoV-2 acute respiratory distress syndrome. Full article
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22 pages, 1880 KiB  
Review
Contributions of Glycolipid Biosurfactants and Glycolipid-Modified Materials to Antimicrobial Strategy: A Review
by Qin Shu, Hanghang Lou, Tianyu Wei, Xiayu Liu and Qihe Chen
Pharmaceutics 2021, 13(2), 227; https://doi.org/10.3390/pharmaceutics13020227 - 06 Feb 2021
Cited by 52 | Viewed by 4282
Abstract
Glycolipid biosurfactants are natural amphiphiles and have gained particular interest recently in their biodegradability, diversity, and bioactivity. Microbial infection has caused severe morbidity and mortality and threatened public health security worldwide. Glycolipids have played an important role in combating many diseases as therapeutic [...] Read more.
Glycolipid biosurfactants are natural amphiphiles and have gained particular interest recently in their biodegradability, diversity, and bioactivity. Microbial infection has caused severe morbidity and mortality and threatened public health security worldwide. Glycolipids have played an important role in combating many diseases as therapeutic agents depending on the self-assembly property, the anticancer and anti-inflammatory properties, and the antimicrobial properties, including antibacterial, antifungal, and antiviral effects. Besides, their role has been highlighted as scavengers in impeding the biofilm formation and rupturing mature biofilm, indicating their utility as suitable anti-adhesive coating agents for medical insertional materials leading to a reduction in vast hospital infections. Notably, glycolipids have been widely applied to the synthesis of novel antimicrobial materials due to their excellent amphipathicity, such as nanoparticles and liposomes. Accordingly, this review will provide various antimicrobial applications of glycolipids as functional ingredients in medical therapy. Full article
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21 pages, 1566 KiB  
Review
Microbial Biosurfactants in Cosmetic and Personal Skincare Pharmaceutical Formulations
by Simms A. Adu, Patrick J. Naughton, Roger Marchant and Ibrahim M. Banat
Pharmaceutics 2020, 12(11), 1099; https://doi.org/10.3390/pharmaceutics12111099 - 16 Nov 2020
Cited by 92 | Viewed by 10149
Abstract
Cosmetic and personal care products are globally used and often applied directly on the human skin. According to a recent survey in Europe, the market value of cosmetic and personal care products in Western Europe reached about 84 billion euros in 2018 and [...] Read more.
Cosmetic and personal care products are globally used and often applied directly on the human skin. According to a recent survey in Europe, the market value of cosmetic and personal care products in Western Europe reached about 84 billion euros in 2018 and are predicted to increase by approximately 6% by the end of 2020. With these significant sums of money spent annually on cosmetic and personal care products, along with chemical surfactants being the main ingredient in a number of their formulations, of which many have been reported to have the potential to cause detrimental effects such as allergic reactions and skin irritations to the human skin; hence, the need for the replacement of chemical surfactants with other compounds that would have less or no negative effects on skin health. Biosurfactants (surfactants of biological origin) have exhibited great potential such as lower toxicity, skin compatibility, protection and surface moisturizing effects which are key components for an effective skincare routine. This review discusses the antimicrobial, skin surface moisturizing and low toxicity properties of glycolipid and lipopeptide biosurfactants which could make them suitable substitutes for chemical surfactants in current cosmetic and personal skincare pharmaceutical formulations. Finally, we discuss some challenges and possible solutions for biosurfactant applications. Full article
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35 pages, 1903 KiB  
Review
Surface Active Agents and Their Health-Promoting Properties: Molecules of Multifunctional Significance
by Ioannis Anestopoulos, Despoina Eugenia Kiousi, Ariel Klavaris, Alex Galanis, Karina Salek, Stephen R. Euston, Aglaia Pappa and Mihalis I. Panayiotidis
Pharmaceutics 2020, 12(7), 688; https://doi.org/10.3390/pharmaceutics12070688 - 21 Jul 2020
Cited by 42 | Viewed by 5266
Abstract
Surface active agents (SAAs) are molecules with the capacity to adsorb to solid surfaces and/or fluid interfaces, a property that allows them to act as multifunctional ingredients (e.g., wetting and dispersion agents, emulsifiers, foaming and anti-foaming agents, lubricants, etc.) in a widerange of [...] Read more.
Surface active agents (SAAs) are molecules with the capacity to adsorb to solid surfaces and/or fluid interfaces, a property that allows them to act as multifunctional ingredients (e.g., wetting and dispersion agents, emulsifiers, foaming and anti-foaming agents, lubricants, etc.) in a widerange of the consumer products of various industrial sectors (e.g., pharmaceuticals, cosmetics, personal care, detergents, food, etc.). Given their widespread utilization, there is a continuously growing interest to explore their role in consumer products (relevant to promoting human health) and how such information can be utilized in order to synthesize better chemical derivatives. In this review article, weaimed to provide updated information on synthetic and biological (biosurfactants) SAAs and their health-promoting properties (e.g., anti-microbial, anti-oxidant, anti-viral, anti-inflammatory, anti-cancer and anti-aging) in an attempt to better define some of the underlying mechanism(s) by which they exert such properties. Full article
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