Sodium Fusidate Cream

Sodium Fusidate Cream

Patented Sodium Fusidate Cream with Chitosan Biopolymer.

Proprietary, Patent Protected Product.

The present invention is a cream formulation of an Active Pharmaceutical Ingredient Sodium Fusidate containing Chitosan as Biopolymer for treating primary, secondary & resistant MRSA skin infections, surgical wounds, bedsores, foot ulcers, first degree & second degree burn wounds.

Sodium Fusidate Cream with Chitosan Biopolymer has been granted patent in US (US 8,895,542 B2).

Sodium Fusidate Cream

Sodium Fusidate is a bacteriostatic antibiotic that is often used topically in creams, ointments and eye drops, but may also be given orally as tablets or systemically as injections. Sodium Fusidate is a true antibiotic, derived from the fungus Fusidium coccineum.

Sodium Fusidate acts as a bacterial protein synthesis inhibitor by preventing the turnover of elongation factor G (EF-G) from the ribosome. Sodium Fusidate is effective primarily on gram-positive bacteria such as Staphylococcus species, Streptococcus species, and Corynebacterium species.

Sodium Fusidate Cream with Chitosan Biopolymer penetrates both intact and damaged skin, crust and cellular debris at a rate similar to glucocorticoids because of it steroidal structure and exerts synergistic antibacterial therapy.

Chitosan Biopolymer

Chitosan is a linear polysaccharide composed of randomly distributed β-(1-4)-linked D-glucosamine (deacetylated unit) and N-acetyl-D-glucosamine (acetylated unit). In medicine, it is useful in bandages to reduce bleeding, hastens healing and as an antibacterial agent and it can also be used to help deliver drugs through the skin.

Chitosan’s properties allow it to rapidly clot blood and have recently gained approval in the United States and Europe for use in bandages and other hemostatic agents. Chitosan hemostatic products have been shown in testing by the U.S. Marine Corps to quickly stop bleeding and to reduce blood loss.

Globally Patented Product achieved through unique Process (patented for both product & process)

Sodium Fusidate Cream with Chitosan Biopolymer has been granted patent in countries including US, Europe, Japan, South Africa, Mexico, China, Israel, New Zealand, Philippines, Russia, Canada, Korea and India. The patented Sodium Fusidate Cream with Chitosan Biopolymer formulation redefines the antibacterial therapy and skin healing in the treatment of primary, secondary infections including MRSA infections, Wounds and Burns.

The patent has been Granted:

  • For an in-situ process of converting Sodium Fusidate into Ultrafine Fusidic Acid Cream with average particle size of 3 micron.
  • For the formulation of Sodium Fusidate cream with Chitosan Biopolymer that offers bactericidal action, faster and superior skin healing compared to Fusidic Acid, Mupirocin Calcium and Framycetin Creams.
  • Ultrafine Sodium Fusidate diffuses freely and rapidly through dermal tissues unlike other Fusidic acid which are found to be above 20 microns. Thereby Sodium Fusidate Cream with Chitosan Biopolymer ensures high penetration and release rate.

Benefits of Chitosan Biopolymer

Chitosan’s known properties include acceleration of blood clotting. It is known to have film forming, mucoadhesive and viscosity-increasing properties. It is biocompatible with both healthy and infected skin and biodegradable.

  • Chitosan Biopolymer acts as a vehicle in the localized delivery of Active Pharmaceutical Ingredients thereby increasing the permeability and availability of the active ingredient in the skin.
  • As a micro-film forming biomaterial, Chitosan Biopolymer found to help in reducing the width of the wound, controls the oxygen permeability at the site, absorbs wound discharge and gets degraded by tissue enzymes which are very much required for healing at a faster rate. It also reduces the skin irritation and reported to be preventing secondary infection.
  • Chitosan Biopolymer with its natural cationic charge acts as a broad spectrum bactericidal agent which immobilizes, arrests and kills the bacteria at the site of application by penetrating intact, damaged skin, crust and cellular debris and forms biodegradable mesh.
  • Chitosan reported to act as a bactericidal by a three way mechanism, hence found to be effective even against resistant pathogens.
  • Chitosan Biopolymer has been studied and published widely in reputed medical journals as a wound healing accelerator in all phases of wound healing and beneficial in reducing scar tissue formation by biphasic regulation of TGF-Beta  which helps to rejuvenate and restore the native skin in wounds.
  • Chitosan Biopolymer films are permeable for oxygen and water, protecting irritated and affected skin. Chitosan forms a clear, elastic film on the skin and hair, thereby increasing its softness, smoothness, and mechanical strength.

Synergistic Advantage of Sodium Fusidate with Chitosan Biopolymer Cream

Sodium Fusidate Cream with Chitosan Biopolymer acts synergistically at the site of application and forms a micro bio-film and protects from secondary skin infection which helps skin healing at a faster rate.

Sodium Fusidate Cream with Chitosan Biopolymer ensures better diffusivity and higher release rate compared to Fusidic Acid alone.

In burn wound healing, Sodium Fusidate Cream with Chitosan Biopolymer ensures quick onset of healing, faster re-epithelialization and accelerated wound contraction compared with Fusidic Acid, Mupirocin Calcium and Framycetin cream. This was substantiated by an increase in amount of collagen in Sodium Fusidate Cream with Chitosan Biopolymer treated group by histopathology studies.

In primary skin infections Sodium Fusidate Cream with Chitosan Biopolymer accelerates wound contraction and wound re-epithelialization and scored higher on Visual Analogue Score and Physician’s Global Evaluation score compared to Mupirocin Calcium and Fusidic Acid creams.

Sodium Fusidate Cream with Chitosan Biopolymer forms a micro bio-film at the site of wound which helps in reducing the width of the wound, absorbs wound discharge and gets degraded by tissue enzymes which are very much required for healing at a faster rate.

The burn wound healing action of Sodium Fusidate Cream with Chitosan Biopolymer when compared to Fusidic Acid, Mupirocin Calcium and Framycetin cream could be due to certain positive factors such as;

  • Effective control of bacterial contamination at wound site
  • Faster wound contraction
  • Faster re-epithelialization
  • Revascularization
  • Faster acceleration of hydroxyproline that lead to formation of Collagen

Proof of Concepts

The proof of concept for the uniqueness of patented formulation was provided through a series of trials conducted at USFDA approved and internationally accredited Clinical Research Organizations and Academic Institutions. The details of clinical trials are furnished below;

Study on Stability – apex R&D, Insights from IIT (Indian Institute of Technology-Madras), India

The stability evaluation confirms that, Sodium Fusidate cream with Chitosan Biopolymer is found to be highly stable for 53 months as per ICH guidelines. The molecular modeling studies conducted at Indian Institute of Technology, Madras revealed that the salt Sodium Fusidate is much stable than the parent Fusidic acid.

Diffusion Study – Dr. Bhanuben Nanavati College of Pharmacy, Mumbai, India

The study reveals that the rate of diffusion and release rate/flux rate of Sodium Fusidate Cream with Chitosan Biopolymer was 74.20% to a flux rate of 20.43% of market lead. This study confirms that, the average particle size of Sodium Fusidate Cream with Chitosan Biopolymer of much lower size than the API particle size in the market lead product.

Blood clotting study – Micro Therapeutic Research Laboratories (USFDA Approved), Chennai, India

Sodium Fusidate Cream with Chitosan Biopolymer showed about 58.62% reduction in blood clotting time against the control.

Clinical study on efficacy in primary skin infections – Quest Life Sciences (USFDA Approved), Chennai, India

In impetigo and pyoderma, Sodium Fusidate Cream with Chitosan Biopolymer accelerated wound contraction and wound re-epithelialization and scored higher on the following parameters as compared to the Fusidic Acid cream.

  • VAS Score (Visual Analogue Score)
  • Wound Contraction
  • Wound Re-epithelialization
  • Physician’s Global Evaluation Score

Clinical study on burn wound healing – Manipal Acunova Clinical Research Centre (USFDA Approved), Manipal, India

In burn wound healing Sodium Fusidate Cream with Chitosan Biopolymer reduced the epithelialization period (17.2 days) significantly (p<0.042) compared to Fusidic Acid, Mupirocin Calcium and Framycetin Cream.

Sodium Fusidate Cream with Chitosan Biopolymer has significantly favoured wound contraction (92.4%) when compared to Fusidic Acid (57.1%), Mupirocin Calcium (75.1%) and Framycetin creams (63.3%) and heals at a faster rate than the comparable marketed products.

Effect of Formulation on burn wound Healing – Center for Advanced Drug Research and Testing, J.S.S. College of Pharmacy, Ooty, India

The results of wound contraction revealed that Sodium Fusidate Cream with Chitosan Biopolymer treated group demonstrated 70.53% wound contraction on day 8. Similar findings are recorded in these groups throughout the experimental period and on day 21, almost 100% wound contraction with scar formation was observed in treated group when compared to control and other treated groups.

Hydroxyproline was estimated on day 21 in regenerated skin, and the results revealed decreased levels of hydroxyproline in Sodium Fusidate Cream with Chitosan Biopolymer treated rats when compared to Fusidic Acid, Mupirocin Calcium and Framycetin Creams. The levels of hydroxyproline are significantly higher in Fusidic Acid, Mupirocin Calcium and Framycetin Creams groups when compared to Sodium Fusidate Cream with Chitosan Biopolymer.

BIOCHITODERM™ is the registered trademark of apex in India representing the Biopolymer Chitosan used in different products by apex as a functional excipient along with various Active Pharmaceutical Ingredients (API).