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Current Pharmaceutical Biotechnology , Vol. 3, No. 3, 2002

 

Contents

 

Management of Acute and Chronic Open Wounds: The Importance of Moist Environment in Optimal Wound Healing Pp-179-195

Bishara S. Atiyeh, John Ioannovich, Christian A. Al-Amm and Kusai A. El-Musa

[Abstract]

 

Drugs that Inhibit Mycolic Acid Biosynthesis in Mycobacterium tuberculosis Pp-197-225

E.K. Schroeder, O.N. de Souza, D.S. Santos, J.S. Blanchard, and L.A. Basso

[Abstract]      

 

Encapsulating DNA within Biodegradable Polymeric Microparticles Pp-227-235

Corinne S. Lengsfeld, Mark C. Manning, and Theodore W. Randolph

[Abstract]

 

Engineering Antibodies for Therapy Pp-237-256

Leonard G. Presta

[Abstract]

 

Localised Delivery of Therapeutic Agents to CNS Malignancies: Old and New Approaches Pp-257-273

Tracy-Ann Read, Frits Thorsen and Rolf Bjerkvig

[Abstract]

 

Modulating Poly (ADP-Ribose) Polymerase Activity: Potential for the Prevention and Therapy of Pathogenic Situations Involving DNA Damage and Oxidative Stress Pp-275-283

Patrice Decker and Sylviane Muller

[Abstract]

                                                                                                                                                            


Abstracts

 

[Back to top] Management of Acute and Chronic Open Wounds: The Importance of Moist Environment in Optimal Wound Healing

Bishara S. Atiyeh, John Ioannovich, Christian A. Al-Amm and Kusai A. El-Musa

 

The history of wound care and management closely parallels that of military surgery which has laid down the principles and dictated the practices of wound cleansing, debridement and coverage. From a treatment standpoint, there are essentially two types of wounds: those characterized by loss of tissue and those in which no tissue has been lost. In the event of tissue loss it is critical to determine whether vital structures such as bone, tendons, nerves and vessels have been exposed. It is also important to determine the amount of soft tissue contusion and contamination. In any case primary wound healing by early closure either primarily or with the help of grafts or flaps is preferred to secondary healing and wound contraction with subsequent contractures which interfere with range of motion and function.

 

Whether the wound is acute or chronic, essential principles of wound care must be observed in order to avoid wound sepsis and achieve rapid and optimal wound healing.

 

- Tissues must be handled gently.

 

- Caustic solutions capable of sterilizing the skin should never be applied to the wound. It is desirable never to put  anything in the wound that cannot be tolerated comfortably in the conjunctival sac.

 

- All devitalized tissues must be debrided either hydrodynamically, chemically, mechanically or surgically.

 

- All dead space must be obliterated

 

- Exposed vital structures must be covered by well vascularized tissues.

 

An essential part of any wound management protocol is wound dressing. It cannot be too strongly emphasized that a wound dressing may have a profound influence on healing particularly of secondary type healing, a critical feature being the extent to which such dressing restricts the evaporation of water from the wound surface. A review of available dressing materials is reported with emphasis on the newly developed concept of moist environment for optimal healing. A practical guide for dressing selection is also proposed.

 

[Back to top] Drugs that Inhibit Mycolic Acid Biosynthesis in Mycobacterium tuberculosis

E.K. Schroeder, O.N. de Souza, D.S. Santos, J.S. Blanchard, and L.A. Basso

 

Tuberculosis resurged in the late 1980s and now kills more than 2 million people a year. The reemergence of tuberculosis as a potential public health threat, the high susceptibility of human immunodeficiency virus-infected persons to the disease, and the proliferation of multidrug- resistant (MDR) strains have created much scientific interest in developing new antimycobacterial agents to both treat Mycobacterium tuberculosis strains resistant to existing drugs, and shorten the duration of short-course treatment to improve patient compliance. Bacterial cell-wall biosynthesis is a proven target for new antibacterial drugs. Mycolic acids, which are key components of the mycobacterial cell wall, are a-alkyl, b-hydroxy fatty acids, with a species-dependent saturated "short" arm of 20-26 carbon atoms and a "long" meromycolic acid arm of 50-60 carbon atoms. The latter arm is functionalized at regular intervals by cyclopropyl, a-methyl ketone, or a-methyl methylethers groups. The mycolic acid biosynthetic pathway has been proposed to involve five distinct stages: (i) synthesis of C20 to C26 straight-chain saturated fatty acids to provide the a-alkyl branch; (ii) synthesis of the meromycolic acid chain to provide the main carbon backbone, (iii) modification of this backbone to introduce other functional groups; (iv) the final Claisen-type condensation step followed by reduction; and (v) various mycolyltransferase processes to cellular lipids. The drugs shown to inhibit mycolic acid biosynthesis are isoniazid, ethionamide, isoxyl, thiolactomycin, and triclosan. In addition, pyrazinamide was shown to inhibit fatty acid synthase type I which, in turn, provides precursors for fatty acid elongation to long-chain mycolic acids by fatty acid synthase II. Here we review the biosynthesis of mycolic acids and the mechanism of action of antimicrobial agents that act upon this pathway. In addition, we describe molecular modeling studies on InhA, the bona-fide target for isoniazid, which should improve our understanding of the amino acid residues involved in the enzyme’s mechanism of action and, accordingly, provide a rational approach to the design of new drugs.

 

[Back to top] Encapsulating DNA within Biodegradable Polymeric Microparticles

Corinne S. Lengsfeld, Mark C. Manning, and Theodore W. Randolph

 

In order for genetic medicines to become viable commercial products, the active form of the drug (e.g., DNA) must be able to reach the site of action and remain there long enough to accomplish its intended function. Encapsulation of plasmid DNA into biodegradable microspheres is one approach towards solving this challenge. This review describes the primary methods for satisfactorily entrapping intact DNA into biodegradable polymeric matrices. In particular, the materials, processes, and equipment required for each encapsulation method are described in detail. The resulting microspheres could be used for parenteral, oral, and inhalation therapy.

 

[Back to top]  Engineering Antibodies for Therapy

Leonard G. Presta

 

With eleven therapeutic antibodies approved worldwide and many more in clinical trials, research on antibody engineering has continued to escalate and expand. This review covers recent progress in generation of antibodies by ex vivo methods, systems for screening these, and the quest for higher affinity, more stable, optimally biodistributed antibody fragments, especially for solid tumors. The latest developments in engineering antibodies for removal or enhancement of effector functions (antibody-dependent cellular cytotoxicity (ADCC), phagosytosis, complement fixation (CDC) and halflife) through protein alteration or carbohydrate optimization may now enable generation of superior antibody therapeutics. Antibody conjugates, including immunotoxins and immunocytokines, as well as multivalent and multispecific antibodies confer expanded utility of therapeutic antibodies. Finally, research into the IgA/FcaRI system has now provided an additional route to therapeutic antibodies.

 

[Back to top] Localised Delivery of Therapeutic Agents to CNS Malignancies: Old and New Approaches

Tracy-Ann Read, Frits Thorsen and Rolf Bjerkvig

 

Despite advances in neuro-imaging, neurosurgery, radiation therapy, and chemotherapy, limited progress has been made in the treatment of patients with high-grade astrocytomas. Primary brain tumours are considered to be among the most difficult neoplasms to treat which is largely due to the invasive nature of these tumours and the complexity of the organ in which they arise. In an attempt to overcome some of the limitations of systemic delivery of anticancer drugs, several methods of localised delivery have been developed. In this article we briefly review some of the current literature on systems for localised delivery of therapeutic agents to brain tumors, which consists of osmotic mini-pumps, infusion pumps (convectionenhanced delivery), and cell grafting. Furthermore, special emphasis is made on bio-degradable polymers, which is at present the best characterised system of local delivery to brain tumors, along with a promising novel delivery system, based on non-degradable polymer encapsulated cell therapy.

 

[Back to top] Modulating Poly (ADP-Ribose) Polymerase Activity: Potential for the Prevention and Therapy of Pathogenic Situations Involving DNA Damage and Oxidative Stress

Patrice Decker and Sylviane Muller

 

Poly (ADP-ribose) polymerase is a zinc-finger DNA-binding enzyme which detects and signals DNA strand breaks generated either directly during base excision repair, or indirectly by genotoxic agents such as oxygen radicals. In response to genotoxic injury, PARP catalyses the synthesis of poly (ADP-ribose), from its substrate b-NAD+ and this polymer is covalently attached to several nuclear proteins and PARP itself. As a result, PARP converts DNA breaks into intracellular signals which activate DNA repair programs or cell death options. Several studies have also shown that PARP is involved in either necrosis and subsequent inflammation or apoptosis. Although this enzyme is not indispensable during the latter cell death program, it has been demonstrated that PARP plays a facilitating role in this process. PARP is activated at an intermediate stage of apoptosis and is then cleaved and inactivated at a late stage by apoptotic proteases, namely caspase-3/CPP-32/Yama/apopain and caspase-7. This cleavage prevents necrosis during apoptosis, avoiding inflammation. All these functions, and the observation that PARP is an abundant and highly conserved enzyme, suggest that this enzyme plays a pivotal role, particularly in the maintenance of genomic DNA stability, apoptosis and in the response to oxidative stress. Since these situations are found in cancer, inflammation, autoimmunity (such as diabetes), myocardial dysfunction, certain infections, ageing and radiation/chemical exposure, attempts have been made to modulate PARP activity. With regard to the increasing interest towards PARP, the aim of this review is to explain the cellular role of PARP and the advantages of modulating its activity in diverse preventive or therapeutic strategies.