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Technical Report: Evaluating the Effects of LoxaSperse™ Using an In Vitro Model of Human Respiratory Tract Tissue

Introduction:

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Abstract:

LoxaSperse™ is an excipient manufactured by PCCA that can be used in compounding as a dispersing or solubilizing agent for active pharmaceutical ingredients (APIs) in nasal nebulizations or irrigations. It can help improve the solubility and therefore potential bioavailability of poorly water soluble drugs or combinations of drugs used in the treatment of respiratory and pulmonary diseases. The in vitro toxicity profile of LoxaSperse was evaluated using normal tracheal/bronchial epithelial cells in an assay which closely resembles the epithelial tissue of the respiratory tract. At concentrations of 0.01 µg/µL, 0.1 µg/µL, and 1 µg/µL, LoxaSperse was shown to be substantially less toxic than the positive control, Polysorbate 20 NF, with mean percent cell viabilities of 96%, 98%, and 69% for LoxaSperse compared to 65%, 28%, and 7% for the toxicant Polysorbate 20 NF, respectively. In addition, LoxaSperse exhibited a low toxicological profile similar to that of a known nontoxic respiratory agent, Monohydrate Lactose inhalation grade (negative control). The results of this study suggest a positive safety profile for the use of LoxaSperse as an excipient for compounding with APIs used in the treatment of respiratory and pulmonary diseases.

Conclusions:

LoxaSperse is an excipient used to enhance the water solubility and dispersibility of APIs, leading to increased bioavailability, which can potentially improve drug efficacy and therapeutic outcome. Using LoxaSperse as an excipient in compounded preparations allows for APIs with low water solubility and combinations of APIs to be delivered locally to the area of treatment. LoxaSperse improves the dissolution of poorly water soluble drugs into hydrophilic and permeable tissue compartments such as the oral and nasal cavities. This study showed that LoxaSperse as an excipient produced very minimal toxicity in the human respiratory tract tissue. The results of this study suggest a positive safety profile for the use of LoxaSperse as an excipient for compounding with APIs used in the treatment of respiratory and pulmonary diseases.

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