Dual targeting lipid-based formulation for enhanced thyroid targeting drug delivery

Abstract

This patent discloses a dual targeting lipid-based formulation designed for precise drug delivery to the thyroid gland, addressing the complexities of thyroid disorders. The formulation integrates two key technologies: the RGDFK Targeting Motif and Iodine Coupling. The RGDFK motif enhances specific binding to αvβ3 integrin receptors, facilitating internalization of therapeutic agents. Simultaneously, the Iodine Coupling technology leverages the thyroid gland's natural affinity for iodine, ensuring increased accumulation of lipid-based vesicles in thyroid tissue. Applications of this formulation extend to targeted treatment of diverse thyroid disorders, symptom-specific relief, and nutritional supplementation. The formulation serves as a fundamental component in pharmaceutical compositions, adaptable for various administration routes. The manufacturing process emphasizes scalability, reproducibility, and standardized quality. A comprehensive treatment kit has been devised, offering a convenient and tailored approach to thyroid drug delivery. In conclusion, this dual targeting lipid-based formulation signifies a paradigm shift in thyroid disorder therapeutics, promising precision, efficacy, and patient-centric care. As it advances towards clinical applications, it holds the potential to redefine the landscape of thyroid health management for enhanced patient outcomes.

Description

[0001] Dual Targeting Lipid-Based Formulation for Enhanced Thyroid Targeting Drug Delivery

[0002] Technical Field:

[0003] The present invention resides in the domain of pharmaceutical formulations and targeted drug delivery systems. Specifically, it addresses challenges in thyroid drug delivery by introducing a novel dual targeting lipid-based formulation. Positioned at the intersection of pharmacology, the formulation employs motifs and coupling agents for enhanced drug specificity, increased absorption, and improved bioavailability to the thyroid gland. Focused on advancing beyond conventional methods, the invention holds promise for more effective thyroid disorder treatments with reduced side effects. Additionally, it aligns with recent developments in lipid- based formulations, capitalizing on their efficacy while addressing challenges associated with precise targeting. This field of invention acknowledges the pivotal role of iodine in thyroid physiology and leverages the thyroid's natural affinity for this element.

[0004] Keywords:

[0005] Dual Targeting, Lipid-Based Formulation, Thyroid Drug Delivery, CYCLO RGDFK, Iodine Coupling, Pharmaceutical Formulations, Thyroid Disorders, Thyroid General Health, Thyroid Supplements, Drug Specificity.

[0006] Background Art :

[0007] The thyroid gland assumes a pivotal role in regulating various physiological processes within the body as an integral component of the endocrine system. Orchestrating metabolic homeostasis, it synthesizes and secretes vital hormones, notably thyroxine (T4) and triiodothyronine (T3).

[0008] The synthesis of T3 and T4 is intricately regulated by the hypothalamus-pituitary- thyroid axis. Iodine, a crucial element, plays a pivotal role in the synthesis of thyroid hormones. The thyroid gland actively takes up iodine from the bloodstream, incorporating it into the structure of T3 and T4. Iodide uptake by the thyroid gland from the bloodstream undergoes conversion into iodine. This iodine is subsequently added to a protein called thyroglobulin, resulting in the production of two forms: MIT and DIT. The combination of MIT and DIT forms the thyroid hormones T3 and T4.

[0009] Overall, iodine is an essential component for the synthesis of T3 and T4 in the thyroid gland. Without adequate iodine, the production of these hormones would be impaired, leading to thyroid disorders such as hypothyroidism or goiter.

[0010] The thyroid gland is susceptible to various physiological and pathological conditions, manifesting as hypothyroidism (underactive thyroid), hyperthyroidism (overactive thyroid), goiter (enlarged thyroid gland), or thyroid nodules and cancer.

[0011] Hypothyroidism arises when the thyroid gland fails to produce sufficient thyroid hormones, resulting in symptoms such as fatigue, weight gain, and cold intolerance. Conversely, hyperthyroidism involves an excessive production of thyroid hormones, leading to symptoms like weight loss and rapid heartbeat. Thyroid nodules, although mostly benign, can pose concerns of malignancy. Goiter, an enlargement of the thyroid gland, is often linked to iodine deficiency or underlying thyroid disorders.

[0012] In the context of targeted drug delivery to the thyroid gland, the present invention introduces a revolutionary lipid-based formulation. Employing dual targeting agents, a motif, and a coupling nutrient, this formulation aims to achieve precise thyroid delivery and specific cell uptake.

[0013] This lipid-based vesicle formulation has the capacity to encapsulate therapeutic agents. By coupling iodine (I-) onto the lipid-based vesicle's surface, it leverages the thyroid glands affinity for iodine, enhancing drug delivery. Additionally, the incorporation of a cyclic peptide motif, CYCLO RGDFK, provides further enhances targeting. The CYCLO RGDFK motif exhibits binding capabilities to cell surface receptors (av03, av05, and a501), which are overexpressed in thyroid cells. This facilitates specific binding and uptake of the lipid-based vesicles by the thyroid gland.

[0014] The versatility of this formulation extends to encapsulating multivitamins and minerals, enabling targeted delivery to the thyroid gland. This approach holds the potential to enhance the uptake and utilization of essential nutrients, addressing specific nutritional deficiencies and supporting overall thyroid health.

[0015] Disclosure Of The invention :

[0016] Summary of the Invention:

[0017] The innovation at the core of this invention lies in a meticulous dual targeting formulation designed to revolutionize drug delivery to the thyroid gland. Employing a synergistic mechanism of action, the formulation harnesses two key technologies: the RGDFK Targeting Motif and Iodine Coupling.

[0018] Detailed Description :

[0019] The dual targeting formulation outlined in this invention is founded on a comprehensive understanding of thyroid physiology and the complex mechanisms underlying thyroid hormone synthesis. The formulation intricately integrates dual targeting strategies, encompassing both active and passive drug targeting approaches. This is accomplished by combining the (RGDFK Targeting Motif) as an active targeting component and (Iodine Coupling) as a passive targeting component, thereby achieving precise and effective drug delivery to the thyroid gland. RGDFK Targeting Motif Mechanism of Action in Detail: The integration of the RGDFK targeting motif involves coupling this cyclic peptide to lipid- based vesicles. This coupling imparts a targeted characteristic to the formulation, allowing for the selective binding of the lipid-based vesicles to the overexpressed av03 integrin receptors in thyroid cells. The subsequent internalization of the encapsulated therapeutic agents, such as multivitamins, is utilized through this receptor-mediated pathway. This targeted strategy not only enhances treatment efficacy but also minimizes systemic side effects, presenting a breakthrough in addressing nutritional deficiencies and supporting thyroid health. Iodine Coupling Mechanism of Action in Detail: The Iodine Coupling focuses on exploiting the thyroid gland's natural affinity for iodine. Through the incorporation of iodine into the lipid-based structure, this will leverage into the sodium-iodide symporter (NIS) mechanism on the surface of thyroid follicular cells. This strategic coupling enhances the specificity of the drug delivery system to the thyroid gland, ensuring optimal accumulation of the lipid-based vesicles within thyroid tissue. The result is an innovative approach that capitalizes on the physiological processes of iodine uptake, presenting a significant advancement in thyroid-targeted drug delivery.

[0020] Applications:

[0021] The dual targeting lipid-based formulation outlined in this invention holds diverse applications in the field of thyroid health and drug delivery. These applications extend across various facets of thyroid disorders, nutritional supplementation, and pharmaceutical compositions.

[0022] 1. Targeted Treatment of Thyroid Disorders: The formulation offers a precise therapeutic approach for a spectrum of thyroid disorders, including hypothyroidism, hyperthyroidism, goiter, thyroid nodules, and thyroid cancer.

[0023] 2. Symptom-Specific Relief: By targeting av03 integrin receptors and optimizing iodine uptake, the formulation aims to alleviate specific symptoms associated with thyroid dysfunction, such as fatigue, weight changes, rapid heartbeat, and mood disturbances.

[0024] 3. Nutritional Supplementation: The formulation's targeted delivery of multivitamins and minerals addresses specific deficiencies, promoting overall thyroid health and well-being.

[0025] 4. Pharmaceutical Composition: This formulation serves as a pivotal component in creating pharmaceutical compositions, providing a safe and effective vehicle for thyroid drug delivery through various administration routes.

[0026] 5. Manufacturing Scalability: The manufacturing process ensures scalability and reproducibility, vital for widespread therapeutic applications, maintaining consistent quality and dosage precision. 6. Comprehensive Treatment Kit: A comprehensive kit has been designed, incorporating the dual targeting lipid-based formulation, instructional materials, and accessories, offering a convenient and tailored approach to thyroid drug delivery.

[0027] Conclusion:

[0028] In conclusion, the dual targeting lipid-based formulation presented in this patent represents a pioneering advancement in the realm of thyroid drug delivery. By integrating the RGDFK Targeting Motif and Iodine Coupling components, the formulation offers a precise and effective approach to address the complexities of thyroid disorders. The diverse applications, ranging from targeted treatment to nutritional supplementation, underscore the versatility and potential impact of this innovative formulation.

[0029] This invention not only addresses the challenges posed by conventional methods but also opens new avenues for customized and effective thyroid health interventions. The applications outlined a new era in thyroid disorder therapeutics, emphasizing precision, efficacy, and patient-centric care. As the formulation progresses towards clinical applications, it holds promise in reshaping the landscape of thyroid health management for improved patient outcomes.

Claims

Claims:

1. A dual targeting lipid-based formulation for thyroid drug delivery, comprising lipid-based vesicles coupled with iodine and a cyclic peptide motif (RGDFK).

2. The formulation of claim 1, wherein the RGDFK motif enhances specific binding and internalization of therapeutic agents by selectively targeting av03 integrin receptors overexpressed in thyroid cells.

3. The formulation of claim 1, wherein the iodine coupling technique facilitates increased accumulation of lipid-based vesicles in the thyroid tissue, leveraging the thyroid gland's natural affinity for iodine.

4. A method for enhancing the efficacy of thyroid drug delivery, comprising the steps of coupling iodine to lipid-based vesicles, incorporating a cyclic peptide motif (RGDFK), and selectively targeting av03 integrin receptors in thyroid cells.

5. The method of claim 4, further comprising the step of exploiting the sodiumiodide symporter (NIS) mechanism for enhanced iodine uptake by thyroid cells, thereby optimizing the accumulation of lipid-based vesicles in the thyroid tissue.

6. A dual targeting lipid-based formulation for thyroid drug delivery, as described in claims 1-3, wherein the therapeutic agents encapsulated within the lipid-based vesicles include multivitamins and minerals.

7. The formulation of claim 6, wherein the targeted delivery of multivitamins and minerals addresses specific nutritional deficiencies in the thyroid, supporting overall thyroid health.

8. A pharmaceutical composition comprising the dual targeting lipid-based formulation of claim 1 and a pharmaceutically acceptable carrier or excipient for effective and safe administration.

9. The pharmaceutical composition of claim 8, formulated for oral administration, intravenous injection, or any other suitable route for optimal thyroid drug delivery.

10. Use of the dual targeting lipid-based formulation of claim 1 for the treatment of thyroid disorders, including but not limited to hypothyroidism, hyperthyroidism, goiter, thyroid nodules, and thyroid cancer.

11. The use of claim 10, wherein the targeted delivery of therapeutic agents addresses specific symptoms associated with thyroid disorders, providing improved patient outcomes.

12. A method for manufacturing the dual targeting lipid-based formulation of claim 1, comprising the steps of synthesizing lipid-based vesicles, coupling iodine, incorporating a cyclic peptide motif (RGDFK), and encapsulating therapeutic agents through established pharmaceutical manufacturing processes.

13. The method of claim 12, wherein the manufacturing process ensures the reproducibility and scalability of the dual targeting lipid-based formulation for widespread therapeutic applications.

14. A kit for thyroid drug delivery, comprising the dual targeting lipid-based formulation of claim 1 , instructional materials for administration, and relevant accessories for convenient use.

15. The kit of claim 14, further comprising additional therapeutic agents, allowing customization based on individual patient needs for targeted thyroid treatment.