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Several pharmacological properties are attributed to ergot alkaloids as a result of their antibacterial, antiproliferative, and antioxidant effects. Although known for their biomedical applications (e.g., for the treatment of glaucoma), most ergot alkaloids exhibit high toxicological risk and may even be lethal to humans and animals. Their pharmacological profile results from the structural similarity between lysergic acid-derived compounds and noradrenalin, dopamine, and serotonin neurotransmitters. To reduce their toxicological risk, while increasing their bioavailability, improved delivery systems were proposed. This review discusses the safety aspects of using ergot alkaloids in ocular pharmacology and proposes the development of lipid and polymeric nanoparticles for the topical administration of these drugs to enhance their therapeutic efficacy for the treatment of glaucoma.

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Bergenin (BER), a key constituent of Bergenia crassifolia (Saxifragaceae), has gained extensive attention, owing to its array of pharmacological actions, including anti-infective, anti-cancer, anti-diabetic, neuroprotective, hepatoprotective, anti-urolithiatic, anti-hyperuricemic, and anti-bradykinin properties. Despite ever-intensifying support for its therapeutic features, the poor solubility, lower oral bioavailability, shorter half-life, and more intestinal pH degradation (pH 6.8 or above) of BER have puzzled researchers. To circumvent these pharmaceutical challenges, and to improve its therapeutic efficacy, newer approaches have been adopted by research scientists. Thus, a discussion of the existing literature may provide complete information about the advances in delivery strategies for enhancing its utility. This paper summarizes up-to-date works on the design and development of novel delivery carriers of this bioactive compound, such as phospholipid complexes, extended-release core tablets, prodrugs, herbal gels, polyherbal ointments, nanoparticles, and poly (lactic acid) polymers, with the objective of harnessing its full potential. This review also provides a deep insight into its bioactivities, along with mechanisms. Additionally, the physicochemical attributes, chemistry, and pharmacokinetics of BER are discussed herein. Hence, the comprehensive information documented in this review may introduce new avenues for research advancements of BER.

Background: Acne vulgaris is a chronic inflammatory disorder involving P. acnes (Propionibacterium acnes) and activation of lymphocytes and neutrophils. Dapsone (sulfone drug) possesses potent antimicrobial activities and hence, used to cure multiple inflamed acne lesions. Howbeit, its therapeutic utility is hampered, owing to its poor solubility and side effects like mild irritation and dryness. These problems along with orange brown discoloration on skin restrict topical application of this drug. Objective: The objective of present investigation was to address the above-mentioned limitations like irritation, dryness and skin discoloration of dapsone via formulating microsponge based gel of this moiety. Method: Dapsone microsponges were fabricated and embedded into a carbopol gel for topical application. The ethylcellulose microsponges were crafted employing quasi emulsion solvent diffusion technique. Besides routine characterization, these microformulations were assessed for entrapment, particle size analysis and drug release. Further, anti-acne potential was also evaluated against Propionibacterium acnes and Staphylococcus aureus to check their therapeutic efficiency. Further, the prepared dapsone microsponge gel was evaluated for viscosity, spreadability, texture and drug release. Results: Results revealed that dapsone loaded microsponges were successfully fabricated and found to possess good encapsulation efficiency (84.68 ± 5.73%), which is in micro size range (88.06 ± 2.97 μm to 315.87 ± 1.99 μm) and showed cumulative drug release 52.52 ± 0.2%. Field emission scanning electron microscopy illustrated spherical, uniform and spongy microparticles. The developed microformulation showed promising activity against chosen acne bacterias and improved stability. Conclusion: The obtained results corroborate the premise that dapsone loaded microsponge gel can be an effective strategy for acne management.